Telotristat (Xermelo)

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General information

Class/mechanism: Tryptophan hydroxylase inhibitor. Tryptophan hydroxylase controls the rate limiting step of the biosynthesis of serotonin, which plays a role in regulating the secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Telotristat reduces the frequency of carcinoid syndrome diarrhea by decreasing the production of serotonin.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Patient drug information

History of changes in FDA indication

History of changes in EMA ndication

  • 2017-09-17: Initial authorization

Also known as

  • Generic name: telotristat ethyl as telotristat etiprate
  • Brand name: Xermelo