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Generic Name: Gefitinib
Brand Name(s): Iressa®
IUPAC: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
FDA Approval: yes
Manufacturer Link
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Usage: Gefitinib was aproved by the FDA on May 5, 2003 as a third line therapy for non-small cell lung cancer that is unresponsive to certain
chemotherapy drugs. Iressa® is administered as an oral tablet.
Mechanism: Gefitinib (Iressa®) is a
tyrosine kinase inhibitor. It works to inhibit the epidermal
growth factor receptor (EGFR) pathway. EGFR is a receptor found on the cell surface that binds EGF
protein, and phosphorylates (adds a phosphate group) tyrosine residues of proteins in a signal pathway. EGFR is overexpressed in a large percentage of cancers, and cancers with such
overexpression are more likely to develop quickly and to
metastasize. Gefitinib binds the EGFR within the cell and blocks the tyrosine kinase, switching off the EGFR signal for the cancer cell to grow.
(1)
Side Effects: Common side effects include diarrhea, rash, acne, dry skin, nausea and vomiting. Most of these side effects are mild to moderate and most commonly occur during the first month of treatment. Women should not become pregnant while taking this drug as it may cause harm to the unborn child. There have been rare cases of interstitial lung disease while taking this drug. Symptoms of this condition include difficulty breathing and cough.
(2)(3)
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