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Annual Review of Cancer Biology

Volume 6, 2022

Targeting KRAS G12C with Covalent Inhibitors

Abstract

is the most frequently mutated oncogene in cancer. Following numerous attempts to inhibit KRAS spanning multiple decades, recent efforts aimed at covalently targeting the mutant cysteine of KRAS G12C have yielded very encouraging results. Indeed, one such molecule, sotorasib, has already received accelerated US Food and Drug Administration approval with phase III clinical trials currently underway. A second molecule, adagrasib, has also progressed to phase III, and several others have entered early-phase clinical trials. The success of these efforts has inspired an array of novel approaches targeting KRAS, with some reporting extension to the two most common oncogenic KRAS mutations, G12V and G12D.

Keyword(s): colorectal cancer, KRAS G12C, lung cancer, mutant-specific
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/content/journals/10.1146/annurev-cancerbio-041621-012549
2022-04-11
2025-04-30
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Targeting KRAS G12C with Covalent Inhibitors
Annual Review of Cancer Biology 6, 49 (2022); https://doi.org/10.1146/annurev-cancerbio-041621-012549
/content/journals/10.1146/annurev-cancerbio-041621-012549
/content/journals/10.1146/annurev-cancerbio-041621-012549
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