Gemcitabine Elaidate
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. [ ]
Term info
Gemcitabine Elaidate
- CP-4126
- GEMCITABINE ELAIDATE
- Gemcitabine 5'-Elaidic Acid Ester
- Gemcitabine Elaidate
NCIT_C116978, NCIT_C128784, NCIT_C63923, NCIT_C157711, NCIT_C116977, NCIT_C157712
210829-30-4
CTRP, FDA
Gemcitabine Elaidate
231C73W7LG
Gemcitabine_5-Elaidic_Acid_Ester
624375
624375
Gemcitabine Elaidate
Pharmacologic Substance, Nucleic Acid, Nucleoside, or Nucleotide
C2703166
C79803
Term relations
- Ribonucleotide Reductase Inhibitor
- Pyrimidine Antagonist
- Chemical_Or_Drug_Has_Physiologic_Effect some DNA Synthesis Inhibition
- Chemical_Or_Drug_Has_Mechanism_Of_Action some Enzyme Inhibition
- Chemical_Or_Drug_Has_Physiologic_Effect some Positive Regulation of Apoptosis
- Chemical_Or_Drug_Affects_Gene_Product some Ribonucleotide Reductase
- Chemical_Or_Drug_Has_Physiologic_Effect some Nucleotide Biosynthesis Process