18F-AMG510

18F-AMG510 is a radiolabeled positron emission tomography (PET) tracer developed for the non-invasive imaging of KRAS G12C mutation status in patients with cancers such as non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). It is synthesized by modifying the structure of AMG510 (sotorasib), a small molecule KRAS G12C inhibitor, with a polyethylene glycol chain and labeling it with fluorine-18. The tracer binds selectively to the KRAS G12C mutant protein, allowing visualization and quantification of tumors harboring this mutation via PET/CT imaging. Preclinical studies demonstrated high binding affinity and specificity for KRAS G12C-mutant cells, which was confirmed in animal models. First-in-human studies showed that 18F-AMG510 is safe, primarily excreted via gallbladder and intestine, and provides effective imaging contrast between mutant and non-mutant tumors[1][5]. Its development enables clinicians to identify patients who may benefit from targeted therapies against KRAS G12C.