Gefitinib
Generic Details
Generic Name
Gefitinib
Other Names
- Iressa
Drug Class
- Tyrosine kinase inhibitor
Chemical Formula
C22H24ClFN4O3
Molecular Weight
446.91 g/mol
Mechanism of Action
- Inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase activity
Indications
- Non-small cell lung cancer (NSCLC) with EGFR mutations
Common Dosage Forms
- Tablet
Typical Dosage
- 250mg orally once daily on an empty stomach
Pediatric Dosage
Geriatric Dosage
Side Effects
- Diarrhea
- Skin rash
- Interstitial lung disease
- Hepatotoxicity
- Anorexia
Contraindications
- Hypersensitivity to gefitinib
- Pregnancy
Pregnancy Category
- Category D
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Strong CYP3A4 inducers/inhibitors
- Proton pump inhibitors
Overdose Symptoms
Antidote for Overdose
Storage Conditions
- Store at room temperature away from moisture and heat
Pharmacokinetics
- Absorption: Well absorbed orally
- Distribution: Protein-bound, distributed widely in tissues
- Metabolism: Primarily hepatic, CYP3A4
- Excretion: Mainly in feces
Precautions
- Regular monitoring of liver function tests
- Close monitoring for interstitial lung disease
Warnings
- Risk of severe diarrhea and skin reactions
- Risk of interstitial lung disease