Promacta

Thrombopoietin (TPO) Receptor Agonists

Oral Administration

Administer without a meal or with a meal low in calcium (50 mg or less).
Administer at least 2 hours before or 4 hours after other medications (e.g., antacids), calcium-rich foods containing more than 50 mg calcium (e.g., dairy, calcium-fortified juices, certain fruits and vegetables), or supplements containing polyvalent cations such as iron, calcium, aluminum, magnesium, selenium, and zinc.[40392]

Oral Solid Formulations

Swallow tablets whole; do not split, chew, or crush tablets and mix with food or liquids.

Oral Liquid Formulations

Powder for Oral Suspension
Ensure that the enclosed mixing bottle, cap, lid, and oral syringe are dry prior to reconstitution.
Avoid contact of the medication with skin; if contact occurs, wash the area immediately with soap and water. Advise caregivers and/or patients to contact their healthcare provider if a skin reaction occurs.
To prevent staining of skin, consider wearing disposable gloves during preparation and clean up.
Fill the oral dosing syringe with 20 mL of cool or cold drinking water; do not use hot water. Use a new (single-dose) oral dosing syringe to prepare each dose.
Place the water into the mixing bottle and add the powder from the appropriate number of packets for the dose.
Tighten the lid onto the mixing bottle and gently shake for at least 20 seconds; avoid vigorous shaking to prevent the mixture from foaming.
Transfer the mixture into the oral dosing syringe, withdrawing the appropriate volume for the prescribed dose. The reconstituted suspension will be dark brown in color.
Place the tip of the oral dosing syringe into the patient's mouth against the inside of the cheek and slowly eject the dose.
Carefully clean up any spill of the powder or suspension with a damp paper towel or disposable cloth. Rinse the mixing bottle and lid and allow to air dry.
Storage: Administer immediately; discard the mixture if not used within 30 minutes of reconstitution. May be stored at room temperature (20 to 25 degrees C [68 to 77 degrees F]) for up to 30 minutes. Discard remaining admixture in the mixing bottle in the trash. Do not pour down the drain. Discard the used oral dosing syringe.[40392]

Severe

thromboembolism / Delayed / 0-6.0
thrombotic microangiopathy / Delayed / 0-1.0
renal failure (unspecified) / Delayed / 0-1.0
hepatotoxicity / Delayed / Incidence not known
hepatic decompensation / Delayed / Incidence not known

Moderate

dyspnea / Early / 14.0-14.0
cataracts / Delayed / 2.0-11.0
peripheral edema / Delayed / 10.0-10.0
hyperbilirubinemia / Delayed / 6.0
elevated hepatic enzymes / Delayed / 10.0
ascites / Delayed / Incidence not known
encephalopathy / Delayed / Incidence not known

Mild

nausea / Early / 4.0-33.0
fever / Early / 9.0-30.0
fatigue / Early / 4.0-28.0
cough / Delayed / 9.0-23.0
diarrhea / Early / 5.0-21.0
headache / Early / 10.0-21.0
anorexia / Delayed / 18.0-18.0
influenza / Delayed / 3.0-18.0
infection / Delayed / 5.0-17.0
insomnia / Early / 16.0-16.0
asthenia / Delayed / 16.0-16.0
pruritus / Rapid / 15.0-15.0
dizziness / Early / 14.0-14.0
chills / Rapid / 14.0-14.0
abdominal pain / Early / 8.0-12.0
pharyngitis / Delayed / 4.0-12.0
rhinorrhea / Early / 4.0-12.0
muscle cramps / Delayed / 12.0-12.0
arthralgia / Delayed / 12.0-12.0
myalgia / Early / 5.0-12.0
ecchymosis / Delayed / 12.0-12.0
rash / Early / 3.0-12.0
rhinitis / Early / 9.0-11.0
alopecia / Delayed / 10.0-10.0
vomiting / Early / 6.0-6.0
dental pain / Delayed / 6.0-6.0
skin hyperpigmentation / Delayed / 5.0-5.0
paresthesias / Delayed / 3.0-3.0
back pain / Delayed / 3.0-3.0

Hepatic decompensation, hepatic disease, hepatitis C infection, hepatotoxicity, hypoalbuminemia

Eltrombopag may increase the risk of severe and potentially life-threatening hepatotoxicity; use with caution in any patient with preexisting hepatic disease. In patients with chronic hepatitis C infection, use of eltrombopag in combination with interferon and ribavirin may increase the risk of hepatic decompensation. This risk is further increased in those with hypoalbuminemia (albumin less than 3.5 g/dL) or a Model for End-Stage Liver Disease (MELD) score of 10 or more at baseline. In patients being treated for ITP, chronic hepatitis C-associated thrombocytopenia, and refractory severe aplastic anemia measure serum ALT, AST, and bilirubin at baseline, every 2 weeks during dose adjustment, and then monthly once a stable dose is achieved. If bilirubin is elevated, fractionation should be performed. Evaluate abnormalities with repeat testing in 3 to 5 days. If confirmed, monitor liver function tests (LFTs) weekly until the abnormalities resolve or stabilize. Discontinue eltrombopag if ALT increases to 3 times or more the upper limit of normal (ULN) in patients with normal liver function. In patients with pretreatment transaminase elevations, discontinue eltrombopag if ALT increases 3 times or more baseline (or more than 5 times the ULN, whichever is less) and are either progressively increasing, persistent for 4 weeks or more, accompanied by increased direct bilirubin, or accompanied by clinical symptoms of liver injury or evidence of hepatic decompensation. Consider reinitiating eltrombopag only if the potential benefit outweighs the risk of hepatoxicity. If reinitiated, monitor LFTs weekly during the dose adjustment phase. Permanently discontinue treatment if LFT abnormalities persist, worsen, or recur. When eltrombopag is used as first-line treatment for severe aplastic anemia, measure ALT, AST, and bilirubin at baseline, every other day while hospitalized for horse antithymocyte (h-ATG) therapy, and then every 2 weeks during treatment. If baseline ALT or AST concentrations are more than 6 times the ULN, do not initiate eltrombopag until values decline to less than 5 times the ULN. If ALT or AST increase to more than 6 times the ULN during treatment, discontinue eltrombopag and reinitiate at the same dose when values decline to less than 5 time the ULN. If ALT or AST increase to more than 6 times the ULN after reinitiation, discontinue treatment and monitor LFTs at least every 3 to 4 days. Reinitiate eltrombopag at a reduced daily dose once ALT and AST are less than 5 times the ULN. If ALT or AST return to values more than 6 times the ULN on the reduced dose, reduce the daily dose until ALT or AST is less than 5 times the ULN.[40392]

Promacta

Rx

Oral non-peptide thrombopoietin receptor agonist
Used for thrombocytopenia in patients with persistent or chronic immune thrombocytopenia or chronic hepatitis C infection and for severe aplastic anemia
May increase the risk of severe and potentially life-threatening hepatotoxicity

For the treatment of thrombocytopenia in patients with chronic hepatitis C to allow the initiation and maintenance of interferon-based therapy. Oral dosage Adults

25 mg PO once daily initially; adjust dose by 25 mg/day PO every 2 weeks as necessary to achieve the target platelet count. During antiviral therapy, adjust dose based on platelet count to avoid dose reductions of peginterferon. For platelets less than 50,000/mm3 after 2 weeks of treatment, increase the dose by 25 mg/day PO; do not exceed 100 mg/day PO. For platelets 50,000/mm3 to less than 200,000/mm3, continue current dose. For platelets 200,000 to 400,000/mm3 at any time, decrease the dose by 25 mg/day PO; wait 2 weeks to assess the effects of any dosage adjustments. For platelets more than 400,000/mm3, stop therapy; increase frequency of platelet monitoring to twice weekly. Once the platelet count is less than 150,000/mm3, reinitiate therapy at a dose reduced by 25 mg/day PO. For patients taking 25 mg once daily, reinitiate therapy at 12.5 mg/day PO. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Discontinue eltrombopag when antiviral therapy is discontinued. Platelet counts generally begin to rise within the first week of treatment. Use the lowest dose to achieve and maintain a platelet count necessary to initiate and maintain antiviral therapy with pegylated interferon and ribavirin; however, do not use eltrombopag to normalize platelet counts.[40392]

For the treatment of persistent or chronic immune thrombocytopenic purpura (ITP) in patients who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy and whose degree of thrombocytopenia and clinical condition increase the risk of bleeding.
NOTE: Eltrombopag has been designated orphan drug status for this indication.
Oral dosage Adults

50 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 25 mg PO once daily. Adjust the dose based on platelet count. For platelets less than 50,000/mm3 after 2 weeks of treatment, increase the dose by 25 mg/day PO; do not exceed 75 mg/day PO. For patients taking 12.5 mg/day, increase the dose to 25 mg/day before increasing the dose by 25 mg. For platelets 50,000/mm3 to less than 200,000/mm3, continue current dose. For platelets 200,000 to 400,000/mm3, decrease the dose by 25 mg/day PO; wait 2 weeks to assess the effects of any dosage adjustments. For patients taking 25 mg once daily, decrease dose to 12.5 mg/day PO. For platelets more than 400,000/mm3, stop therapy; increase frequency of platelet monitoring to twice weekly. Once the platelet count is less than 150,000/mm3, reinitiate therapy at a dose reduced by 25 mg/day PO. For patients taking 25 mg once daily, reinitiate therapy at 12.5 mg/day PO. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Platelet counts generally increase within 1 to 2 weeks of initiation and decrease within 1 to 2 weeks of discontinuation. Use the lowest possible dose to maintain platelet counts of 50,000/mm3 or more and prevent clinically important bleeding; however, do not use eltrombopag to normalize platelet concentrations. When switching between the oral suspension and the tablet, monitor platelet counts weekly for 2 weeks, and then monthly.[40392]

Children and Adolescents 6 to 17 years

50 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 25 mg PO once daily. Adjust the dose based on platelet count. For platelets less than 50,000/mm3 after 2 weeks of treatment, increase the dose by 25 mg/day PO; do not exceed 75 mg/day PO. For patients taking 12.5 mg/day, increase the dose to 25 mg/day before increasing the dose by 25 mg. For platelets 50,000/mm3 to less than 200,000/mm3, continue current dose. For platelets 200,000 to 400,000/mm3, decrease the dose by 25 mg/day PO; wait 2 weeks to assess the effects of any dosage adjustments. For patients taking 25 mg once daily, decrease dose to 12.5 mg/day PO. For platelets more than 400,000/mm3, stop therapy; increase frequency of platelet monitoring to twice weekly. Once the platelet count is less than 150,000/mm3, reinitiate therapy at a dose reduced by 25 mg/day PO. For patients taking 25 mg once daily, reinitiate therapy at 12.5 mg/day PO. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Platelet counts generally increase within 1 to 2 weeks of initiation and decrease within 1 to 2 weeks of discontinuation. Use the lowest possible dose to maintain platelet counts of 50,000/mm3 or more and prevent clinically important bleeding; however, do not use eltrombopag to normalize platelet concentrations. When switching between the oral suspension and the tablet, monitor platelet counts weekly for 2 weeks, and then monthly.[40392]

Children 1 to 5 years

25 mg PO once daily initially. Adjust the dose based on platelet count. For platelets less than 50,000/mm3 after 2 weeks of treatment, increase the dose by 25 mg/day PO; do not exceed 75 mg/day PO. For patients taking 12.5 mg/day, increase the dose to 25 mg/day before increasing the dose by 25 mg. For platelets 50,000/mm3 to less than 200,000/mm3, continue current dose. For platelets 200,000 to 400,000/mm3, decrease the dose by 25 mg/day PO; wait 2 weeks to assess the effects of any dosage adjustments. For patients taking 25 mg once daily, decrease dose to 12.5 mg/day PO. For platelets more than 400,000/mm3, stop therapy; increase frequency of platelet monitoring to twice weekly. Once the platelet count is less than 150,000/mm3, reinitiate therapy at a dose reduced by 25 mg/day PO. For patients taking 25 mg once daily, reinitiate therapy at 12.5 mg/day PO. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Platelet counts generally increase within 1 to 2 weeks of initiation and decrease within 1 to 2 weeks of discontinuation. Use the lowest possible dose to maintain platelet counts of 50,000/mm3 or more and prevent clinically important bleeding; however, do not use eltrombopag to normalize platelet concentrations. When switching between the oral suspension and the tablet, monitor platelet counts weekly for 2 weeks, and then monthly.[40392]

For the treatment of severe aplastic anemia. For the treatment of severe aplastic anemia in patients who have had an insufficient response to immunosuppressive therapy. Oral dosage Adults

50 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 25 mg PO once daily. Adjust dose by 50 mg/day PO every 2 weeks as necessary to achieve a target platelet count of 50,000/mm3 or more; do not exceed 150 mg/day PO. For platelets less than 50,000/mm3 after at least 2 weeks of treatment, increase the dose by 50 mg/day; in those taking 25 mg/day, increase the dose to 50 mg/day before increasing the dose by 50 mg. For platelets 50,000/mm3 to less than 200,000/mm3, continue current dose. For platelets 200,000 to 400,000/mm3, decrease the dose by 50 mg/day; wait 2 weeks to assess the effects of any dosage adjustments. For platelets more than 400,000/mm3, stop therapy for 1 week. Once the platelet count is less than 150,000/mm3, reinitiate therapy at a dose reduced by 50 mg/day. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Reduce the dose by 50% in patients who achieve tri-lineage response, including transfusion independence, lasting at least 8 weeks. Discontinue and monitor blood counts if counts remain stable for 8 weeks at reduced dose. Reinitiate at previous effective dose if platelet counts drop to less than 30,000/mm3, hemoglobin less than 9 g/dL, or ANC less than 500/mm3. Discontinue if no hematologic response has occurred after 16 weeks of therapy; consider discontinuation if new cytogenic abnormalities occur. Use the lowest dose to achieve and maintain a hematologic response.[40392]

For the first-line treatment of severe aplastic anemia in combination with standard immunosuppressive therapy. Oral dosage Adults

150 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 75 mg PO once daily. Do not exceed 150 mg/day PO; treat for 6 months. Monitor hematologic and hepatic tests regularly and adjust the dose as necessary. For platelets 200,000 to 400,000/mm3, decrease the dose by 25 mg/day every 2 weeks to the lowest dose that maintains a platelet count of 50,000/mm3 or more. For platelets more than 400,000/mm3, stop therapy for 1 week. Once the platelet count is less than 200,000/mm3, reinitiate at a dose reduced by 25 mg/day. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Discontinue eltrombopag but continue horse antithymocyte globulin (h-ATG) and cyclosporine if thromboembolic events occur.[40392]

Children and Adolescents 12 to 17 years

150 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 75 mg PO once daily. Do not exceed 150 mg/day PO; treat for 6 months. Monitor hematologic and hepatic tests regularly and adjust the dose as necessary. For platelets 200,000 to 400,000/mm3, decrease the dose by 25 mg/day every 2 weeks to the lowest dose that maintains a platelet count of 50,000/mm3 or more. For platelets more than 400,000/mm3, stop therapy for 1 week. Once the platelet count is less than 200,000/mm3, reinitiate at a dose reduced by 25 mg/day. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Discontinue eltrombopag but continue horse antithymocyte globulin (h-ATG) and cyclosporine if thromboembolic events occur.[40392]

Children 6 to 11 years

75 mg PO once daily initially; for patients of East/Southeast-Asian ancestry, 37.5 mg PO once daily. Do not exceed 75 mg/day PO; treat for 6 months. Monitor hematologic and hepatic tests regularly and adjust the dose as necessary. For platelets 200,000 to 400,000/mm3, decrease the dose by 12.5 mg/day every 2 weeks to the lowest dose that maintains a platelet count of 50,000/mm3 or more. For platelets more than 400,000/mm3, stop therapy for 1 week. Once the platelet count is less than 200,000/mm3, reinitiate at a dose reduced by 12.5 mg/day. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Discontinue eltrombopag but remain on horse antithymocyte globulin (h-ATG) and cyclosporine if thromboembolic events occur.[40392]

Children 2 to 5 years

2.5 mg/kg/dose PO once daily initially; for patients of East/Southeast-Asian ancestry, 1.25 mg/kg/dose PO once daily. Do not exceed 2.5 mg/kg/day; treat for 6 months. Monitor hematologic and hepatic tests regularly and adjust the dose as necessary. For platelets 200,000 to 400,000/mm3, decrease the dose by 12.5 mg/day every 2 weeks to the lowest dose that maintains a platelet count of 50,000/mm3 or more. For platelets more than 400,000/mm3, stop therapy for 1 week. Once the platelet count is less than 200,000/mm3, reinitiate at a dose reduced by 12.5 mg/day. If platelets are more than 400,000/mm3 after 2 weeks of the lowest dose, discontinue eltrombopag. Discontinue eltrombopag but remain on horse antithymocyte globulin (h-ATG) and cyclosporine if thromboembolic events occur.[40392]

Hepatic Impairment

Patients with mild to severe hepatic impairment (Child-Pugh Class A, B, or C) treated for ITP, chronic hepatitis C-associated thrombocytopenia, and refractory severe aplastic anemia:
Patients with hepatitis C: No dose adjustment needed.
Patients with ITP: Reduce the initial dose to 25 mg PO once daily and do not increase the dose more frequently than every 3 weeks. Consider reducing the initial dose to 12.5 mg once daily for patients of East/Southeast-Asian ancestry.
Patients with refractory severe aplastic anemia: Reduce the initial dose to 25 mg PO once daily.
Monitor ALT, AST, and bilirubin at baseline, every 2 weeks during dose adjustment, and monthly after the establishment of a stable dose. If abnormalities are confirmed, monitor weekly until resolved or stabilized. Discontinue eltrombopag if ALT concentrations increase to 3 times or more the upper limit of normal (ULN) in patients with normal liver function at baseline. In patients with pretreatment elevations in transaminases, discontinue eltrombopag if ALT concentrations increase to 3 times or more baseline (or more than 5 times ULN, whichever is least) and the increases are progressive, persistent for 4 weeks or more, or accompanied by increased direct bilirubin, clinical symptoms of liver injury, or evidence of hepatic decompensation.[40392]
 
Patients with mild to severe hepatic impairment (Child-Pugh Class A, B, or C) treated for severe aplastic anemia first-line:
Do not initiate treatment until transaminase concentrations are less than 5 times the ULN. Monitor ALT, AST, and bilirubin at baseline, every other day while hospitalized for horse antithymocyte (h-ATG) therapy, and every 2 weeks afterward.
12 years and older: Reduce the initial dose to 75 mg PO once daily.
6 to 11 years: Reduce the initial dose to 37.5 mg PO once daily.
2 to 5 years: Reduce the initial dose to 1.25 mg/kg PO once daily.
Discontinue eltrombopag if ALT/AST concentrations increase more than 6 times the ULN; may reinitiate treatment at the same dose once the AST/ALT is less than 5 times the ULN. If concentrations increase more than 6 times the ULN after reinitiation, discontinue eltrombopag and monitor liver function at least every 3 to 4 days. Once ALT/AST are less than 5 times the ULN, reinitiate treatment at a dose reduced by 25 mg/day compared to the previous dose. If the ALT/AST returns to more than 6 times the ULN on the reduced dose, reduce the dose by 25 mg/day until the ALT/AST is less than 5 times the ULN. In patients younger than 12 years, reduce the daily dose by at least 15% to the nearest dose that can be administered.[40392]

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Acetaminophen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Aspirin, ASA; Caffeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Aspirin: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Aspirin; Diphenhydramine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Caffeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Caffeine; Dihydrocodeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Caffeine; Pyrilamine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Chlorpheniramine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Chlorpheniramine; Dextromethorphan: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Chlorpheniramine; Phenylephrine : (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Codeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan; Doxylamine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan; Guaifenesin; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan; Phenylephrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dextromethorphan; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Dichloralphenazone; Isometheptene: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Diphenhydramine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Guaifenesin; Phenylephrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Hydrocodone: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Ibuprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered. (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Acetaminophen; Oxycodone: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Pamabrom; Pyrilamine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Phenylephrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Acetaminophen; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Alpelisib: (Major) Avoid coadministration of alpelisib with eltrombopag due to increased exposure to alpelisib and the risk of alpelisib-related toxicity. If concomitant use is unavoidable, closely monitor for alpelisib-related adverse reactions. Alpelisib is a BCRP substrate and eltrombopag is a BCRP inhibitor.
Aluminum Hydroxide: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Aluminum Hydroxide; Magnesium Carbonate: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Aluminum Hydroxide; Magnesium Hydroxide: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Aluminum Hydroxide; Magnesium Hydroxide; Simethicone: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Aluminum Hydroxide; Magnesium Trisilicate: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Amlodipine; Atorvastatin: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as atorvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Amlodipine; Celecoxib: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Amlodipine; Olmesartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and olmesartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as olmesartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Amlodipine; Valsartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Amlodipine; Valsartan; Hydrochlorothiazide, HCTZ: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Amobarbital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Amoxicillin; Clarithromycin; Omeprazole: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as omeprazole, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Anticoagulants: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Antithrombin III: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Apixaban: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Argatroban: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Aspirin, ASA; Butalbital; Caffeine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Aspirin, ASA; Citric Acid; Sodium Bicarbonate: (Major) Eltrombopag chelates polyvalent cations (e.g., antacids) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as magaldrate.
Aspirin, ASA; Omeprazole: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as omeprazole, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Atazanavir: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering weak inhibitors of CYP2C8, such as atazanavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Atazanavir; Cobicistat: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering weak inhibitors of CYP2C8, such as atazanavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Atogepant: (Major) Limit the dose of atogepant to 10 or 30 mg PO once daily for episodic migraine or 30 mg PO once daily for chronic migraine if coadministered with eltrombopag. Concurrent use may increase atogepant exposure and the risk of adverse effects. Atogepant is a substrate of OATP1B1 and OATP1B3 and eltrombopag is an OATP inhibitor. Coadministration with an OATP1B1/3 inhibitor resulted in a 2.85-fold increase in atogepant overall exposure and a 2.23-fold increase in atogepant peak concentration.
Atorvastatin: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as atorvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Atorvastatin; Ezetimibe: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as atorvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered. (Moderate) Use caution and monitor for adverse reactions if eltrombopag and ezetimibe are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as ezetimibe, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Barbiturates: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Bempedoic Acid; Ezetimibe: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and ezetimibe are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as ezetimibe, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Benzhydrocodone; Acetaminophen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Berotralstat: (Major) Reduce the berotralstat dose to 110 mg PO once daily in patients chronically taking eltrombopag. Concurrent use may increase berotralstat exposure and the risk of adverse effects. Berotralstat is a BCRP substrate and eltrombopag is a BCRP inhibitor. Coadministration with another BCRP inhibitor increased berotralstat exposure by 69%.
Betrixaban: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Bivalirudin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Bosentan: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and bosentan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as bosentan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Brincidofovir: (Moderate) Postpone the administration of eltrombopag for at least three hours after brincidofovir administration and increase monitoring for brincidofovir-related adverse reactions (i.e., elevated hepatic enzymes and bilirubin, diarrhea, other gastrointestinal adverse events) if concomitant use of brincidofovir and eltrombopag is necessary. Brincidofovir is an OATP1B1 substrate and eltrombopag is an OATP1B1 inhibitor. In a drug interaction study, the mean AUC and Cmax of brincidofovir increased by 374% and 269%, respectively, when administered with another OATP1B1 inhibitor.
Bupivacaine; Meloxicam: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Butabarbital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Butalbital; Acetaminophen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered. (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Butalbital; Acetaminophen; Caffeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered. (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Butalbital; Acetaminophen; Caffeine; Codeine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered. (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Butalbital; Aspirin; Caffeine; Codeine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Calcium: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Carbamazepine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as carbamazepine, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Celecoxib: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Celecoxib; Tramadol: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Chlorpheniramine; Ibuprofen; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Chlorpheniramine; Pseudoephedrine: (Major) Eltrombopag chelates polyvalent cations (e.g., zinc salts) in foods, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag 2 hours before or 4 hours after any oral products containing zinc salts.
Cimetidine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inhibitors of CYP1A2, such as cimetidine, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Ciprofloxacin: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inhibitors of CYP1A2, such as ciprofloxacin, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Dabigatran: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Dalteparin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Desirudin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Diclofenac: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Diclofenac; Misoprostol: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Diflunisal: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Diphenhydramine; Ibuprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Diphenhydramine; Naproxen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Edoxaban: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Elagolix: (Contraindicated) Concomitant use of elagolix and strong organic anion transporting polypeptide (OATP) 1B1 inhibitors such as eltrombopag is contraindicated. Use of elagolix with drugs that inhibit OATP1B1 may increase elagolix plasma concentrations. Elagolix is a substrate of CYP3A, P-gp, and OATP1B1. Eltrombopag is an inhibitor of OATP1B1 in vitro and can increase the systemic exposure of other drugs that are substrates of OATP1B1. Increased elagolix concentrations increase the risk for dose-related side effects, including loss of bone mineral density.
Elagolix; Estradiol; Norethindrone acetate: (Contraindicated) Concomitant use of elagolix and strong organic anion transporting polypeptide (OATP) 1B1 inhibitors such as eltrombopag is contraindicated. Use of elagolix with drugs that inhibit OATP1B1 may increase elagolix plasma concentrations. Elagolix is a substrate of CYP3A, P-gp, and OATP1B1. Eltrombopag is an inhibitor of OATP1B1 in vitro and can increase the systemic exposure of other drugs that are substrates of OATP1B1. Increased elagolix concentrations increase the risk for dose-related side effects, including loss of bone mineral density.
Eluxadoline: (Major) When administered concurrently with eltrombopag, the dose of eluxadoline must be reduced to 75 mg PO twice daily, and the patient should be closely monitored for eluxadoline-related adverse effects (i.e., decreased mental and physical acuity). Eluxadoline is a substrate of the organic anion-transporting peptide (OATP1B1); eltrombopag is an in vitro inhibitor of OATP1B1. Advise patients against driving or operating machinery until the combine effects of these drugs on the individual patient is known.
Enoxaparin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Etodolac: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ezetimibe: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and ezetimibe are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as ezetimibe, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Ezetimibe; Simvastatin: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and ezetimibe are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as ezetimibe, may exhibit an increase in systemic exposure if coadministered with eltrombopag. (Moderate) Use caution and monitor for adverse reactions if eltrombopag and simvastatin are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as simvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Fenoprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Fexofenadine: (Moderate) Monitor patients for fexofenadine adverse reactions if coadministered with eltrombopag. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as fexofenadine, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Fexofenadine; Pseudoephedrine: (Moderate) Monitor patients for fexofenadine adverse reactions if coadministered with eltrombopag. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as fexofenadine, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Flurbiprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Fluvastatin: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as fluvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Fluvoxamine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inhibitors of CYP1A2, such as fluvoxamine, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Fondaparinux: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Food: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food. Systemic exposure to eltrombopag may be decreased when it is coadministered with a polyvalent cation-containing product. Eltrombopag should not be taken within 4 hours of any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts. (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food. Systemic exposure to eltrombopag may be decreased when it is coadministered with a polyvalent cation-containing product. Eltrombopag should not be taken within 4 hours of any oral products containing polyvalent cations, such as calcium salts.
Gemfibrozil: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering inhibitors of CYP2C8, such as gemfibrozil, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Glecaprevir; Pibrentasvir: (Moderate) Caution is advised with the coadministration of glecaprevir and eltrombopag as coadministration may increase serum concentrations of glecaprevir and increase the risk of adverse effects. Glecaprevir is a substrate of organic anion transporting polypeptide (OATP) 1B1 and breast cancer resistance protein (BCRP); eltrombopag is an inhibitor of OATP1B1 and BCRP. (Moderate) Caution is advised with the coadministration of pibrentasvir and eltrombopag as coadministration may increase serum concentrations of pibrentasvir and increase the risk of adverse effects. Pibrentasvir is a substrate of breast cancer resistance protein (BCRP); eltrombopag is an inhibitor of BCRP.
Glyburide: (Moderate) Use caution and monitor blood glucose carefully if eltrombopag and glyburide are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as glyburide, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Glyburide; Metformin: (Moderate) Use caution and monitor blood glucose carefully if eltrombopag and glyburide are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as glyburide, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Heparin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Hydrocodone; Ibuprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ibuprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ibuprofen; Famotidine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ibuprofen; Oxycodone: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ibuprofen; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Imatinib: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and imatinib, STI-571 are coadministered. Eltrombopag is an inhibitor of Breast Cancer Resistance Protein (BCRP). Drugs that are substrates for this transporter, such as imatinib, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Indomethacin: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Iron: (Major) Eltrombopag chelates polyvalent cations (e.g., iron) in foods and mineral supplements. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as iron salts, multivitamins that contain iron, or polysaccharide-iron complex.
Isoniazid, INH; Pyrazinamide, PZA; Rifampin: (Major) Eltrombopag is metabolized by CYP1A2 and CYP2C8. The significance of administering inducers of CYP1A2 and CYP2C8, such as rifampin, on the systemic exposure of eltrombopag has not been established. Additionally, eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as rifampin, may exhibit an increase in systemic exposure if coadministered with eltrombopag. Monitor patients for a decrease in the efficacy of eltrombopag and for an increase in adverse reactions of rifampin if these drugs are coadministered.
Isoniazid, INH; Rifampin: (Major) Eltrombopag is metabolized by CYP1A2 and CYP2C8. The significance of administering inducers of CYP1A2 and CYP2C8, such as rifampin, on the systemic exposure of eltrombopag has not been established. Additionally, eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as rifampin, may exhibit an increase in systemic exposure if coadministered with eltrombopag. Monitor patients for a decrease in the efficacy of eltrombopag and for an increase in adverse reactions of rifampin if these drugs are coadministered.
Ketoprofen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Ketorolac: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Lapatinib: (Moderate) Use caution and monitor for signs of lapatinib toxicity if these drugs are coadministered; a lapatinib dosage reduction may be necessary.
Letermovir: (Moderate) Closely monitor for letermovir-related adverse events (i.e., tachycardia, atrial fibrillation, and gastrointestinal events) if administered with eltrombopag, as use of these drugs together may result in elevated letermovir plasma concentration. Letermovir is a substrate of the organic anion-transporting polypeptide (OATP1B1); eltrombopag is an inhibitor of OATP1B1.
Lopinavir; Ritonavir: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as ritonavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Magnesium: (Major) Eltrombopag chelates polyvalent cations (e.g., calcium, aluminum, and magnesium) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as aluminum salts, (like aluminum hydroxide), calcium salts, (including calcium carbonate), and magnesium salts.
Maraviroc: (Moderate) Use caution and closely monitor for increased adverse effects during concurrent administration of maraviroc and eltrombopag as increased maraviroc concentrations may occur. Maraviroc is a substrate of organic anion-transporting polypeptide (OATP1B1); eltrombopag is an inhibitor of OATP1B1. The effects of this transporter on the concentrations of maraviroc are unknown, although an increase in concentrations and thus, toxicity, are possible.
Meclofenamate Sodium: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Mefenamic Acid: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Meloxicam: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Metformin; Repaglinide: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as repaglinide, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Methohexital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Methotrexate: (Moderate) Eltrombopag is an inhibitor of OATP1B1 and Breast Cancer Resistance Protein (BCRP). Drugs that are substrates for these transporters, such as methotrexate, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for increased methotrexate toxicity if these drugs are coadministered. In a clinical study, administration of a single dose of rosuvastatin, another substrate of both OATP1B1 and BCRP, in combination with eltrombopag increased plasma rosuvastatin AUC by 55% and the Cmax by 103%. A 50% rosuvastatin dosage reduction was recommended.
Mexiletine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inhibitors of CYP1A2, such as mexiletine, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Mitoxantrone: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and mitoxantrone are coadministered. Eltrombopag is an inhibitor of Breast Cancer Resistance Protein (BCRP). Drugs that are substrates for this transporter, such as mitoxantrone, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Nabumetone: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Naproxen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Naproxen; Esomeprazole: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Naproxen; Pseudoephedrine: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Nateglinide: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as nateglinide, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Nebivolol; Valsartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Niacin; Simvastatin: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and simvastatin are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as simvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Nirmatrelvir; Ritonavir: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as ritonavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Nonsteroidal antiinflammatory drugs: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Olmesartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and olmesartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as olmesartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Olmesartan; Amlodipine; Hydrochlorothiazide, HCTZ: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and olmesartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as olmesartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Olmesartan; Hydrochlorothiazide, HCTZ: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and olmesartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as olmesartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Omeprazole: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as omeprazole, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Omeprazole; Amoxicillin; Rifabutin: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as omeprazole, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Omeprazole; Sodium Bicarbonate: (Major) Eltrombopag chelates polyvalent cations (e.g., antacids) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as magaldrate. (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as omeprazole, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Oxaprozin: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Paclitaxel: (Moderate) Monitor patients for paclitaxel adverse reactions if coadministered with eltrombopag. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as paclitaxel, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Pazopanib: (Major) Avoid administering pazopanib with strong breast cancer resistance protein (BCRP) inhibitors, such as eltrombopag. The concomitant use of pazopanib, a BCRP substrate,and eltrombopag, a BCRP inhibitor, may result in increased pazopanib concentrations.
Pentobarbital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Pentosan: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Phenobarbital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Piroxicam: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Pitavastatin: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and pitavastatin are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as pitavastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Pravastatin: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as pravastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Primidone: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Quinine: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as quinine, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Repaglinide: (Moderate) Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as repaglinide, may exhibit an increase in systemic exposure if coadministered with eltrombopag; monitor patients for adverse reactions if these drugs are coadministered.
Revefenacin: (Major) Coadministration of revefenacin is not recommended with eltrombopag because it could lead to an increase in systemic exposure of the active metabolite of revefenacin and an increased potential for anticholinergic adverse effects. The active metabolite of revefenacin is a substrate of OATP1B1 and OATP1B3; eltrombopag is an inhibitor of OATP1B1.
Rifampin: (Major) Eltrombopag is metabolized by CYP1A2 and CYP2C8. The significance of administering inducers of CYP1A2 and CYP2C8, such as rifampin, on the systemic exposure of eltrombopag has not been established. Additionally, eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as rifampin, may exhibit an increase in systemic exposure if coadministered with eltrombopag. Monitor patients for a decrease in the efficacy of eltrombopag and for an increase in adverse reactions of rifampin if these drugs are coadministered.
Ritonavir: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as ritonavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Rivaroxaban: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Rosuvastatin: (Moderate) Use caution and monitor for signs of rosuvastatin toxicity if this drug is coadministered with eltrombopag. In clinical trials, a 50% dose reduction of rosuvastatin was recommended. Eltrombopag is an inhibitor of OATP1B1 and BCRP, and rosuvastatin is a substrate of both of these transporters. In a clinical study, administration of a single dose of rosuvastatin with eltrombopag increased plasma rosuvastatin AUC by 55% and the Cmax by 103%.
Rosuvastatin; Ezetimibe: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and ezetimibe are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as ezetimibe, may exhibit an increase in systemic exposure if coadministered with eltrombopag.

(Moderate) Use caution and monitor for signs of rosuvastatin toxicity if this drug is coadministered with eltrombopag. In clinical trials, a 50% dose reduction of rosuvastatin was recommended. Eltrombopag is an inhibitor of OATP1B1 and BCRP, and rosuvastatin is a substrate of both of these transporters. In a clinical study, administration of a single dose of rosuvastatin with eltrombopag increased plasma rosuvastatin AUC by 55% and the Cmax by 103%.
Sacubitril; Valsartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Secobarbital: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as barbiturates, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Selenium: (Major) Eltrombopag chelates polyvalent cations (e.g., selenium) in foods, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag 2 hours before or 4 hours after any oral products containing selenium.
Simvastatin: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and simvastatin are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as simvastatin, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Sodium Bicarbonate: (Major) Eltrombopag chelates polyvalent cations (e.g., antacids) in food, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag at least 2 hours before or 4 hours after any oral products containing polyvalent cations, such as magaldrate.
Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering inhibitors of CYP2C8, such as trimethoprim, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Sulfasalazine: (Moderate) Use caution and monitor for adverse reactions if eltrombopag and sulfasalazine are coadministered. Eltrombopag is an inhibitor of Breast Cancer Resistance Protein (BCRP). Drugs that are substrates for this transporter, such as sulfasalazine, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Sulindac: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Sumatriptan; Naproxen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Talazoparib: (Moderate) Monitor for an increase in talazoparib-related adverse reactions if concomitant use of eltrombopag is necessary. Concomitant use may increase talazoparib exposure. Talazoparib is a BCRP substrate and eltrombopag is a BCRP inhibitor.
Teriflunomide: (Moderate) In vitro studies indicate that teriflunomide is a substrate of ABCG2 (breast cancer resistance protein, BCRP). Drugs that are inhibitors of BCRP, such as eltrombopag, may cause increases in teriflunomide plasma concentrations. Monitor patients for adverse effects, including symptoms serious liver injury and immunosuppression.
Tipranavir: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inducers of CYP1A2, such as tipranavir, on the systemic exposure of eltrombopag has not been established. Monitor patients for a decrease in the efficacy of eltrombopag if these drugs are coadministered.
Tolmetin: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Topotecan: (Major) Avoid coadministration of eltrombopag with oral topotecan due to increased topotecan exposure; eltrombopag may be administered with intravenous topotecan. Oral topotecan is a substrate of the Breast Cancer Resistance Protein (BCRP) and eltrombopag is a BCRP inhibitor. Coadministration increases the risk of topotecan-related adverse reactions.
Tramadol; Acetaminophen: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. Acetaminophen is a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of acetaminophen are possible. Monitor patients for adverse reactions if these drugs are coadministered.
Trimethoprim: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering inhibitors of CYP2C8, such as trimethoprim, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Ubrogepant: (Major) Limit the initial and second dose of ubrogepant to 50 mg if coadministered with eltrombopag. Concurrent use may increase ubrogepant exposure and the risk of adverse effects. Ubrogepant is a substrate of the BCRP drug transporter; eltrombopag is a BCRP inhibitor.
Valdecoxib: (Moderate) Eltrombopag is a UDP-glucuronyltransferase inhibitor. NSAIDs are a substrate of UDP-glucuronyltransferases. The significance or effect of this interaction is not known; however, elevated concentrations of the NSAID are possible. Monitor patients for adverse reactions if eltrombopag is administered with an NSAID.
Valsartan: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Valsartan; Hydrochlorothiazide, HCTZ: (Moderate) Use caution and monitor blood pressure closely if eltrombopag and valsartan are coadministered. Eltrombopag is an inhibitor of the transporter OATP1B1. Drugs that are substrates for this transporter, such as valsartan, may exhibit an increase in systemic exposure if coadministered with eltrombopag.
Warfarin: (Moderate) Use caution when discontinuing eltrombopag in patients receiving anticoagulants (e.g., warfarin, enoxaparin, dabigatran, rivaroxaban). The risk of bleeding and recurrent thrombocytopenia is increased in patients receiving these drugs when eltrombopag is discontinued.
Zafirlukast: (Moderate) Eltrombopag is metabolized by CYP2C8. The significance of administering inhibitors of CYP2C8, such as zafirlukast, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Zileuton: (Moderate) Eltrombopag is metabolized by CYP1A2. The significance of administering inhibitors of CYP1A2, such as zileuton, on the systemic exposure of eltrombopag has not been established. Monitor patients for signs of eltrombopag toxicity if these drugs are coadministered.
Zinc Salts: (Major) Eltrombopag chelates polyvalent cations (e.g., zinc salts) in foods, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag 2 hours before or 4 hours after any oral products containing zinc salts.
Zinc: (Major) Eltrombopag chelates polyvalent cations (e.g., zinc salts) in foods, mineral supplements, and antacids. In a clinical study, systemic exposure to eltrombopag was decreased by 70% when it was administered with a polyvalent cation-containing antacid. Administer eltrombopag 2 hours before or 4 hours after any oral products containing zinc salts.

Eltrombopag/Promacta Oral Pwd F/Recon: 12.5mg, 25mg
Promacta Oral Tab: 12.5mg, 25mg, 50mg, 75mg

Adults

75 mg/day PO for idiopathic thrombocytopenic purpura; 100 mg/day PO in patients with chronic hepatitis C; 150 mg/day PO for aplastic anemia.

Geriatric

75 mg/day PO for idiopathic thrombocytopenic purpura; 100 mg/day PO in patients with chronic hepatitis C; 150 mg/day PO for aplastic anemia.

Adolescents

75 mg/day PO for idiopathic thrombocytopenic purpura; 150 mg/day PO for severe aplastic anemia.

Children

12 years: 75 mg/day PO for idiopathic thrombocytopenic purpura; 150 mg/day PO for aplastic anemia.
6 to 11 years: 75 mg/day PO for idiopathic thrombocytopenic purpura; 75 mg/day PO for aplastic anemia.
2 to 5 years: 75 mg/day PO for idiopathic thrombocytopenic purpura; 2.5 mg/kg/day PO for aplastic anemia.
1 year: 75 mg/day PO for idiopathic thrombocytopenic purpura; safety and efficacy have not been established for other indications.

Infants

Safety and efficacy have not been established.

Eltrombopag is a non-peptide thrombopoietin (TPO) receptor agonist that interacts with the transmembrane domain of the human TPO receptor. Specifically, eltrombopag binds to the TPO receptor (also known as cMpl) and causes proliferation and differentiation of megakaryocytes leading to increased platelet production. Additionally, it may bind to a location that is distinct from where endogenous TPO binds to the receptor; in vitro data suggest that eltrombopag's effects may be additive to TPO. In animal and early clinical studies, eltrombopag caused dose-dependent increases in platelet counts without affecting platelet function.

Eltrombopag is administered orally. The concentration in blood cells is 50% to 79% of plasma concentrations; in vitro studies indicate more than 99% protein binding. Eltrombopag undergoes extensive metabolism, predominantly through cleavage, oxidation, and conjugation with glucuronic acid, glutathione, or cysteine. In vitro studies have found that CYP1A2 and CYP2C8 are responsible for the oxidative metabolism of eltrombopag, and UGT1A1 and UGT1A3 are responsible for glucuronidation. Elimination occurs primarily by the feces (59%) and the urine (31%); unchanged drug accounts for approximately 20% of the dose in the feces, and unchanged drug is not detected in the urine. The plasma elimination half-life is 21 to 32 hours in healthy subjects.[40392]
 
Affected cytochrome P450 isoenzymes and drug transporters: CYP1A2, CYP2C8, CYP2C9, BCRP, OATP1B1, UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, UGT2B15
In vitro studies suggest that eltrombopag has the potential to inhibit CYP2C8 and CYP2C9, the organic anion transporting peptide OATP1B1, the breast cancer resistance protein (BCRP), and the UDP-glucuronyltransferases UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, and UGT2B15.[40392] The effects on eltrombopag of coadministration of moderate or strong inhibitors or inducers of CYP1A2, CYP2C8, UGT1A1, and UGT1A3 have not been adequately assessed.

Oral Route

Peak plasma concentrations occur 2 to 6 hours after oral administration. After administration of a 75 mg oral suspension dose, approximately 52% of drug-related material is absorbed. Eltrombopag oral suspension delivers a 22% higher plasma AUC than the tablet formulation. When administered with a polyvalent cation antacid (aluminum hydroxide; aluminum carbonate; and sodium alginate), the AUC of eltrombopag is decreased by approximately 70%; similarly, when administered with a high-fat meal, the AUC is decreased by 59%, the Cmax is decreased by 65%, and the Tmax is delayed by 1 hour. Administration of a single 25 mg dose of eltrombopag oral suspension to adults with a high-calcium, moderate-fat meal reduced the AUC by 75% and the Cmax by 79%. Administration of a single 25 mg dose of eltrombopag oral suspension 2 hours before and 2 hours after the high-calcium meal reduced the AUC by 20% and 47%, respectively, while the Cmax was reduced by 14% and 48%, respectively.[40392]
 
Eltrombopag demonstrates dose-proportional increases in exposure between doses of 50 to 150 mg/day in healthy adult subjects. AUC is approximately 1.7-fold, 2.8-fold, and 3.2-fold higher in patients with chronic immune thrombocytopenia, hepatitis C, and immunosuppressive therapy-naive severe aplastic anemia, respectively, compared to healthy subjects.[40392]

Pregnancy

Limited data from published case reports and postmarketing experience with eltrombopag use in human pregnancy are insufficient to assess any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction and developmental toxicity studies, embryolethality and reduced fetal weights occurred when eltrombopag was given to rats in maternally toxic doses (6 times the human clinical exposure based on AUC in patients with persistent or chronic immune thrombocytopenia at 75 mg/day and 3 times the AUC in patients with chronic hepatitis C at 100 mg/day). There is a pregnancy exposure registry that monitors outcomes in pregnant patients exposed to eltrombopag; information about the registry can be obtained by calling 1-888-825-5249.

There are no data regarding the presence of eltrombopag or its metabolites in human breast milk, the effects on the breast-fed child, or the effects on milk production. Eltrombopag was detected in the pups of lactating rats at 10 days postpartum, suggesting the potential for transfer during lactation. Breast-feeding is not recommended during eltrombopag treatment due to the potential for serious adverse reactions in the breast-fed child from eltrombopag.