Gemcitabine elaidate 是 Gemcitabine 的亲脂性前药。它通过酯酶转化为 Gemcitabine 以被磷酸化。它具有抗肿瘤活性。

Gemcitabine elaidate, is 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.

Gemcitabine analog 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. Gemcitabine 5'-elaidic acid ester shows an enhanced cellular uptake and accumulation, resulting in increased conversion to active metabolites, compared to gemcitabine. This formulation of gemcitabine may be less susceptible to deamination and deactivation by deoxycytidine deaminase. Check for active clinical trials or closed clinical trials using this agent.

210829-30-4

C27H43F2N3O5

527.64

CO-101;反油酸吉西他滨;CP-4126;吉西他滨反油酸酯;Gemcitabine (elaidate);Gemcitabine 5'-elaidate

DMSO:26 mg/mL (49.28 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years