Drug intelligence / Profile preview

dasatinib + rabeprazole

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Dasatinib + rabeprazole is not a fixed-dose combination drug but refers to the coadministration of dasatinib, an oral small molecule tyrosine kinase inhibitor used primarily for Philadelphia chromosome-positive leukemias (chronic myeloid leukemia and acute lymphoblastic leukemia), and rabeprazole, a proton pump inhibitor (PPI) used to reduce gastric acid. Dasatinib’s absorption is highly pH-dependent; concomitant use with PPIs like rabeprazole significantly reduces its bioavailability by increasing gastric pH. Studies show that coadministration of rabeprazole can decrease dasatinib Cmax and AUC by over 90%, potentially compromising therapeutic efficacy[1][3][5]. This interaction is clinically significant and generally contraindicated unless no alternatives exist.

02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)ATP4A (Potassium–transporting ATPase alpha chain 1)EPHA2 (Ephrin type-A receptor 2)SFK (SRC family kinases)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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