Drug intelligence / Profile preview

18F-fluoropemetrexed

Development stage
Unknown
Lead developer
VU University Medical Center
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

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.

Other names
[18F]fluoropemetrexedFluorine-18 fluoropemetrexedFluorine18 fluoropemetrexedFluorine 18 fluoropemetrexed18F-labeled pemetrexed
02

Targets

FOLR1 (FRα)SLC46A1 (Proton-coupled folate transporter)RFC1 (Reduced folate carrier type 1)TS (Thymidylate synthase)

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