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A phase Ia/Ib dose escalation trial of the oral selective KRAS G12C inhibitor divarasib was published in 2023, where the drug was tested in non-small cell lung cancer, colorectal cancer, and other solid tumors with KRAS G12C mutations. [55] It continues in phase I and II studies for several cancer types as of August 2023. [56] [57] [58] [59]
Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. [4] [5] It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for various forms of cancer.
K-Ras(G12C) inhibitor 6 is an irreversible inhibitor of oncogenic K-Ras(G12C), subverting the native nucleotide preference to favour GDP over GTP. Its family of inhibitors allosterically control GTP affinity and effector interactions by fitting inside a "pocket", or binding site, of mutant K-Ras. It is the most frequently mutated oncogene. [1]
mRNA-5671 also known as V941 is a cancer vaccine candidate developed by Moderna. [1] It is a tetravalent vaccine that targets G12D, G12V, G13D or G12C driver mutations in the KRAS gene. [ 2 ] It is currently being evaluated for the treatment of either non-small cell lung cancer , colorectal cancers with microsatellite instability , or ...
Adagrasib, sold under the brand name Krazati, is an anticancer medication used to treat non-small cell lung cancer. [1] [2] Adagrasib is an inhibitor of G12C mutated KRAS GTPase. [1] It is taken by mouth. [1] It is being developed by Mirati Therapeutics. [1] [5]
Lewis lung carcinoma is a hypermutated Kras/Nras–mutant cancer with extensive regional mutation clusters in its genome. A tumor that spontaneously developed as an epidermoid carcinoma in the lung of a C57BL mouse. It was discovered in 1951 by Dr. Margaret Lewis of the Wistar Institute and became one of the first transplantable tumors. [1]
non-small cell lung cancer with EGFR exon 20 insertion mutations Sotorasib: Amgen: non-small cell lung cancer with KRAS G12C mutation Avapritinib: Blueprint Medicines Corp: granted for two indications: mast cell leukemia and advanced systemic mastocytosis: Belumosudil: Kadmon Pharmaceuticals: chronic graft-versus-host disease: Pembrolizumab: Merck
AMG 510 by Amgen is a KRAS p.G12C covalent inhibitor that has recently finished Phase I clinical trial. [23] The drug elicited partial responses in half of evaluable patients with KRAS G12C-mutant non–small cell lung cancer, and led to stable disease in most evaluable patients with colorectal (or appendix) cancer.
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