Drug intelligence / Profile preview

GW-833972A

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

GW-833972A is a small-molecule inhibitor and degrader of BMAL2 (Basic Helix-Loop-Helix ARNT Like Effector 2), a circadian transcription factor. Identified through structure-based virtual screening, the compound effectively binds to BMAL2, leading to its degradation. In ovarian clear cell carcinoma (OCCC) models, BMAL2 inhibition by GW-833972A downregulates RAD51 and impairs homologous recombination-mediated DNA repair, thereby suppressing tumor growth and overcoming chemoresistance. The compound has demonstrated efficacy in suppressing tumor growth in vivo and is being investigated as a novel therapeutic strategy for chemoresistant ovarian cancers.

02

Targets

CNR1 (Cannabinoid receptor 1)

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