molecules of the month


oral KRASG12C(ON) tri-complex inhibitor

Ph. I/Ib for adv. solid tumors

from FBDD + SBDD

AACR, April 2023

Revolution Medicines, Redwood City, CA

RMC-6291,KRASG12C, oral KRASG12C(ON) tri-complex inhibitor, Ph. I/Ib for adv. solid tumors, from FBDD + SBDD, AACR, April 2023, REVOLUTION MEDICINES, REDWOOD CITY, CA
7 mins read

And now for something completely different. The recent approvals of Ras(off)-targeting KRASG12C inhibitors sotorasib and adagrasib, decades in the making, mark the beginning of a new phase of KRAS drug discovery. Clinical data with both molecules suggest that there are opportunities for brain-penetrant KRAS inhibitors, a need for novel modalities to address drug resistance and the spectrum of KRAS mutants beyond KRASG12C, and a need for better tolerated molecules that can combine well with other classes of therapies like immunotherapy. While an increasing number of follow-on KRAS inhibitors are emerging with similar mechanisms of action to sotorasib, Revolution Medicines’ RMC-6291 is representative of a completely novel approach that could become a strong addition to the clinical toolbox for KRAS, but…

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