Imatinib

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Imatinib (UK: Glivac®; US: Gleevac®) is a relatively low potency tyrosine kinase (KIT) inhibitor used in the treatment of Philadelphia-positive chronic myeloid leukaemia and KIT positive gastrointestinal stromal tumours. It is one of several examples of where understanding of the steps in carcinogenesis have allowed targetting of specific molecular targets.

In GIST, response to imatinib can be assessed using PET or CT scanning. A good response supports the continued usage of the drug, whereas a poor response, not surprisingly, predicts a lack of efficacy. Secondary resistance to the drug may be a result of selection for a Ser650Thr missense mutation.[1]

A chronic side effect is heart failure,[2][3] whose clinical importance will only be demonstrated in long term studies. Interestingly its actions on myocytes may yet have therapeutic application.

Contents

Pharmacology

Side-effects

See Also

NICE Guidance: http://www.nice.org.uk/page.aspx?o=TA086

References

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