[18F]PFPMD

[18F]PFPMD is a novel positron emission tomography (PET) radiotracer designed for the noninvasive imaging of tumors harboring the KRAS G12C mutation. It is a fluorine-18 labeled small molecule that selectively binds to the KRAS G12C oncoprotein, enabling visualization and quantification of this specific mutation in vivo. The tracer was developed based on the structure of recently FDA-approved KRAS G12C inhibitors and incorporates modifications such as a polyethylene glycol chain attached to a quinazolinone core to enhance its imaging properties. Preclinical studies demonstrated high radiochemical yield, purity, stability, and selective binding to mutant KRAS G12C protein. In first-in-human studies involving healthy volunteers and patients with non-small cell lung cancer (NSCLC) or colorectal cancer (CRC), [18F]PFPMD showed favorable safety profiles and rapid clearance via hepatobiliary excretion. Tumor uptake was significantly higher in patients with confirmed KRAS G12C mutations compared to those without, supporting its utility for screening mutation status, guiding targeted therapy selection, monitoring therapeutic response, and assessing drug resistance in oncology[1][2][6].