Gemcitabine (Gemzar)

Nucleoside antimetabolite that undergoes intracellular phosphorylation to activated diphosphate and triphosphate forms.

A nucleoside analog of deoxycytidine.

Undergoes metabolic activation by kinases to form a cytotoxic trinucleotide in the cell.

Metabolic inactivation is by deamination is catalyzed by cytidine deaminase or after phosphorylation by deoxycytidylate deaminase.

Structure similar to cytarbrine.

Exerts effects by interacting with genomic DNA.

A nucleoside analogue that when incorporated into DNA inhibits DNA polymerase during cell replication or repair.


Induces an S-phase arrest and triggers apoptosis.

Fixed dose rate of 10mg/m2/min allows maximum intracellular accumulation of the active triphosphate form of the drug.

Phase II studies reveal response rates of 4-18% in soft tissue sarcomas.

A potent radiation sensitizer in vitro and in vivo.

In a phase III randomized study og the addition of gemcitabine to concurrent cisplatin chemoradiotherapy in locally advanced cervical cancer: 515 treatment naive stage IIB to IVA disease patients-3 year PFS significantly improved in gemcitabine arm, as was time to progression, and overall survival (Duenas-

May be associated with posterior reversible encephalopathy syndrome.

Its use may be associated with an increased rate of toxicity during and after antibiotic therapy suggesting intratumor bacteria metabolize gemcitabine mean to an inactive form.

Leave a Reply

Your email address will not be published. Required fields are marked *