Odalade Drug Interactions

Eltrombopag is a substrate of BCRP/ABCG2, CYP1A2 (minor), CYP2C8 (minor), UGT1A1, UGT1A3. Eltrombopag inhibits BCRP/ABCG2, OATP1B1/1B3 (SLCO1B1/1B3), UGT1A1, UGT1A3, UGT1A6, UGT1A9, UGT2B15, UGT2B7.
Effects of other drugs on eltrombopag: Cyclosporine: A decrease in eltrombopag exposure was observed with co-administration of 200 mg and 600 mg cyclosporine (a BCRP inhibitor). This decrease in exposure is not considered clinically meaningful. Eltrombopag dose adjustment is permitted during the course of the treatment based on the patient's platelet count. Platelet count should be monitored at least weekly for 2 to 3 weeks when eltrombopag is coadministered with cyclosporine. Eltrombopag dose may need to be increased based on these platelet counts.
Polyvalent Cations Chelation: Eltrombopag chelates with polyvalent cations such as aluminium, calcium, iron, magnesium, selenium, and zinc. Administration of a single dose of eltrombopag 75 mg with a polyvalent cation-containing antacid (1524 mg aluminium hydroxide and 1425 mg magnesium carbonate) decreased plasma eltrombopag AUCinf and Cmax. Eltrombopag should be taken at least two hours before or four hours after any products such as antacids, dairy products, or mineral supplements containing polyvalent cations to avoid significant reduction in eltrombopag absorption.
Lopinavir/ritonavir: Co-administration of eltrombopag with lopinavir/ritonavir may cause a decrease in the concentration of eltrombopag. Therefore, caution should be used when co-administration of eltrombopag with lopinavir/ritonavir takes place. Platelet count should be monitored at least weekly for 2 to 3 weeks in order to ensure appropriate medical management of the dose of eltrombopag when lopinavir/ritonavir therapy is initiated or discontinued.
HCV protease inhibitors: Co-administration of repeat doses of boceprevir 800 mg every 8 hours or telaprevir 750 mg every 8 hours with a single dose of eltrombopag 200 mg did not alter plasma eltrombopag exposure to a clinically significant extent.
Effects of eltrombopag on other drugs: Rosuvastatin: Administration of eltrombopag 75 mg once daily for 5 days with a single 10 mg dose of the OATP1B1 and BCRP substrate rosuvastatin increased plasma rosuvastatin Cmax and AUCinf. When co-administered with eltrombopag, a reduced dose of rosuvastatin should be considered and careful monitoring should be undertaken. A dose reduction of rosuvastatin by 50% was recommended for co-administration of rosuvastatin and eltrombopag. Concomitant administration of eltrombopag and other OATP1B1 and BCRP substrates should be undertaken with caution.
Cytochrome P450 substrates: Administration of eltrombopag 75 mg once daily for 7 days did not inhibit or induce the metabolism of probe substrates for 1A2 (caffeine), 2C19 (omeprazole), 2C9 (flurbiprofen), or 3A4 (midazolam) in humans. No clinically significant interactions are expected when eltrombopag and CYP450 substrates, inducers or inhibitors are co-administered.
HCV Protease inhibitors: Co-administration of a single dose of eltrombopag 200 mg with telaprevir 750 mg every 8 hours did not alter plasma telaprevir exposure. Co-administration of a single dose of eltrombopag 200 mg with boceprevir 800 mg every 8 hours did not alter plasma boceprevir AUCtau, increased Cmax by 19%, and decreased Cmin by 32%. Dose adjustment is not required when eltrombopag is co-administered with either telaprevir or boceprevir.
Drug-food/drink interactions: Food, especially dairy products, may decrease the absorption of eltrombopag.
Take eltrombopag on an empty stomach at least 1 hour before or at least 2 hours after a meal. Take eltrombopag at least 2 hours before and 4 hours after foods high in calcium.