Revolade Drug Interactions

Drug Interactions: Rosuvastatin: In vitro studies demonstrated that eltrombopag is not a substrate for the OATP1B1 but is an inhibitor of this transporter and that eltrombopag is a BCRP substrate and inhibitor. When Revoladem and rosuvastatin were co-administered in a clinical drug interaction study (see Pharmacokinetics under Actions) there was increased plasma rosuvastatin exposure. When co-administered with Revolade, a reduced dose of rosuvastatin should be considered and careful monitoring should be undertaken. In clinical trials with Revolade, a dose reduction of rosuvastatin by 50% was recommended for co-administration of rosuvastatin and Revolade. Concomitant administration of Revolade and other OATP1B1 and BCRP substrates should be undertaken with caution.
Polyvalent Cations (Chelation): Eltrombopag chelates with polyvalent cations eg, aluminium, calcium, iron, magnesium, selenium and zinc (see Pharmacokinetics under Actions). Antacids, dairy products and other products containing polyvalent cations eg, mineral supplements should be administered at least 4 hrs apart from Revolade dosing to avoid significant reduction in eltrombopag absorption (see Dosage & Administration).
Food Interaction: Administration of a single 50 mg-dose of Revolade with a standard high-calorie, high-fat breakfast that included dairy products reduced plasma eltrombopag AUC_0-∞ by 59% (90% CI: 54%, 64%) and C_max by 65% (90% CI: 59%, 70%). Food low in calcium (<50 mg calcium) including fruit, lean ham, beef and unfortified (no added calcium, magnesium, iron) fruit juice, soy milk and grain did not significantly impact plasma eltrombopag exposure, regardless of calorie and fat content (see Dosage & Administration).