|Brivudine Phosphoramidate (Code C1882)|
|Terms & Properties|
Preferred Name: Brivudine Phosphoramidate
Definition: A small molecule phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVdU) with potential antineoplastic activity. Selectively active against tumor cells expressing high levels of thymidylate synthase (TS), brivudine is converted intracellularly by TS to bromovinyldeoxyuridine monophosphate (BVdUMP) which competes with the natural substrate, deoxyuridine monophosphate, for binding to TS. Unlike TS inhibitors, this agent is a reversible substrate for TS catalysis. Thus, TS retains activity and converts BVdUMP into cytotoxic metabolites. As key enzyme in the de novo synthesis of dTMP, TS is an enzyme critical to DNA biosynthesis and is overexpressed in many solid tumors.
NCI-GLOSS Definition: A substance that is being studied for its ability to make cancer cells respond to drugs to which they have become resistant. It is a type of nucleoside analog.
Label: Brivudine Phosphoramidate
NCI Metathesaurus Link: C0964443 (see NCI Metathesaurus info)
Synonyms & Abbreviations: (see Synonym Details)
|(E)-5-(2-Bromovinyl)-2'-deoxy-5'-uridyl Phenyl L-methoxyalaninylphosphoramidate|
External Source Codes:
|PDQ Closed Trial Search ID||38549|
|PDQ Open Trial Search ID||38549 (check for NCI PDQ open clinical trial info)|
|Name||Value (qualifiers indented underneath)|
|Semantic_Type||Nucleic Acid, Nucleoside, or Nucleotide|
Additional Concept Data:
|Defined Fully by Roles: No|