Gemcitabine hydrochloride

Описание

Gemcitabine is a novel nucleoside analog that was launched in 1995 in the Netherlands for the treatment of non-small cell lung cancer (nsclc) and in Sweden for pancreatic cancer. Gemcitabine is a prodrug which is phosphorylated intracellularly by deoxycytadine kinase to its active forms, the di- and triphosphates which bind to DNA competitively. This insertion inhibits processes required for DNA synthesis and metabolism, the essential function for both cell replication and repair. Furthermore, gemcitabine displays an extraordinary array of self-potentiating mechanisms that increase the concentration and prolong the retention of its active nucleotides in tumor cells. The title compound has shown activity against a wide spectrum of human solid tumors including colon, mammary, breast, bladder cancers. Synergistic activity of gemcitabine with other anticancer agents such as cisplatin has been reported.

Химические свойства

White crystalline granular, odorless

Определение

ChEBI: A 2'-deoxycytidine hydrochloriode having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine hydrochloride is used in the treatment of various carcinomas, including non-small cell lung cancer, pancreatic ca cer, bladder cancer and breast cancer.

Биологическая активность

Deoxycytidine analog that inhibits DNA synthesis. Metabolized to form gemcitabine triphosphate (dFdCTP) and gemcitabine diphosphate (dFdCDP). dFdCTD inhibits ribonucleotide reductase causing a reduction in cellular nucleotides. dFdCTP is incorporated in DNA resulting in DNA strand termination. Displays antitumor activity in vitro and in vivo .