Telotristat (Xermelo)
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, HemOnc.org 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
- Brief patient counseling information can be found in the Telotristat (Xermelo) package insert[1]
History of changes in FDA indication
- 2017-02-28: Initial FDA approval to be used in combination with somatostatin analog (SSA) therapy for the treatment of adults with carcinoid syndrome diarrhea that SSA therapy alone has inadequately controlled.
History of changes in EMA ndication
- 2017-09-17: Initial authorization
Also known as
- Generic name: telotristat ethyl as telotristat etiprate
- Brand name: Xermelo