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Drug intelligence / Profile preview
[F-18]-5-fluoro-2'-deoxycytidine + tetrahydrouridine
- Development stage
- Phase 1
- Lead developer
- National Cancer Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
[F-18]-5-fluoro-2'-deoxycytidine ([F-18]-FdCyd) in combination with tetrahydrouridine (THU) is a radiopharmaceutical imaging regimen developed by the National Cancer Institute (NCI). [F-18]-FdCyd is a radiolabeled analog of the therapeutic agent 5-fluoro-2'-deoxycytidine (FdCyd), which acts as a DNA methyltransferase (DNMT) inhibitor to promote the re-expression of genes silenced by DNA hypermethylation. The combination includes THU, a cytidine deaminase inhibitor, to prevent the rapid degradation of FdCyd, thereby enhancing its bioavailability and exposure. This imaging agent is primarily used in Phase 0 clinical trials to evaluate the safety, radiation dosimetry, and biodistribution of FdCyd in patients with advanced solid tumors, including head and neck, lung, urinary bladder, and breast neoplasms, providing insights into drug distribution during therapy.
- Other names
- 18F-FdCyd + THU5-fluoro-2'-deoxycytidine + tetrahydrouridine
02
Targets
CDA (Cytidine deaminase)DNMT (DNA methyltransferase)TS (Thymidylate synthase)
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