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Drugs Fut 2021, 46(7): 521
ISSN 0377-8282
Copyright 2021 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2021.46.7.3301489
 
 
Sotorasib. GTPase KRAS (G12C mutant) inhibitor, Treatment of non-small cell lung cancer, Treatment of colorectal cancer, Treatment of solid tumors
Gras, J.
 
 
The most frequent and lethal cancer worldwide is lung cancer, wherein RAS is the most frequently mutated oncogene in cancer, and the specific KRAS mutation glycine 12 to cysteine (KRAS G12C) is present in around 13% of lung adenocarcinoma, 3% of colorectal cancer (CRC) and 2% of other solid tumors. In in vitro and in vivo relevant models harboring KRAS G12C mutation, sotorasib (AMG-510; Amgen), the first KRAS G12C inhibitor that entered clinical trials, showed antitumor efficacy, and in a phase II study in KRAS G12C non-small cell lung cancer (NSCLC) patients, tumor shrinkage was recorded in 71% of patients. The drug recently obtained accelerated approval in the U.S. for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic NSCLC. Meanwhile, a phase Ib study of sotorasib combined with other anticancer therapies in subjects with KRAS G12C mutation is recruiting participants, and a phase III study with sotorasib in comparison with docetaxel in KRAS G12C NSCLC subjects is ongoing. Sotorasib was granted orphan drug designation by the U.S. Food and Drug Administration for the treatment of KRAS G12C NSCLC and KRAS G12C CRC; it also has received fast track and breakthrough therapy designations for the treatment of KRAS G12C NSCLC.


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