Suicide attempt with an overdose of imatinib

Abstract

Imatinib is approved for the treatment of chronic myelogenous leukaemia (CML) as well as gastrointestinal stromal tumour (GIST), both of which show dysregulated imatinib-sensitive tyrosine kinase activity. Imatinib is rapidly absorbed after oral administration (bioavailability 86%) and is mainly metabolized by the CYP3A4 and CYP3A5 isoenzymes of the liver [1]. Although the drug is usually well-tolerated, grade 1–2 adverse effects, such as musculoskeletal events, are frequently observed [2–4]. In a phase I clinical trial in patients with CML, the minimum therapeutic dose of imatinib required to obtain an optimal therapeutic response was determined to be 300 mg day−1. However, the maximum tolerated dose has not yet been defined. In addition, there have been few case reports of imatinib overdose [5]. We herein report the results of a pharmacokinetic analysis in a patient with CML who took 2000 mg of imatinib as a single dose together with brotizolam and triazolam in an attempt to commit suicide.