TABLE 7

PBPK model-predicted pharmacokinetic parameters of bosutinib in healthy subjects after a single oral administration of bosutinib with repeated coadministration of weak and moderate CYP3A inhibitors

Data are expressed as geometric means with percent coefficients of variation in parentheses.

PrecipitantPK ParameterRatioa
CmaxAUCCmaxRAUCR
ng/mlng⋅h/ml
Fluvoxamine84 (42)2603 (51)1.01.0
Fluconazole190 (34)8689 (40)2.33.4
Erythromycin210 (36)10,197 (50)2.54.0
Verapamil181 (41)7466 (63)2.43.1
  • a Ratios of Cmax and AUC in the treatment group (bosutinib with CYP3A inhibitor) to the control group (bosutinib alone).