Sotorasib is an experimental KRAS inhibitor being investigated for the treatment of KRAS G12C mutant non small cell lung cancer, colorectal cancer, and appendix cancer. Sotorasib, also known as AMG-510, is an acrylamide-derived KRAS inhibitor developed by Amgen.
- Mechanism
- Curator reviewed · 6 references
Normally GTP binds to KRAS, activating the protein and promoting effectors to the MAP kinase pathway. GTP is hydrolyzed to GDP, and KRAS is inactivated. KRAS G12C mutations impair hydrolysis of GTP, leaving it in the active form.
Sotorasib binds to the cysteine residue in KRAS G12C mutations, holding the protein in its inactive form. The cysteine residue that sotorasib targets is not present in the wild type KRAS, which prevents off-target effects. This mutation is present in 13% of non small cell lung cancer, 3% of colorectal and appendix cancer, and 1-3% of solid tumors.
- Primary indication
- Sotorasib is indicated in the treatment of KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) in adults who have received at least one prior systemic therapy.Curator reviewed · 5 structured indications
- Formula / weight
- C30H30F2N6O3 · 560.606 g/mol (avg)
- First approval
- Canada, 2021 · United States, 2021 · European Union, 2022
- Code names
- AMG-510
- Brand names
Resolves to
NXQKSXLFSAEQCZ-SFHVURJKSA-NSMILESCC(C)C1=NC=CC(C)=C1N1C(=O)N=C(N2CCN(C[C@@H]2C)C(=O)C=C)C2=CC(F)=C(N=C12)C1=C(O)C=CC=C1FWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Sotorasib, and which of those have an active Phase 3 trial?
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