Drug intelligence / Profile preview

fluorine F 18 d-FMAU

Development stage
Phase 1
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Fluorine F 18 d-FMAU is a radiolabeled nucleoside analog and a thymidine derivative used as a PET imaging tracer. Specifically, it is the D-enantiomer of 2'-fluoro-5-methyl-1-beta-D-arabinofuranosyluracil labeled with the positron-emitting isotope fluorine-18. It acts as a substrate for thymidine kinase enzymes, particularly thymidine kinase 1 (TK1), which is associated with cellular proliferation, and mitochondrial thymidine kinase 2 (TK2). Once transported into cells, it undergoes phosphorylation by these kinases, leading to intracellular metabolic trapping and incorporation into DNA. This mechanism allows for the visualization of high-proliferation tissues and mitochondrial activity using Positron Emission Tomography/Computed Tomography (PET/CT), making it a valuable tool for diagnosing, staging, and monitoring the treatment response of various malignancies, including prostate and other advanced cancers.

Other names
2'-deoxy-2'-[18F]fluoro-5-methyl-1-beta-D-arabinofuranosyluracil1-(2-deoxy-2-[18F]fluoro-beta-D-arabinofuranosyl)-5-methyluracilF-18 D-FMAUF18 D-FMAUF 18 D-FMAU18F-labeled d-FMAU
02

Targets

TK2 (Thymidine kinase 2)TK1 (Thymidine kinase 1)

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