Telotristat ethyl is a tryptophan hydroxylase inhibitor that is used to treat carcinoid syndrome diarrhea. Telotristat ethyl is a prodrug of telotristat that was approved by the FDA in March 2017 as Xermelo.
- Mechanism
- Curator reviewed · 1 reference
Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate-limiting step in serotonin biosynthesis. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea.
- Primary indication
- Xermelo is indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.Curator reviewed · 1 structured indication
- Formula / weight
- C27H26ClF3N6O3 · 574.99 g/mol (avg)
- First approval
- Canada, 2023 · United States, 2017 · European Union, 2020
- Code names
- LX-1032 · LX-1606
- Brand names
Resolves to
MDSQOJYHHZBZKA-GBXCKJPGSA-NSMILESCCOC(=O)[C@@H](N)CC1=CC=C(C=C1)C1=NC(N)=NC(O[C@H](C2=CC=C(Cl)C=C2N2C=CC(C)=N2)C(F)(F)F)=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Telotristat ethyl, and which of those have an active Phase 3 trial?
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