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Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.

The human CYP isoenzymes are involved in the metabolism of revexepride, which is mainly metabolized in vitro in humans by CYP3A4 (99.9%) with a minor contribution of CYP2D6 (0.1%). Revexepride exhibits direct inhibition of human CYP3A4 in vitro with IC50 values of 16-49 μM[1].

[1]. David Pierce, et al. A phase 1 randomized study evaluating the effect of omeprazole on the pharmacokinetics of a novel 5-hydroxytryptamine receptor 4 agonist, revexepride (SSP-002358), in healthy adults. Drug Des Devel Ther. 2015; 9: 1257-1268.

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