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Price of Gefitinib
Tarceva 25 mg tablet
* price without discount in nearest pharmacy. Price may vary.
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Gefitinib volume of distribution
* 1400 L (IV administration)
What is Gefitinib
Gefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa. (Wikipedia)
Gefitinib mechanism of action
Gefitinib inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas – for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation.
Dosage forms of Gefitinib
|Film-coated tablet||Oral use||250 mg|
|Tablet, coated||oral||250 mg/1|
Astra Zeneca Pharmaceuticals Lp
Humans and other mammals
Indication of Gefitinib
For the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies.
Toxicity of Gefitinib
The acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m sup 2 /sup (about 80 times the recommended clinical dose on a mg/m sup 2 /sup basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash.
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