GTPase KRAS (G12C mutant) inhibitor Treatment of non-small cell lung cancer Treatment of colorectal cancer

DRUGS OF THE FUTURE(2022)

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摘要
Colorectal cancer (CRC) is one of the cancers with high mor-bidity and mortality worldwide, and its treatment and prog-nosis have undergone tremendous changes because of the emergence of molecular targeted therapy. Kirsten rat sarco-ma viral oncogene homologue (KRAS) is the most frequently mutated oncogene in CRC. For a long time, due to the diffi- culty of effectively blocking KRAS function with traditional small-molecule inhibitors, KRAS protein was considered as an "undruggable" target. There has been amazing progress in directly targeting drugs against KRAS for cancer treatment, especially KRASG12C inhibitors, that have achieved promising outcomes in clinical studies. Adagrasib is a first-in-class co- valent small-molecule inhibitor against KRASG12C. This article reviews the mechanism of action of adagrasib and the latest preclinical and clinical research in the treatment of CRC and other cancers to provide a reference for the development of antitumor drugs.
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关键词
KRASG12C mutation inhibitors,Colorectal Cancer,Non-small cell lung cancer,Adagrasib,MRTX-849,Targeted&nbsp,therapy
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