Drug intelligence / Profile preview

CC-99282 + valemetostat

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

Overview

**CC-99282 + valemetostat** is an investigational combination therapy under clinical evaluation, primarily for the treatment of various subtypes of relapsed or refractory non-Hodgkin's lymphomas. - **CC-99282** (also known as golcadomide) is a novel, oral small molecule that functions as a cereblon modulator, influencing ubiquitin-mediated protein degradation and exerting immunomodulatory and anti-proliferative effects. - **Valemetostat tosilate** (brand name valemetostat) is an oral small molecule dual inhibitor of the histone methyltransferases EZH1 and EZH2, with epigenetic modulator activity that suppresses gene expression involved in lymphoma cell growth and survival. Both agents have shown efficacy as monotherapies in T-cell and B-cell lymphomas, and their combination is under investigation for potentially synergistic anti-lymphoma activity, particularly in patients with relapsed or refractory diseases who have failed other therapies[4][6][5][1].

Brand names
golcadomidevalemetostat tosilate
02

Targets

EZH1CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)EZH2 (Histone-lysine N-methyltransferase EZH2)IKZF1 (Ikaros family zinc finger protein 1)

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