Telotristat ethyl

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Telotristat ethyl
Telotristat ethyl.svg
Clinical data
Trade namesXermelo
SynonymsLX1032, LX1606
AHFS/Drugs.comMultum Consumer Information
Routes of
By mouth (tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding>99% (both telotristat ethyl and telotristat)
MetabolismHydrolysis via carboxylesterases
Elimination half-life0.6 hours (telotristat ethyl), 5 hours (telotristat)
ExcretionFeces (92.8%), urine (less than 0.4%)[1]
CAS Number
PubChem CID
Chemical and physical data
Molar mass838.8696 g/mol g·mol−1
3D model (JSmol)

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]

On February 28, 2017, the U.S. Food and Drug Administration approved Xermelo 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.[2]


Telotristat is an inhibitor of tryptophan hydroxylase,[3] which mediates the rate-limiting step in serotonin biosynthesis.[1]

Action of telotristat on tryptophan hydroxylase

Adverse effects[edit]

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).[4]


It is marketed by Lexicon Pharmaceuticals (as telotristat etiprate). 328 mg telotristat etiprate is equivalent to 250 mg telotristate ethyl.[1]

Telotristat etiprate


  1. ^ a b c d "Xermelo (telotristat ethyl) Tablets, for Oral Use. Full Prescribing Information" (PDF). Lexicon Pharmaceuticals, Inc. 8800 Technology Forest Place. The Woodlands, TX 77381. Retrieved 1 March 2017.
  2. ^ "FDA Approves Xermelo for Carcinoid Syndrome Diarrhea". U.S. Food and Drug Administration. February 28, 2017. Retrieved 1 March 2017.
  3. ^ Kulke, M; Hörsch, D; Caplin, M; Anthony, L; Bergsland, E; Oberg, K; Welin, S; Warner, R; Bohas, CL; Kunz, PL; Grande, E; Valle, JW; Lapuerta, P; Banks, P; Jackson, S; Jiang, W; Biran, T; Pavel, M (1 October 2016). "Integrated Placebo-Controlled Safety Analysis from Clinical Studies of Telotristat Ethyl for the Treatment of Carcinoid Syndrome". Annals of Oncology. 27 (6): 136–48. doi:10.1093/annonc/mdw369.07.
  4. ^ "FDA approves Xermelo for carcinoid syndrome diarrhea". FDA. Retrieved 15 March 2017.

External links and further reading[edit]