telotristat etiprate

Telotristat etiprate is an orally bioavailable, small-molecule inhibitor of tryptophan hydroxylase (TPH), the rate-limiting enzyme in serotonin biosynthesis. Developed by Lexicon Pharmaceuticals, it is specifically designed to reduce peripheral serotonin production in patients with carcinoid syndrome, particularly those whose diarrhea is inadequately controlled by somatostatin analogs (SSAs). By targeting TPH, the drug addresses the underlying cause of carcinoid syndrome symptoms without crossing the blood-brain barrier, thus avoiding interference with central nervous system serotonin levels. It was approved by the FDA in 2017 under the brand name Xermelo for use in combination with SSA therapy.

Brand names

Xermelo

Other names

telotristat ethyltelotristat