Gefitinib
Gefitinib is a targeted cancer therapy that belongs to the class of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. It is specifically indicated for the treatment of non-small cell lung cancer (NSCLC) in patients whose tumors harbor EGFR-activating mutations. By blocking EGFR signaling, the drug inhibits tumor cell proliferation and survival.
Gefitinib is an EGFR-targeted therapy for NSCLC with specific genetic mutations.
Key facts at a glance
- ATC
- L01EB01
- RxNorm
- 328134
- Generic
- Gefitinib
- Class
- atc-l01
- Brands
- Iressa
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
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Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Treatment of metastatic non-small cell lung cancer (NSCLC) in patients whose tumors have EGFR-activating mutations (exon 19 deletions or exon 21 L858R point mutation). EGFR mutation testing is required prior to treatment initiation.
Gefitinib selectively inhibits the EGFR tyrosine kinase by binding to the intracellular kinase domain. This prevents EGFR autophosphorylation and blocks downstream signaling cascades involved in cell proliferation, survival, and tumor angiogenesis.
Common adverse effects include skin rash, diarrhea, acne, and nausea. May cause serious interstitial lung disease, hepatotoxicity, or ocular disorders. Use with caution in patients with hepatic impairment. Efficacy and tolerability should be monitored throughout treatment.
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy