fbpx

molecules of the month

CC-90009

CRBN-based GSPT1 molecular glue degrader

intravenous agent in Ph. I for AML + MDS

from phenotypic screen of CRBN mod library

J. Med. Chem., Feb. 16, 2021

Celgene/Bristol Myers Squibb, San Diego, CA

CC-90009
1 min read

1. The Bristol Myers Squibb (BMS)/Celgene GSPT1 degrader (CC-90009) is a CRBN-based molecular glue (CELMoD). It is a clinical candidate in Ph. I for AML and MDS, and in contrast to CC-92480 highlighted last March, spares the primary targets of prior imide drugs (IKZF1/3) and instead selectively degrades GSPT1 (a target previously identified in their discovery of CC-885). The starting point was identified through a phenotypic screen against a panel of AML cell lines using their cereblon (CRBN) modulator library and the nontumor human epithelial cell line (THLE-2) as a counterscreen. Clinically, at a dose of 2.4 mg, 90% GSPT1 reduction was observed, representing an important proof-of-concept for expanding the scope of molecular glue-type degraders.


request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.


already a member? log in: