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Buy Generic Iressa (Gefitinib) »



US Brand: Iressa

Indian (Generic) Brand: Geftinat

Manufacturing: Natco (India)

Active Substance: Gefitinib

Dosage: 250mg

Form release: Bottle 30 tablets

Order: through enquiry form

Shipping time: 9 – 14 days








Description


Gefitinib being a selective inhibitor of tyrosine kinase epidermal growth factor receptors, whose expression occurs in many tumors sólidnyh inhibits tumor growth, metastasis and angiogenesis, and accelerates apoptosis of tumor cells.

Inhibits the growth of different human tumor cell lines and enhances the antitumor activity of chemotherapeutic drugs, radiation and hormonal therapy.

Gefitinib is a drug that is used to treat several types of lung cancer. It works by preventing lung cancer cells from growing and multiplying. Many cells, including cancer cells, have receptors on their surfaces for epidermal growth factor (EGF), a protein that is normally produced by the body and that promotes the growth and multiplication of cells. When EGF attaches to epidermal growth factor receptors (EGFRs), it causes an enzyme called tyrosine kinase to become active within the cells. Tyrosine kinase triggers chemical processes that cause the cells, including cancer cells, to grow, multiply, and spread. Gefitinib attaches to EGFRs and thereby blocks the attachment of EGF and the activation of tyrosine kinase. This mechanism for stopping cancer cells from growing and multiplying is very different from the mechanisms of chemotherapy and hormonal therapy. Gefitinib was approved by the FDA in May 2003.

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Mechanism of Action



Gefitinib is an EGFR tyrosine kinase inhibitor. It works by binding to the intracellular enzyme (tyrosine kinase) of the EGFR to directly block signals turned on by triggers outside or inside the cell.

The activity of epidermal growth factor and its receptor, the EGFR, have been identified as key drivers in the process of cell growth and replication. Heightened activity at the EGF receptor, whether caused by an increase in the concentration of ligand around the cell, an increase in receptor numbers or a decrease in receptor turnover or receptor mutation, can lead to an increase in the drive for the cell to replicate. There is now a body of evidence to show that the EGFR-mediated drive is increased in a wide variety of solid tumours, including non-small cell lung cancer, prostate cancer, breast cancer, gastric cancer, colon cancer, ovarian cancer and tumours of the head and neck.

Gefitinib is an anilinoquinazoline with the chemical name 4-Quinazolinamine. The mechanism of the clinical antitumor action of gefitinib is not fully characterized. Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells. No clinical studies have been performed that demonstrate a correlation between EGFR receptor expression and response to gefitinib.

Dosage Modifications



Non-small Cell Lung Cancer

Indicated for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test

250 mg PO qDay until disease progression or unacceptable toxicity

Withhold for up to 14 days following adverse effects

- Acute onset or worsening pulmonary symptoms (dyspnea, cough, fever)

- Grade 2 ALT and/or AST elevations

- Grade 3 diarrhea

- Signs and symptoms of severe or worsening ocular disorders including keratitis

- Grade 3 skin reactions

- May resume gefitinib when adverse effect fully resolves or improves to Grade 1

Permanently discontinue for

- Confirmed interstitial lung disease

- Severe hepatic impairment

- Gastrointestinal perforation

- Persistent ulcerative keratitis

Coadministration with strong CYP3A4 inducers

- Increase dose to 500 mg PO qDay in the absence of severe adverse drug reactions

- Resume 250 mg qDay after discontinuation of the strong CYP3A4 inducer