gemcitabine

Gemcitabine is a nucleoside analog and antimetabolite chemotherapy drug used to treat various cancers, including pancreatic, non-small cell lung, ovarian, breast, bladder, and testicular cancers. It acts as a prodrug that is transported into cells via nucleoside transporters and phosphorylated by deoxycytidine kinase to its active forms. The diphosphate metabolite inhibits ribonucleotide reductase (reducing the pool of deoxynucleotides needed for DNA synthesis), while the triphosphate form is incorporated into DNA during replication. This incorporation results in masked chain termination—after one additional nucleotide is added following gemcitabine’s insertion into DNA, further elongation halts and apoptosis ensues. Gemcitabine may be used alone or in combination with other chemotherapeutic agents such as carboplatin (for ovarian cancer), paclitaxel (for breast cancer), or cisplatin (for lung and bladder cancers). It was originally developed for antiviral purposes but found broader use as an anticancer agent due to its mechanism of action.

Brand names

GemzarInfugem

Other names

2'-deoxy-2',2'-difluorocytidine2',2'-DifluorodeoxycytidineGemcitabine hydrochlorideGemcitabinum