fbpx

molecules of the month

BI-0474

IP KRASG12Ci related to oral candidate BI 1823911

TGI in NCI-H358 cancer xenograft mouse model

from 13k cmpd. HSQC-based screen and SBDD

J. Med. Chem.

Boehringer Ingelheim, Vienna, AT

BI-0474 chemical structure IP KRASG12Ci related to oral candidate BI 1823911 - Boehringer Ingelheim, Vienna, AT
5 mins read

Context. BI-0474 (Boehringer Ingelheim) is a covalent KRASG12C inhibitor. KRAS continues to be a hotly pursued oncotarget since the first report by the Shokat group of the druggability of the KRASG12C mutant. Recently, Amgen’s first-in-class sotorasib (Lumakras) was approved, while Mirati Therapeutics’ adagrasib (MRTX84) may be approved in December 2022, based on its PDUFA date. For BI-0474, Boehringer Ingelheim scientists started with a reversible switch II pocket binder and optimized affinity of the reversible molecule via structure-based design before introducing an acrylamide covalent warhead as a last step. While BI-0474 is a non-oral tool molecule, Boehringer Ingelheim mentions an advanced, orally bioavailable compound from the series (BI 1823911) is currently in early clinical development. Opportunities for differentiation could be better…


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: