Locally advanced or metastatic non small cell lung carcinoma
Adult: 250 mg once daily.

Special Populations: For patients on potent CYP3A4 inducer: 500 mg daily if tolerated. For patients with poorly tolerated diarrhoea or skin ADR: Up to 14 days therapy interruption followed by reinstatement of the 250 mg daily dose.
Hypersensitivity; pregnancy; lactation.
Warnings / Precautions
Severe renal or hepatic impairment; idiopathic pulmonary fibrosis; acute onset or worsening of pulmonary or eye symptoms. Monitor hepatic function periodically. Monitor regularly for changes in prothrombin time or International Normalized Ratio in patients on warfarin treatment.
Adverse Reactions
GI disturbances, anorexia; hepatotoxicity; rash, acne, dry skin, skin blemishes; weakness; peripheral oedema; amblyopia; cough, dyspnoea; conjunctivitis; mouth ulceration; eye irritation, corneal membrane sloughing, ocular ischaemia or haemorrhage; pancreatitis; toxic epidermal necrolysis; erythema multiforme; hypersensitivity reactions.
Potentially Fatal: Interstitial lung disease.
Drug Interactions
CYP3A4 inducers and H2-receptor antagonists decrease effectiveness of gefitinib. CYP3A4 inhibitors increase efficacy of gefitinib. Increased metoprolol concentrations. INR elevations and/or bleeding events with warfarin. Increased plasma concentrations of metoprolol when used with gefitinib.
See Below for More gefitinib Drug Interactions
Mechanism of Actions
Gefitinib is an anilinoquinazoline. Gefitinib generally attaches to epidermal growth factor receptors (EGFRs), thereby blocking the attachment of EGF and the activation of tyrosine kinase. It is used as monotherapy for the treatment of locally advanced or metastatic nonsmall cell lung cancer after failure of both platinum-based and docetaxel chemotherapies.
Film-coated tab: May be taken with or without food. (May also be dispersed in ½ glass of plain, non-carbonated water. No other liqds should be used. Drop the tab in water & stir w/o crushing until it disperses (approx 10 min). Drink immediately. Rinse glass w/ another ½ glass of water & drink. Dispersed liqd may also be administered via NG tube.)
ATC Classification
L01XE02 - gefitinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Available As
  • Gefitinib 250 mg
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