Drug intelligence / Profile preview

dasatinib + rabeprazole + betaine hydrochloride

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

Overview

This is a combination of three agents: dasatinib, rabeprazole, and betaine hydrochloride. Dasatinib is an oral second-generation small molecule tyrosine kinase inhibitor primarily used for the treatment of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL). It inhibits BCR-ABL, SRC family kinases, c-KIT, EPHA2, and PDGFRβ. Rabeprazole is a proton pump inhibitor that suppresses gastric acid secretion by inhibiting the H+/K+ ATPase in gastric parietal cells; it is used to treat conditions like gastroesophageal reflux disease but can reduce the absorption of drugs with pH-dependent solubility such as dasatinib. Betaine hydrochloride (BHCl) is an acidic supplement that transiently re-acidifies gastric pH after acid suppression by agents like rabeprazole. In clinical studies, coadministration of BHCl with dasatinib in subjects pretreated with rabeprazole restored dasatinib absorption to levels comparable to administration without acid suppression[1][2][7]. This combination has been studied as a strategy to mitigate drug-drug interactions between oral anticancer drugs requiring acidic environments for optimal absorption and concurrent use of acid-reducing agents.

Brand names
Acidil
Other names
BHCl
02

Targets

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

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