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Drug intelligence / Profile preview
2'-deoxy-2'-fluoro-5-methyl-1-β-D-arabinofuranosyluracil
- Development stage
- Preclinical
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
2'-deoxy-2'-fluoro-5-methyl-1-β-D-arabinofuranosyluracil (FMAU) is a synthetic pyrimidine analogue and a thymidine analogue. It was initially developed as an antiviral drug in the 1960s and 1970s for the treatment of herpes simplex virus infection but was withdrawn from Phase I clinical trials due to neurotoxicity at pharmacological doses. More recently, radiolabeled forms of FMAU, such as 18F-FMAU or 11C-FMAU, have been developed as tracers for positron emission tomography (PET) imaging. In this diagnostic application, FMAU acts by binding to human thymidine kinase, an enzyme that is often upregulated in cancer cells, and by being incorporated into replicated DNA. This allows for the assessment of cell proliferation and DNA synthesis, making it useful for the early detection of cancer and the evaluation of treatment response.
- Other names
- 1-(2-Deoxy-2-fluoro-b-D-arabinofuranosyl)-5-methyluracil2'-Fluoro-5-methyl-1-beta-D-arabinofuranosyluracil1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)thymine
02
Targets
DNADNA polymerase familyTK1 (Thymidine kinase 1)TK2 (Thymidine kinase 2)
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