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Compound

Telotristat ethyl

Also called Xermelo

Original Wikipedia articleen.wikipedia.org/wiki/Telotristat_ethyl revision used (24 October 2026)

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Part of the metabolic pathway of Telotristat ethyl. See the timeline on the metabolic highway.

Enzymes that break it down: carboxylesterases. Wikipedia’s drug infobox says: “Hydrolysis via carboxylesterases” (revision 1292972573).

Overview

Telotristat ethyl (USAN, brand name Xermelo) is a prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase. It is formulated as telotristat etiprate — a hippurate salt of telotristat ethyl.[1] WP

On February 28, 2017, the U.S. Food and Drug Administration (FDA) approved telotristat ethyl in combination with somatostatin analog (SSA) therapy for the treatment of adults with diarrhea associated with carcinoid syndrome that SSA therapy alone has inadequately controlled. Telotristat ethyl was approved for use in the European Union in September 2017.[2][3][4] WP

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[5] WP

Risks and side effects

Adverse effects

Common adverse effects noted in clinical trials include nausea, headache, elevated liver enzymes, depression, accumulation of fluid causing swelling (peripheral edema), flatulence, decreased appetite, and fever. Constipation is also common, and may be serious or life-threatening (especially in overdose).[2] WP

Pharmacology

Pharmacology

Telotristat is an inhibitor of tryptophan hydroxylase, which mediates the rate-limiting step in serotonin biosynthesis.[1][6] WP

Chemistry

Formula
C27H26ClF3N6O3 PC
CAS number
1033805-22-9 PC
Molar mass (g/mol)
575.0 PC
IUPAC name (computed by PubChem)
ethyl (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate PC
SMILES
CCOC(=O)[C@H](CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N PC
InChIKey
MDSQOJYHHZBZKA-GBXCKJPGSA-N PC
PubChem CID
25181577

Harm reduction information

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Sources

  1. Journal / agency Xermelo- telotristat ethyl tablet. 30 October 2020
  2. Journal / agency FDA Approves Xermelo for Carcinoid Syndrome Diarrhea. February 28, 2017
  3. Journal / agency Xermelo (telotristat ethyl) Tablets. 4 April 2017
  4. Journal / agency Xermelo EPAR. 20 October 2017
  5. Journal / agency New Drug Therapy Approvals 2017. January 2018
  6. Journal / agency Kulke M, Hörsch D, Caplin M, Anthony L, Bergsland E, Oberg K, Welin S, Warner R, Bohas CL, Kunz PL, Grande E. Integrated Placebo-Controlled Safety Analysis from Clinical Studies of Telotristat Ethyl for the Treatment of Carcinoid Syndrome. Annals of Oncology. 1 October 2016. doi:10.1093/annonc/mdw369.07

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.