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gefitinib

Structure via PubChem · Public domain (PubChem)

EntityQ417824· pop 25· linked from 582 articles

Also known as ZD 1839, ZD1839, 4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine

Gefitinib, sold under the brand name Iressa, is a medication used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR, but resistances to gefitinib can arise through other mutations. It is marketed by AstraZeneca and Teva.

Chemical data

Formula
C22H24ClFN4O3
Molecular weight
446.9 g/mol
IUPAC name
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
SMILES
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
InChIKey
XGALLCVXEZPNRQ-UHFFFAOYSA-N
XLogP
4.1
Polar surface area
68.7 Ų
H-bond donors
1
H-bond acceptors
8
Formal charge
0

via PubChem

Research

9,418 papers

via PubMed

~8 min read

Encyclopedic overview

9 sections
Contents
  • Mechanism of action
  • Clinical uses
  • Experimental uses
  • Studies
  • EGFR diagnostic tests
  • Adverse effects
  • Resistance
  • References
  • External links

Gefitinib, sold under the brand name Iressa, is a medication used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR, but resistances to gefitinib can arise through other mutations. It is marketed by AstraZeneca and Teva.

Gefitinib is a therapeutic alternative on the World Health Organization's List of Essential Medicines. It is available as a generic medication.

Excerpted from Wikipedia’s “gefitinib” article, available under the CC BY-SA 4.0 licence.