IN VITRO, CYP1A2, CYP2C8, UGT1A1, AND UGT1A3 ARE INVOLVED IN THE METABOLISM OF ELTROMBOPAG. IN VITRO, ELTROMBOPAG INHIBITS THE FOLLOWING METABOLIC OR TRANSPORTER SYSTEMS: CYP2C8, CYP2C9, UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, UGT2B15, OATP1B1, AND BREAST CANCER RESISTANCE PROTEIN (BCRP).
ELTROMBOPAG CHELATES POLYVALENT CATIONS (SUCH AS IRON, CALCIUM, ALUMINUM, MAGNESIUM, SELENIUM, AND ZINC) IN FOODS, MINERAL SUPPLEMENTS, AND ANTACIDS WHICH DECREASE PLASMA ELTROMBOPAG SYSTEMIC EXPOSURE BY APPROXIMATELY 70%. TAKE ELTROMBOPAG AT LEAST 2 HOURS BEFORE OR 4 HOURS AFTER ANY MEDICATIONS.
COADMINISTRATION OF ELTROMBOPAG WITH THE OATP1B1 AND BCRP SUBSTRATE, ROSUVASTATIN, TO HEALTHY ADULT SUBJECTS INCREASED PLASMA ROSUVASTATIN CONC. BY 103%. SO REDUCE ROSUVASTATIN DOSE BY 50%.
USE CAUTION WHEN CONCOMITANTLY ADMINISTERING ELTROMBOPAG AND DRUGS THAT ARE SUBSTRATES OF OATP1B1 (E.G., ATORVASTATIN, BOSENTAN, EZETIMIBE, FLUVASTATIN, GLYBURIDE, OLMESARTAN, PITAVASTATIN, PRAVASTATIN, ROSUVASTATIN, REPAGLINIDE, RIFAMPIN, SIMVASTATIN ACID, SN-38 [ACTIVE METABOLITE OF IRINOTECAN], VALSARTAN) OR BCRP (E.G., IMATINIB, IRINOTECAN, LAPATINIB, METHOTREXATE, MITOXANTRONE, ROSUVASTATIN, SULFASALAZINE, TOPOTECAN) SINCE IT INCREAESES PLASMA CONC. OF THESE DRUGS.
HIV PROTEASE INHIBITORS HAVE NO SIGNIFICANT INTERACTIONS.