作者
Henrik Gréen, Karin Skoglund, Franz Rommel, Rajaa A Mirghani, Kourosh Lotfi
发表日期
2010/4
期刊
European journal of clinical pharmacology
卷号
66
页码范围
383-386
出版商
Springer-Verlag
简介
Purpose
Imatinib is currently used for the treatment of chronic myeloid leukemia (CML). The main metabolite CGP74588 has similar potency to that of imatinib and is a product of CYP3A4 and CYP3A5 metabolism. However, the clinical significance of the metabolism on therapeutic response and pharmacokinetics is still unclear. We designed this study to investigate the role of the CYP3A activity in the response to imatinib therapy.
Methods
Fourteen CML patients were phenotyped for in vivo CYP3A activity using quinine as a probe drug. The plasma concentration ratio of quinine and its CYP3A metabolite was used for assessing CYP3A activity. The patients were divided into complete molecular responders with undetectable levels of BCR-ABL transcripts after 12 months of therapy and into partial molecular responders who had failed to achieve a complete …
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H Gréen, K Skoglund, F Rommel, RA Mirghani, K Lotfi - European journal of clinical pharmacology, 2010