Telotristat etiprate

Telotristat etiprate (CAS No.: 1137608-69-5) is an orally bioavailable small-molecule tryptophan hydroxylase (TPH) inhibitor prodrug. After entering the body, it is converted to its active form, telotristat (LP-778902). By binding to TPH and inhibiting its activity, it reduces the synthesis of peripheral serotonin (5-hydroxytryptamine, 5-HT), thereby improving serotonin-mediated gastrointestinal symptoms such as severe diarrhea. TPH is the rate-limiting enzyme in serotonin biosynthesis, regulation. In in vitro studies, telotristat etiprate showed an antiproliferative activity against rat RBL-2H3 cells with an IC50 of approximately 0.4 μM. In animal models, oral administration of telotristat etiprate significantly reduced 5-HT levels in the intestine and blood, but had no significant effect on brain 5-HT levels. In addition, in a trinitrobenzenesulfonic acid (TNBS)-induced inflammatory bowel disease mouse model, oral administration of telotristat etiprate alleviated enteritis symptoms and reduced the expression of inflammation-related cytokines and chemokines. The dose or concentration used in experiments typically depends on the experimental design and research objectives.