Last reviewed 2026-05-15 · How we verify

Gefitinib mono-therapy

Gefitinib is a tyrosine kinase inhibitor that selectively blocks epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation.

Gefitinib is a tyrosine kinase inhibitor that selectively blocks epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. Used for Non-small cell lung cancer (NSCLC) with EGFR mutations, Advanced or metastatic NSCLC as first-line monotherapy.

At a glance

Mechanism of action

Gefitinib binds to the ATP-binding pocket of EGFR and prevents autophosphorylation of the receptor, thereby blocking downstream signaling pathways (PI3K/Akt and MAPK/ERK) that drive cell growth and survival. This mechanism is particularly effective in tumors with activating EGFR mutations, which are common in non-small cell lung cancer, especially in Asian populations and never-smokers.

Approved indications

• Non-small cell lung cancer (NSCLC) with EGFR mutations
• Advanced or metastatic NSCLC as first-line monotherapy

Common side effects

• Rash/acneiform dermatitis
• Diarrhea
• Nausea
• Vomiting
• Anorexia
• Asthenia/fatigue
• Interstitial lung disease

Key clinical trials

• Gefitinib With or Without Chemotherapy in Brain Metastases From Non-small Cell Lung Cancer (PHASE3)
• Phase II Study of Gefitinib Plus Nimotuzumab Versus Gefitinib in Non-small Cell Lung Cancer (PHASE2)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Gefitinib mono-therapy CI brief — competitive landscape report
• Gefitinib mono-therapy updates RSS · CI watch RSS
• Sun Yat-sen University portfolio CI