Drug intelligence / Profile preview

bosutinib + dabigatran

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**Bosutinib + dabigatran** is a combination comprising bosutinib, a small molecule tyrosine kinase inhibitor primarily targeting Bcr-Abl and Src family kinases for treatment of Philadelphia chromosome-positive chronic myelogenous leukemia (CML), and dabigatran, a direct oral anticoagulant that acts as a direct thrombin inhibitor for the prevention and treatment of thromboembolic disorders. This combination is of interest primarily for drug-drug interaction studies: bosutinib is a substrate and mild inhibitor of the P-glycoprotein (P-gp) transporter, while dabigatran is a P-gp substrate. Clinical studies have shown that co-administration does not result in clinically significant changes in dabigatran exposure, and bosutinib is not considered a clinically relevant inhibitor of P-gp when used acutely. No combination product is marketed; clinical use would be as co-prescription when both CML and an indication for anticoagulation coexist[1][3][4][6].

02

Targets

SFK (SRC family kinases)ABCB1 (P-glycoprotein)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)F2 (Thrombin)

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