Drug intelligence / Profile preview

BMS-986497 + azacitidine + venetoclax

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

Overview

BMS-986497 + azacitidine + venetoclax is an investigational combination therapy being studied for the treatment of **relapsed or refractory acute myeloid leukemia (AML)** and **myelodysplastic syndrome (MDS)** expressing CD33. BMS-986497 (also known as ORM-6151) is a **protein degrader** that targets both **CD33** and **GSPT1** on certain leukemic cells, aiming to eliminate cells expressing these proteins. Venetoclax is a **BCL2 inhibitor**, classified as a small molecule that induces apoptosis in cancer cells by blocking the anti-apoptotic protein BCL2. Azacitidine is a **hypomethylating agent** that induces DNA hypomethylation and cytotoxicity in abnormal hematopoietic cells. In this triple combination, the drugs are used together to maximize therapeutic efficacy through complementary mechanisms: targeted protein degradation, apoptosis induction, and disruption of aberrant DNA methylation[1][2][3][5][6].

02

Targets

BCL-2 (BCL-2 family)DNMT (DNA methyltransferase)GSPT1 (G1 to S phase transition 1)CD33 (Myeloid cell surface antigen CD33)

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