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18F-fluoropemetrexed is a radiolabeled analog of the multi-targeted antifolate pemetrexed, developed as a positron emission tomography (PET) imaging agent. It is designed to non-invasively assess the expression and functional activity of folate transporters and receptors, such as the reduced folate carrier (RFC) and folate receptor alpha (FRα), within tumor tissues. By mimicking the pharmacokinetic distribution and cellular uptake mechanisms of the parent drug pemetrexed, this radiotracer serves as a companion diagnostic tool to identify patients with high target expression who are most likely to benefit from pemetrexed-based chemotherapy. It has primarily been investigated for use in thoracic malignancies, including non-small cell lung cancer (NSCLC) and malignant pleural mesothelioma, to predict treatment efficacy and monitor tumor folate metabolism.
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