Purpose: Covalent inhibitors of KRASG12C specifically target tumors driven by this form of
mutant KRAS, yet early studies show that bypass signaling drives adaptive resistance …

Despite decades of research, efforts to directly target KRAS have been challenging.
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that …

Purpose: Although KRAS represents the most commonly mutated oncogene, it has long
been considered an “undruggable” target. Novel covalent inhibitors selective for the …

Mutant-selective KRASG12C inhibitors, such as MRTX849 (adagrasib) and AMG 510
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …

Abstract KRAS G12C inhibitors have shown promise in KRAS G12C–mutant lung cancer but
intrinsic and acquired resistance are common. Cotreatment with inhibitors of the protein …

BACKGROUND The KRAS proto-oncogene is among the most frequently mutated genes in
cancer, yet for 40 years it remained an elusive therapeutic target. Recently, allosteric …

Background Clinical trials of the KRAS inhibitors adagrasib and sotorasib have shown
promising activity in cancers harboring KRAS glycine-to-cysteine amino acid substitutions at …

KRAS mutations are among the most prevalent tumor drivers, but targeting them
pharmacologically has been challenging. Recent landmark studies have demonstrated …

Despite the discovery of RAS oncogenes in human tumor DNA 40 years ago, the
development of effective targeted therapies directed against RAS has lagged behind those …

KRAS mutations are one of the most prevalent oncogenic alterations in cancer. Until
recently, drug development targeting KRAS did not convey clinical benefits to patients …