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0091270007305298v1
47/10/1277    most recent
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PHARMACOKINETICS

Influence of Food Intake on the Pharmacokinetics of Miglustat, an Inhibitor of Glucosylceramide Synthase

Paul L. M. van Giersbergen, PhD and Jasper Dingemanse, PhD

From Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Allschwil, Switzerland.

The objective of this study was to investigate the effect of food on the pharmacokinetics of miglustat, an inhibitor of glucosylceramide synthase. Twenty-four healthy male (n = 9) and female (n = 15) subjects were treated in a randomized, 2-way crossover design with a single oral dose of 100 mg miglustat with or without food. Consumption of a standard high-fat breakfast within 30 minutes before administration of miglustat significantly reduced peak exposure but did not significantly affect the extent of systemic exposure to miglustat. The peak plasma concentration (Cmax) decreased by 36% on average following administration with food. Area under the plasma concentration-time curve (AUC0-{infty}) showed a modest (14%) decrease with food, but the 90% confidence interval was within the acceptance limit of 80% to 125%. The median (min-max) time to Cmax (tmax) was prolonged from 2.5 (1.0-4.0) hours in the fasted state to 4.5 (1.5-8.0) hours in the fed state, whereas the apparent terminal half-life was approximately 8 hours and not affected by food. In conclusion, the intake of food has an effect on some pharmacokinetic parameters such as Cmax and tmax but does not affect the extent of exposure to miglustat. The observed effects of food intake on the pharmacokinetics of miglustat are not considered to be of clinical relevance.

Key Words: Miglustat • food effect • pharmacokinetics • healthy subjects • gender effect

Address for correspondence: Paul van Giersbergen, PhD, Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology, Gewerbestrasse 16, 4123 Allschwil, Switzerland; e-mail: paul.vangiersbergen{at}actelion.com.


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