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Version: 16.11d (Release date: 2016-11-28)
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Gemcitabine Prodrug LY2334737 (Code C102856)

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Terms & Properties

Preferred Name: Gemcitabine Prodrug LY2334737

Definition: An orally available valproic acid prodrug of gemcitabine, a broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine prodrug LY2334737 is hydrolyzed by carboxylesterase 2 (CES2) and releases gemcitabine systemically over a period of time consistent with formation rate-limited kinetics. In turn, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate and triphosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually the induction of apoptosis. Compared to gemcitabine, this prodrug is able to avoid hydrolysis in enterocytes and the portal circulation thus avoiding first pass metabolism and increasing systemic gemcitabine availability. In addition, the slow release of gemcitabine may enhance efficacy while lowering toxicity. CES2, a serine ester hydrolase, is expressed in certain tumors which may allow for increased conversion of gemcitabine at the tumor site thus increases cytotoxicity.

Display Name: Gemcitabine Prodrug LY2334737

Label: Gemcitabine Prodrug LY2334737

NCI Thesaurus Code: C102856 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3252354  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Gemcitabine Prodrug LY2334737
LY2334737

External Source Codes: 
PDQ Closed Trial Search ID 737787
PDQ Open Trial Search ID 737787 (check for NCI PDQ open clinical trial info)
UMLS CUI C3252354

Other Properties:
Name Value (qualifiers indented underneath)
code C102856
Contributing_Source CTRP
Semantic_Type Nucleic Acid, Nucleoside, or Nucleotide
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C102856

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