Adagrasib (MRTX849) showed efficacy and safety in KRASG12C NSCLCs from KRYSTAL-1 study

KRAS is the first human oncogene discovered in 1983; however, no any approved KRAS target therapy till now. The challenges are protein itself lack of known allosteric regulatory sites and binding affinity to GTP/GDP, thus directly targeting oncogenic KRAS with small molecules in the nucleotide-binding site has been difficult.

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