Article
A UGT2B10 splicing polymorphism common in african populations may greatly increase drug exposure.
The Journal of pharmacology and experimental therapeutics - 1 Feb 2015
Fowler Stephen, Kletzl Heidemarie, Finel Moshe, Manevski Nenad, Schmid Paul, Tuerck Dietrich, Norcross Roger D, Hoener Marius C, Spleiss Olivia, Iglesias Victor A
Abstract excerpt
RO5263397 [(S)-4-(3-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine], a new compound that showed promising results in animal models of schizophrenia, is mainly metabolized in humans by N-glucuronidation. Enzyme studies, using the (then) available commercial uridine 5'-diphosphate-glucuronosyltransferases (UGTs), suggested that UGT1A4 is responsible for its conjugation. In the first clinical trial, in which...
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