Last reviewed 2026-04-22 · How we verify

AMG 510

AMG 510 is a small-molecule inhibitor that selectively targets KRAS G12C mutations, blocking oncogenic signaling in cancer cells.

AMG 510 is a small-molecule inhibitor that selectively targets KRAS G12C mutations, blocking oncogenic signaling in cancer cells. Used for Non-small cell lung cancer with KRAS G12C mutation, Colorectal cancer with KRAS G12C mutation, Pancreatic cancer with KRAS G12C mutation.

At a glance

Mechanism of action

AMG 510 binds covalently to the mutant KRAS G12C protein in its inactive GDP-bound state, preventing its activation and downstream signaling through the MAPK and PI3K pathways. This mechanism is specific to tumors harboring the KRAS G12C mutation, which is found in approximately 3-4% of human cancers. By selectively inhibiting this driver mutation, the drug can induce tumor regression in KRAS G12C-dependent malignancies.

Approved indications

• Non-small cell lung cancer with KRAS G12C mutation
• Colorectal cancer with KRAS G12C mutation
• Pancreatic cancer with KRAS G12C mutation

Common side effects

• Diarrhea
• Nausea
• Fatigue
• Vomiting
• Abdominal pain

Key clinical trials

• Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial (PHASE2)
• Study to Compare AMG 510 "Proposed INN Sotorasib" With Docetaxel in Non Small Cell Lung Cancer (NSCLC) (CodeBreak 200). (PHASE3)
• A Rollover Study Evaluating Sotorasib With or Without Panitumumab in Participants With KRAS p.G12C Mutation (PHASE2)
• Sotorasib in Combination With Trastuzumab Deruxtecan for the Treatment of Locally Advanced and Metastatic Non-small Cell Lung Cancer With a KRAS G12C Mutation (PHASE1, PHASE2)
• Testing the Use of AMG 510 (Sotorasib) and Panitumumab as a Targeted Treatment for KRAS G12C Mutant Solid Tumor Cancers (A ComboMATCH Treatment Trial) (PHASE2)
• AMG 510 Ethnic Sensitivity Study (CodeBreaK 105). (PHASE1)
• Study of Sotorasib, Panitumumab and FOLFIRI Versus FOLFIRI With or Without Bevacizumab-awwb in Treatment-naïve Participants With Metastatic Colorectal Cancer With KRAS p.G12C Mutation (PHASE3)
• A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of Sotorasib (AMG 510) in Subjects With Solid Tumors With a Specific KRAS Mutation (CodeBreaK 100) (PHASE1, PHASE2)

Primary sources

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