Gefitinib

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Definition
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Pharmacodynamics (Effect)
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Gefitinib inhibits the "Epidermal Growth Factor Receptor" by preventing the ATP binding site of tyrosine kinase and thus autophosphorylation. This prevents the induction of the EGF-receptor-mediated signaling cascade to the cell nucleus. The consequences are reduced cell proliferation, angiogenesis and metastasis with simultaneously increased apoptosis rate.

Indication
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Breast carcinomas, chemotherapeutically pre-treated patients with non-small cell lung carcinoma.

Pregnancy/nursing period
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No sufficient data available, therefore no application during pregnancy and lactation recommended.

Undesirable effects
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  • Frequent: Acne-like exanthema (see Acne medicamentosa), vomiting, stomatitis, diarrhoea, paronychia, stomatitis, conjunctivitis.
  • Less frequent: lung diseases, corneal erosions, hypertrichosis.

Preparations
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Iressa

Note(s)
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In the USA, gefitinib has been approved for the treatment of non-small cell lung cancer (third therapy when the tumor progresses despite two different chemotherapies). In the meantime, results of a study have been published by the US FDA. In a preliminary analysis, this double-blind study involving almost 1700 people showed that gefitinib does not offer a significant survival advantage over placebo.

Literature
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  1. Knight LA et al (2004) The in vitro effect of gefitinib ('Iressa') alone and in combination with cytotoxic chemotherapy on human solid tumours. BMC Cancer 23: 83
  2. Mebes K et al (2007) Acneiform eruptions associated with EGFR inhibitor therapy in metastatic or-hypopharygeal carcinoma of the 13: 116-123

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Last updated on: 29.10.2020