gemcitabine_HCl: profile and news

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Other information

Indication
For the first-line treatment of patients with metastatic breast cancer , locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer and as first-line treatment for patients with adenocarcinoma of the pancreas

Pharmacology
Gemcitabine is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (or DNA synthesis phase of the cell cycle), stopping normal development and division. Gemcitabine blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Gemcitabine blocks the incorporation of the thymidine nucleotide into the DNA strand.

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 inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA.

Drug Category
Radiation-Sensitizing Agents; Immunosuppressive Agents; Antivirals; Antimetabolites; Antineoplastic Agents; ATC:L01BC05

Brand Names/Synonyms
CCRIS 8984; DDFC; Dfdc; GEO; Gemcin; Gemcitabina [Inn-Spanish]; Gemcitabine; Gemcitabine Hcl; Gemcitabine Hydrochloride; Gemcitabine [Usan:Ban:Inn]; Gemcitabinum [Inn-Latin]; Gemtro; Gemzar

Dosage Forms
lyophilized powder for injection

Absorption
100%

Interactions
-->Interactions for Gemcitabine:

No specific drug interaction studies have been conducted. For information on the pharmacokinetics of Gemzar and cisplatin in combination, see Drug Interactions under CLINICAL PHARMACOLOGY section.

Chemical IUPAC Name
4-amino-1-[3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1H-pyrimidin-2-one

Chemical Formula
C9H11F2N3O4

Half Life
short infusions ranged from 32 to 94 minutes, and the value for long infusions vary from 245 to 638 minutes, depending on age and gender

Drug Type
Approved Drug

# Accession No
APRD00201

CAS Registry Number
95058-81-4