Product Information
Registration Status: ActiveGEMITA LYOPHILISED POWDER FOR SOLUTION FOR INJECTION 1g/vial is approved to be sold in Singapore with effective from 2016-01-25. It is marketed by FRESENIUS KABI (SINGAPORE) PTE LTD, with the registration number of SIN14926P.
This product contains Gemcitabine 1g/vial in the form of INTRAVENOUS INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION. It is approved for INTRAVENOUS use.
This product is manufactured by Fresenius Kabi Oncology Limited in INDIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. As with fluorouracil and other analogues of pyrimidines, the drug replaces one of the building blocks of nucleic acids, in this case cytidine, during DNA replication. The process arrests tumor growth, as new nucleosides cannot be attached to the "faulty" nucleoside, resulting in apoptosis (cellular "suicide"). Gemcitabine is used in various carcinomas: non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. It is being investigated for use in oesophageal cancer, and is used experimentally in lymphomas and various other tumor types.
Indication
Gemcitabine is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy; metastatic ovarian cancer; inoperable, locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer; and locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas.
Mechanism of Action
Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occurs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine diphosphate also inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Finally, Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA.
Pharmacokinetics
- Absorption
- The pharmacokinetics of gemcitabine are described by a 2-compartment model.
- Distribution
- * 50 L/m^2 [infusions lasting <70 minutes] * 370 L/m^2 [long infusions]
- Metabolism
- Transformed via nucleoside kinases to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate. Can also undergo deamination via cytidine deaminase to an inactive uracil metabolite (dFdU).
- Elimination
Clearance
* 92.2 L/hr/m2 [Men 29 yrs] * 75.7 L/hr/m2 [Men 45 yrs] * 55.1 L/hr/m2 [Men 65 yrs] * 40.7 L/hr/m2 [Men 79 yrs] * 69.4 L/hr/m2 [Women 29 yrs] * 57 L/hr/m2 [Women 45 yrs] * 41.5 L/hr/m2 [Women 65 yrs] * 30.7 L/hr/m2 [Women 79 yrs]
Toxicity
Myelosuppression, paresthesias, and severe rash were the principal toxicities, LD50=500 mg/kg (orally in mice and rats)
Active Ingredient/Synonyms
2'-Deoxy-2',2'-difluorocytidine | 2',2'-Difluorodeoxycytidine | 4-amino-1-((2R,4R,5R)-3,3-Difluoro-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one | Gemcitabin | Gemcitabina | Gemcitabine | Gemcitabinum | Gemcitabine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.