Bosutinib (Bosulif)
(Pfiizer) Food increases exposure; following 15 daily doses of bosutinib 500 mg with food: Cmax = 200 ng/mL; AUC = 3650 ng∙h/mL;
compared to initial administration, plasma drug exposure did not increase significantly; following 15 daily doses 400 mg once daily:
AUC =2235 ng*h/mL;
Tmax=4 h;
Has acceptable exposure;
Vd= 6080 ± 1230 L;
(substrate of ABCB1) Metabolized mainly by CYP3A4, which can increase AUC and Cmax 500 mg orally once daily (chronic myeloid leukmia (chronic and accelerated phases and blast crisis with resistance/intolerance to prior therapy)); 400 mg orally once daily (newly diagnosed chronic myeloid leukemia (chronic phase));
94% binding to human plasma proteins in vitro; 96% bound to human plasma proteins in healthy subjects ex vivo Pleural effusion is the main lung toxicity associated with bosutinib; 8% of patients in one study developed pleural effusions (207)