Revexepride

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

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Research Areas >> Others

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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