Impact of the organic cation transporter 2 inhibitor cimetidine on the single-dose pharmacokinetics of the glucosylceramide synthase inhibitor lucerastat in healthy subjects
- 13 December 2019
- journal article
- research article
- Published by Springer Science and Business Media LLC in European Journal of Clinical Pharmacology
- Vol. 76 (3), 431-437
- https://doi.org/10.1007/s00228-019-02808-9
Abstract
Lucerastat is an orally available glucosylceramide synthase inhibitor with a potential to provide substrate reduction therapy for Fabry patients independent of their α-galactosidase A genotype. In humans, lucerastat is mainly eliminated as unchanged parent compound through renal excretion both by active secretion and passive filtration. In vitro studies indicated that lucerastat is a substrate of human organic cation transporter 2 (OCT2) mainly expressed in the kidney.Keywords
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