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.
화학적 성질
White crystalline granular, odorless
정의
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.
생물학적 활성
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 .
