KRAS mutation: from undruggable to druggable in cancer
Nov 15, 2021 · Recently, there has been light on the horizon for one specific mutation, KRAS (G12C). With the discovery of a new allosteric site of KRAS (G12C), several irreversible …
The KRAS-G12C inhibitor: activity and resistance
Sep 1, 2021 · Although it has long been deemed “undruggable”, with the development of drugs specifically binding the KRAS-G12C mutant protein, clinical trials that directly inhibit oncogenic …
KRAS G12C inhibitor combination therapies: current evidence and ...
Multiple combinations of KRAS G12C inhibitors with other targeted therapies, such as RTK, SHP2, and MEK inhibitors, have been investigated in clinical trials to overcome the resistance. …
Treatment for KRAS G12C-mutated metastatic CRC approved by …
Jan 17, 2025 · The KRAS G12C mutation is present in approximately 3-5% of colorectal cancers, emphasizing the important role of comprehensive biomarker testing in mCRC. By detecting an …
Sotorasib is First KRAS Inhibitor Approved by FDA - NCI
Jun 25, 2021 · The discovery and approval of sotorasib “opens up opportunities for developing compounds that bind to other mutant [KRAS] proteins,” Dr. McCormick said. G12C is one of …
The path to the clinic: a comprehensive review on direct KRAS G12C ...
Jan 19, 2022 · Analyzing amino acid-specific KRAS mutations in the three cancer types responsible for most KRAS mutations, the most common KRAS mutation in NSCLC …
KRAS G12C Inhibition with Sotorasib in Advanced Solid Tumors
Sep 20, 2020 · We conducted a phase 1 trial of sotorasib in patients with advanced solid tumors harboring the KRAS p.G12C mutation. Patients received sotorasib orally once daily. The …
Targeting KRAS in cancer - Nature Medicine
Apr 18, 2024 · The first successes occurred with allele-specific targeting of KRAS p.Gly12Cys (G12C) in non-small cell lung cancer, resulting in regulatory approval of two agents—sotorasib …
Sotorasib for Lung Cancers with KRAS p.G12C Mutation
Jun 4, 2021 · Sotorasib showed anticancer activity in patients with KRAS p.G12C–mutated advanced solid tumors in a phase 1 study, and particularly promising anticancer activity was …
Landscape of KRASG12C, Associated Genomic Alterations, and ...
Mar 23, 2022 · KRAS G12C was most prevalent in patients with non–small-cell lung cancer, appendiceal, colorectal, tumor of unknown origin, small bowel, and pancreatic cancers. KRAS …