Gemcitabine Hydrochloride: A Fluorinated Deoxycytidine Analog with Antitumor Activity
Gemcitabine [
G0544] and its hydrochloride are fluorinated deoxycytidine analogs with antitumor activity against solid tumors. Once inside the cell, gemcitabine is rapidly phosphorylated by deoxycytidine kinase to form the active metabolites gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP). dFdCDP inhibits ribonucleotide reductase, which is responsible for producing the deoxynucleotides required for DNA synthesis and repair. dFdCTP can be incorporated into DNA, leading to inhibition of DNA synthesis. On the other hand, a concomitant treatment with gemcitabine and cisplatin [
D3371] is used for the treatment of several different types of cancer. Cisplatin acts by formation of platinum (Pt)-DNA adducts; gemcitabine acts by dFdCTP incorporation into DNA, subsequently leading to inhibition of exonuclease and DNA repair. (The product is for research purpose only.)