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Gefitinib

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Gefitinib

Gefitinib is a drug used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor in target cells. More

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Description

Gefitinib is a drug used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor in target cells.

Generic Name

Gefitinib

Chemical names

Iressa; efitinib; ZD1839; Irressat; N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

Brand names

Chemofit, Gefitec, Gefitero, Gefonib, Geftib, Geftifos, Geftilon, Geftinat

IUPAC name

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine

Pharmacokinetics

Absorbed slowly after oral administration

Actions

Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells.

Dosage/Dosage form

The recommended daily dose is one 250mg as PO.

Therapeutic uses

It is a chemotherapeutic agent, prescribed for non small cell lung cancer.

Adverse effects/Side effects

Hepatotoxicity; GI disturbances, acne, anorexia; rash, dry skin, weakness; skin blemishes; 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.

Interaction

  • CYP3A4 inducers and H2-receptor antagonists decrease effectiveness of gefitinib.
  • CYP3A4 inhibitors increase efficacy of gefitinib.
  • Increased metoprolol concentrations.
  • Increased plasma concentrations of metoprolol when used with gefitinib.
  • INR elevations and/or bleeding events with warfarin. 

Contraindications

Hypersensitivity; pregnancy; lactation

Storage

Store it at controlled room temperature.

Information

Molecular weight

446.902

Molecular formula

C22H24ClFN4O3

CAS number

184475-35-2

Precautions

  • Severe renal or hepatic impairment; idiopathic pulmonary fibrosis; acute onset or worsening of pulmonary or eye symptoms.
  • Monitor hepatic function periodically.
  • Changes in prothrombin time or International Normalized Ratio Monitor regularly in patients on warfarin treatment.

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