Gemcitabine is a nucleoside analog and a chemotherapeutic agent. It was originally investigated for its antiviral effects, but it is now used as an anticancer therapy for various cancers.[A233135] Gemcitabine is a cytidine analog with two fluorine atoms replacing the hydroxyl on the ribose.[A233145] As a prodrug, gemcitabine is transformed into its active metabolites that work by replacing the building blocks of nucleic acids during DNA elongation, arresting tumour growth and promoting apoptosis of malignant cells.[L32960] The structure, metabolism, and mechanism of action of gemcitabine are similar to [cytarabine], but gemcitabine has a wider spectrum of antitumour activity.[A233140] Gemcitabine is marketed as Gemzar and it is available as intravenous injection. It is approved by the FDA to treat advanced ovarian cancer in combination with [carboplatin], metastatic breast cancer in combination with [paclitaxel], non-small cell lung cancer in combination with [cisplatin], and pancreatic cancer as monotherapy.[L32950] It is also being investigated in other cancer and tumour types.
Gemcitabine is a chemotherapeutic agent used as monotherapy or in combination with other anticancer agents. In combination with [carboplatin], it is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy.[L32950] Gemcitabine in combination with [paclitaxel] is indicated for the first-line treatment of patients with metastatic breast cancer after failure of prior anthracycline-containing adjuvant chemotherapy, unless anthracyclines were clinically contraindicated.[L32950] In combination with [cisplatin], gemcitabine is indicated for the first-line treatment of patients with inoperable, locally advanced (Stage IIIA or IIIB) or metastatic (Stage IV) non-small cell lung cancer (NSCLC).[L32950] Dual therapy with cisplatin is also used to treat patients with Stage IV (locally advanced or metastatic) transitional cell carcinoma (TCC) of the bladder.[L32955] Gemcitabine is indicated as first-line treatment for patients with locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas. Gemcitabine is indicated for patients previously treated with [fluorouracil].[L32950]
Categories
Antimetabolites
Antineoplastic Agents
Antineoplastic and Immunomodulating Agents
Carbohydrates
Cytidine Deaminase Substrates
Deoxycytidine
Deoxyribonucleosides
Drugs that are Mainly Renally Excreted
Enzyme Inhibitors
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Narrow Therapeutic Index Drugs
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Nucleic Acid Synthesis Inhibitors
Nucleic Acids, Nucleotides, and Nucleosides
Nucleoside Metabolic Inhibitor
Nucleosides
P-glycoprotein substrates
P-glycoprotein substrates with a Narrow Therapeutic Index
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS.
Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682
