AMG 510


AMG 510 is an experimental cancer drug. It targets a specific mutation, G12C, in the protein KRAS which is responsible for various forms of cancer.

Clinical development

AMG 510 is being developed by Amgen and, as of 2019, it was in Phase 1 clinical trials. In December, it was approved to begin Phase 2 clinical trials.
Because the G12C KRAS mutation is relatively common in some cancer types, 14% of non-small-cell lung cancer adenocarcinoma patients and 5% of colorectal cancer patients, and AMG 510 is the first drug candidate to target this mutation, there have been high expectations for the drug. The Food and Drug Administration has granted a fast track designation to AMG 510 for the treatment of metastatic non-small-cell lung carcinoma with the G12C KRAS mutation.

Chemistry and pharmacology

AMG 510 can exist in either of two atropisomeric forms and one is more active than the other. It selectively forms an irreversible covalent bond to the sulfur atom in the cysteine residue that is present in the mutated form of KRAS, but not in the normal form.