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Gefitinib information from DrugsUpdate  

See Available Brands of Gefitinib in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Gefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets proteins in malignant cells. It is marketed by AstraZeneca and Teva under the trade name Iressa.

Pharmacodynamics

Pharmacokinetics

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.

Gefitinib Indications / Gefitinib Uses

Information Not Available

Gefitinib Adverse Reactions / Gefitinib Side Effects

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.

Precautions

Information Not Available

Special 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.

Other 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.

Other Interactions

Information Not Available

Dosage

Oral
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.

Food(before/after)

Film-coated tab: May be taken with or without food. (May also be dispersed in ? glass of plain, non-carbonated water. No other liqds should be used. Drop the tab in water & stir without crushing until it disperses (approx 10 mins). Drink immediately. Rinse glass w/ another ? glass of water & drink. Dispersed liqd may also be administered via NG tube.)

List of Contraindications

Gefitinib and Pregnancy

Contraindicated in pregnancy

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Gefitinib and Lactation

Contraindicated in lactation

Gefitinib and Children

Information Not Available

Gefitinib and Geriatic

Information Not Available

Gefitinib and Other Contraindications

Hypersensitivity; pregnancy; lactation

Storage

Information Not Available

Lab interference

Information Not Available

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