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Adagrasib is a small molecule inhibitor of the KRAS G12C mutation, which is a common driver mutation in various types of cancer, including non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and pancreatic cancer.
Mechanism of Action:
Adagrasib works by selectively inhibiting the activity of the KRAS G12C protein, which is a key player in the RAS/MAPK signaling pathway. By blocking the activity of KRAS G12C, adagrasib prevents the growth and proliferation of cancer cells, leading to tumor shrinkage and improved survival.
Adagrasib is a promising treatment for patients with NSCLC and CRC who have the KRAS G12C mutation. Its ability to selectively inhibit KRAS G12C activity makes it a valuable option for patients who have limited treatment options. However, resistance to adagrasib can occur, and combination therapy may be necessary to overcome this resistance.
Adagrasib is a novel KRAS G12C inhibitor that targets the mutant KRAS protein by covalently binding to its switch II pocket, thereby locking it in an inactive form. This inhibition blocks critical downstream signaling pathways, such as RAF/MEK/ERK and potentially PI3K/AKT/mTOR, which are essential for tumor growth and survival. Clinically, adagrasib is being developed and used primarily to treat NSCLC and other solid tumors with the KRAS G12C mutation, providing a targeted therapy option in a subset of cancers that historically have few effective targeted treatments.