Preferred Label : Gemcitabine Elaidate;
NCIt synonyms : Gemcitabine 5'-Elaidic Acid Ester; Gemcitabine 5-Elaidic Acid Ester;
NCIt definition : A lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite
deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis
intracellularly by esterases, the prodrug gemcitabine is converted into the active
metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine
kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide
pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA
strand termination and apoptosis. Due to its lipophilicity, gemcitabine 5'-elaidic
acid ester exhibits an increased cellular uptake and accumulation, resulting in an
increased conversion to active metabolites, compared to gemcitabine. In addition,
this formulation of gemcitabine may be less susceptible to deamination and deactivation
by deoxycytidine deaminase.;
UNII : 231C73W7LG;
InChIKey : HESSNRGIEVBPRB-QDDPNBLJSA-N;
CAS number : 210829-30-4;
Molecule name : CP-4126;
Origin ID : C79803;
UMLS CUI : C2697495;
Currated CISMeF NLP mapping
- Semantic type(s)
- chemical_or_drug_affects_gene_product
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
