molecules of the month


oral reversible pan-KRAS inhibitor

oral activity in xenograft models (10-90 mpk BID)

from prior covalent KRAS(G12C) inhibitor

Nature, May 31, 2023

Boehringer Ingelheim, Vienna, AT

BI-2493, pan-KRAS, oral reversible pan-KRAS inhibitor, oral activity in xenograft models (10-90 mpk BID), from prior covalent KRAS(G12C) inhibitor, Nature, May 31, 2023, BOEHRINGER INGELHEIM, VIENNA, AT
6 mins read

Why is the pan-KRAS inhibitor, BI-2493, a big deal? The RAS proteins, KRAS4A, KRAS4B, HRAS, and NRAS control diverse cellular processes, and gain-of-function mutations in RAS genes are found in ~25% of cancers in humans, with KRAS mutations accounting for up to 85% of RAS mutations across cancers. While KRAS(G12C) has been successfully targeted by approved drugs sotorasib and adagrasib and numerous candidates (e.g. BI-0474, AZD4625, JDQ443, ASP2453, ‘compound 25’), it is only the most common KRAS mutation in NSCLC (41% of NSCLC KRAS mutations) – the majority of KRAS mutations observed across cancers involve other mutants. Boehringer Ingelheim recently disclosed a pair of pan-KRAS inhibitors in Nature (BI-2865 and in vivo tool BI-2493, derived from previously disclosed covalent molecule…

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