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Imatinib

Brand names: Glivec®
Synonymes: Imatinibum, Imatinib mesylate, Imatinibmesilat
German: Imatinib

1 Definition

Imatinib is an active substance that belongs to the tyrosine-kinase inhibitor group of active ingredients. It is used in the treatment of various malign tumors, among others chronic myelocytic leukemias (CML) and gastrointestinal stromal tumors (GIST).

2 Chemistry

The empirical formula of Imatinib is: C29H31N7O. This cytostatic agent is an aromatic hydrocarbon. It has the form of a 2-phenylaminopyrimidine derivative.

3 Mechanism of Action

The chronic myelotic leukemia is caused through a singular genetic modification of the so called Philadelphia-chromosome. The modification happens through an exchange (translocation) of genetic material between the ninth chromosome and the twentysecond chromosome. The mutated cells synthesize the fusion protein BCR-Abl which is, in comparison to Abl, a more active tyrosine kinase. This increase in activity enables the unchecked proliferation of leukocytes.

Imatinib inhibits the tyrosine kinase and subsequently suppresses the pathological proliferation of the mutated hematopoietic stem cells.

4 Indications

Imatinib is effective against a broad spectrum of cancers. The most common indication is for chronic myelotic leukemia. Further it can be used against acute lymphatic leukemias, hypereosinophilic syndrome (HES), some skin tumors, malign masses present in the gastrointestinal tract , aggressive forms of mastocytosis and specific myeloproliferative disorders.

5 Form of administration

Imatinib is administered orally as tablets. With this form of administration It has a bioavailability of ~ 98%.

6 Undesirable Side effects

7 Drug interactions

Imantanib inhibts the glucuronidation of paracetamol. This makes the regular and simultaneous use of Imantinib and paracetamol problematic. The cytostatic also influences certain subgroups of the cytochrom P450 enzyme and thus can lead to interactions with additional substances. Imatinib inhibits the following subunits: CYP2C9, CYP2D6, CYP3A4 and CYP2C19. It acts as a substrate of CYP3A4.

8 Contraindications

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