Mechanism of action

Bosutinib is a tyrosine kinase inhibitor. Bosutinib inhibits the BCR-ABL kinase that promotes CML; it is also an inhibitor of SRC-family kinases including SRC, LYN, and HCK1 
BOSULIF is a potent inhibitor against the majority of imatinib-resistant BCR-ABL mutations1-3
Evaluated in vitro, bosutinib inhibited 16 of 18 imatinib-resistant forms of BCR-ABL expressed in murine myeloid cell lines, with the exceptions of V299L and T315I 1,2
Preclinical inhibition does not necessarily correlate with clinical activity.
BCR-ABL=breakpoint cluster region-Abelson; Ph+=Philadelphia chromosome–positive.
BOSULIF Prescribing Information. New York, NY: Pfizer Inc.
Redaelli S, Piazza R, Rostagno R, et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol. 2009;27(3):469-471.
Hantschel O, Grebien F, Superti-Furga G. The growing arsenal of ATP-competitive and allosteric inhibitors of BCR‑ABL. Cancer Res. 2012;72(19):4890-4895.