molecules of the month


oral brain-penetrant SOS1:KRASG12C PPI inhibitor

efficacy in MIA PaCa-2 tumor mouse xenograft model

from literature starting point and opt

J. Med. Chem.

Mirati Therapeutics, San Diego, CA

MRTX0902 Chemical Structure oral brain-penetrant SOS1:KRASG12C PPI inhibitor - Mirati Therapeutics, San Diego, CA
5 mins read

Context. MRTX0902 (Mirati Therapeutics) is an oral brain penetrating SOS1:KRAS protein-protein interaction inhibitor. Since the first report of the druggability of the KRASG12C mutant, KRAS has been a hotly pursued oncotarget. Notably, the first-in-class sotorasib (Lumakras; Amgen) was recently approved, while Mirati Therapeutics’ highly promising adagrasib (MRTX84) is on track to be approved by regulators. However, emerging data on acquired resistance to adagrasib and sotorasib suggest that additional therapies that enhance the duration of response to KRASG12C inhibitors may be useful. Considered the “pacemaker” of KRAS due to its key role in switching the GTPase to the active state, SOS may be a desirable target for inhibiting KRAS activity. The SOS1 binder MRTX0902 uniquely disrupts the KRAS:SOS1 protein-protein interaction which,…

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