Gefitinib

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

L01XE02

White, crystalline, non- hygroscopic powder

Cytostatics

Tyrosine kinase inhibitor

119-120 ° C (crystals from toluene )

Slightly soluble in glacial acetic acid and in dimethylsulfoxide, soluble in pyridine, sparingly soluble in tetrahydrofuran, and slightly soluble in methanol, ethanol, ethyl acetate, 2-propanol and acetonitrile

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Gefitinib (trade name Iressa, AstraZeneca ) is an administrable as a tablet drug from the drug class of tyrosine kinase inhibitors. The usual dose is 250 mg daily.

Mechanism of Action

Gefitinib inhibits mainly the tyrosine kinases of the EGFR family (Epidermal Growth Factor Receptor, receptor for the epidermal growth factor ). In some tumors EGF receptors are overexpressed. Inhibition of EGF - receptors leads to slowing of tumor growth or even tumor regression.

Studies about application

In the years 2009 and 2010 therapy trials for the treatment of patients with non - small cell lung cancer have been published in which the administration of gefitinib compared with conventional chemotherapy. It was found that treatment with gefitinib was more effective in a subgroup of these patients, as treatment with a "standard" chemotherapy of carboplatin / cisplatin and taxol. However, gefitinib was more effective only if the corresponding patients had mutations in the EGFR gene. Documents such mutations not present, then gefitinib was worse effective than the standard therapy. These mutations were more common in female patients, patients who had never smoked, and to find patients with adenocarcinomas.

These results led to the American Society of Clinical Oncology recommended in its guidelines for the treatment of non-small cell lung cancer in 2009, used for patients with EGFR mutations gefitinib.

On 24 June 2009, the European Commission granted AstraZeneca AB, a marketing authorization of Iressa throughout the European Union for the treatment of non-small cell lung cancer with activating EGFR mutations.

Unwanted side effects

The possible side effects of gefitinib are mainly rashes and diarrhea.