Simulation outline of crizotinib single- and multiple-dose pharmacokinetic and drug-drug interaction studies

CrizotinibDoseTreatment DayCoadministrationDoseTreatment DayAnalysis
Single-dose oral bioavailability studyIV501Pred versus Obs
PO2501Pred versus Obs
Single-dose drug-drug interaction studiesPO1504Ketoconazole200 bid1–16Pred versus Obs
PO2509Rifampin600 qd1–14Pred versus Obs
Multiple-dose pharmacokinetic and drug-drug interaction studiesPO250 bid1–28Pred versus Obs
PO150 bid1–28Ketoconazole200 bid1–28Pred
PO250 bid1–28Rifampin600 qd1–28Pred
PO150 bid1–28Diltiazem120 bid1–28Pred
PO150 bid1–28Erythromycin500 tid1–28Pred
PO150 bid1–28Fluconazole200 qd1–28Pred
PO150 bid1–28Fluvoxamine50 qd1–28Pred
  • IV, intravenous administration; PO, oral administration; qd, once a day; bid, twice a day; tid, three times a day; Pred, predicted; Obs, observed.