Chemical formula: C₂₇H₂₆ClF₃N₆O₃ Molecular mass: 546.94 g/mol
Both the prodrug (telotristat ethyl) and its active metabolite (telotristat) are inhibitors of L-tryptophan hydroxylases (TPH1 and TPH2, the rate limiting steps in serotonin biosynthesis). Serotonin plays a critical role in regulating several major physiological processes, including secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-secreted in patients with carcinoid syndrome. Through inhibition of peripheral TPH1, telotristat reduces the production of serotonin, thus alleviating symptoms associated with carcinoid syndrome.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
| ATC code | Group title | Classification |
|---|---|---|
| A16AX15 | A Alimentary tract and metabolism → A16 Other alimentary tract and metabolism products → A16A Other alimentary tract and metabolism products → A16AX Various alimentary tract and metabolism products | |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| XERMELO Film-coated tablet | European Medicines Agency (EU) | MPI, EU: SmPC |
Telotristat is an active ingredient of these brands:
United States (US)
Austria (AT)
Canada (CA)
Croatia (HR)
Estonia (EE)
Finland (FI)
France (FR)
Ireland (IE)
Israel (IL)
Italy (IT)
Lithuania (LT)
Netherlands (NL)
Poland (PL)
Romania (RO)
Spain (ES)
United Kingdom (UK)
Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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