What it does
Geftinib is a medication used to treat certain types of lung cancer by blocking the growth of cancer cells.
Commonly used for: lung cancer (non-small cell lung cancer)
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 20:48:28 · updated 2026-07-26 11:38:57
About this medicine
Geftinib is a medication used to treat certain types of lung cancer by blocking the growth of cancer cells.
What it treats
- lung cancer (non-small cell lung cancer)
How it works
It works by blocking a specific protein that helps cancer cells grow and divide, slowing down their growth.
Who it's for
This medication is for adults diagnosed with specific types of lung cancer.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: geftinib
Gefitinib is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, primarily used in the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations. It works by blocking the phosphorylation and activation of signaling pathways that promote cell proliferation and survival, thus inhibiting cancer cell growth.
Indications
- Non-small cell lung cancer (NSCLC) with EGFR mutations
- Locally advanced or metastatic NSCLC after failure of chemotherapy
- First-line treatment for patients with specific EGFR mutations
Dosage
Children: Refer to the BNF for Children for specific dosage guidelines, as pediatric use is not commonly established.
Adults: Refer to the BNF for specific dosing information, typically starting at 250 mg once daily.
Mechanism of action
Gefitinib selectively binds to the ATP-binding site of the EGFR tyrosine kinase domain, inhibiting its phosphorylation. This results in the downregulation of downstream signaling pathways, particularly the MAPK and PI3K/AKT pathways, which are involved in cell division, survival, and angiogenesis.
Pharmacodynamics
The pharmacodynamics of gefitinib involve the inhibition of EGFR-mediated signaling, leading to reduced tumor cell proliferation and increased apoptosis in cancer cells that overexpress EGFR. The drug has shown efficacy in patients whose tumors possess specific mutations in the EGFR gene, leading to improved survival rates compared to conventional chemotherapy.
Pharmacokinetics
Gefitinib has a bioavailability of approximately 60% when taken orally. It is extensively metabolized in the liver by cytochrome P450 enzymes, primarily CYP3A4, with a half-life of approximately 48 hours. The drug exhibits linear pharmacokinetics at doses up to 500 mg. It is primarily excreted in the feces, with a small percentage eliminated in the urine.
Contra-indications
- Hypersensitivity to gefitinib or any component of the formulation
- Severe hepatic impairment
Adverse effects
- Diarrhea
- Rash
- Nausea
- Vomiting
- Anorexia
- Fatigue
- Interstitial lung disease
- Hepatotoxicity
- Corneal disorders
Interactions
- Strong CYP3A4 inducers may decrease gefitinib efficacy
- CYP3A4 inhibitors may increase gefitinib levels and toxicity
- Antacids and proton pump inhibitors may reduce gefitinib absorption
Precautions
- Monitor for signs of interstitial lung disease
- Use caution in patients with pre-existing hepatic impairment
- Assess for potential drug interactions due to hepatic metabolism
Pregnancy
Use is not recommended during pregnancy due to potential harm to the fetus.
Breast-feeding
It is not known whether gefitinib is excreted in human milk. Use caution if breastfeeding.
Storage
Store at room temperature, away from moisture and heat.
Formulations
- Tablets: 250 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.