Drug intelligence / Profile preview

sendegobresib

Development stage
Unknown
Lead developer
C4 Therapeutics, Inc.
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

Sendegobresib (CFT8634) is an orally bioavailable, investigational small molecule that functions as a heterobifunctional protein degrader targeting bromodomain-containing protein 9 (BRD9). It is designed using the BiDAC™ platform and consists of an E3 ligase-binding moiety and a BRD9-binding moiety. Upon binding to BRD9, it recruits the CRL4-CRBN E3 ubiquitin ligase complex, leading to proteasome-mediated degradation of BRD9. This mechanism inhibits the growth of tumor cells dependent on BRD9 for survival, particularly in cancers such as synovial sarcoma and SMARCB1-null solid tumors. Sendegobresib has received FDA orphan drug designation for synovial sarcoma and is being developed by C4 Therapeutics[1][5][6][7].

Other names
sendegobresib
02

Targets

CRBN (Cereblon)BRD9 (Bromodomain-containing protein 9)

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