cp 4126 hydrochloride

Gemcitabine elaidate (CP-4126) hydrochloride is a lipophilic pro-drug of Gemcitabine, converted to Gemcitabine by esterases for phosphorylation. Unlike gemcitabine, Gemcitabine elaidate hydrochloride can be administered orally, displaying schedule and dose-dependent toxicity and antitumor activity.

Gemcitabine elaidate (CP-4126), 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.