Drug intelligence / Profile preview

fau f-18

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

[F-18]FAU is a radiolabeled nucleoside analog, specifically 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl) uracil, developed as a positron emission tomography (PET) imaging agent and investigated as a potential antineoplastic therapy. It functions as a DNA synthesis inhibitor by serving as a substrate for cellular enzymes; it is phosphorylated by thymidine kinase and methylated by thymidylate synthase, eventually becoming incorporated into the DNA of proliferating cells. This mechanism allows for the visualization of tumor activity and cellular proliferation. Clinical evaluation in a first-in-human study demonstrated significant retention in breast tumors and lymph node metastases with minimal bone marrow toxicity, suggesting its potential utility as both a diagnostic tool and an unlabeled therapeutic agent, although its imaging contrast may be limited for some clinical applications.

Other names
1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl) uracil2'-fluoro-2'-deoxy-beta-D-arabinofuranosyluracilF-18-FAUF18-FAUF 18-FAU2'-deoxy-2'-[18F]fluoro-beta-D-arabinofuranosyluracil
02

Targets

DNA polymerase familyTK1 (Thymidine kinase 1)TS (Thymidylate synthase)DNATK2 (Thymidine kinase 2)

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