Drug intelligence / Profile preview

telotristat ethyl

Development stage
Approved
Lead developer
Lexicon Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Telotristat ethyl is a small molecule prodrug of telotristat, developed for the treatment of carcinoid syndrome diarrhea in adults whose symptoms are inadequately controlled by somatostatin analog (SSA) therapy. It is marketed under the brand name Xermelo. Telotristat ethyl acts as an inhibitor of tryptophan hydroxylase, the rate-limiting enzyme in serotonin biosynthesis. By inhibiting this enzyme, it reduces peripheral serotonin production and thereby decreases the frequency and severity of diarrhea associated with carcinoid syndrome. The drug does not cross the blood–brain barrier and primarily targets peripheral serotonin synthesis[2][3][4][5][6][8].

Brand names
Xermelo
Other names
telotristattelotristat etiprate
02

Targets

TPH2 (Tryptophan hydroxylase 2)TPH1 (Tryptophan 5-hydroxylase 1)

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