Products
Telotristat was approved in the United States in 2017 and in many countries in 2018 in film-coated tablet form (Xermelo).
Structure and properties
Telotristat (C27H26ClF3N6O3, Mr = 574.9 g/mol) is present in the drug as a salt of hippuric acid and as an ethyl ester prodrug. After absorption, the prodrug is rapidly hydrolyzed by carboxylesterases to the active drug telotristat.
Effects
Telotristat inhibits the biosynthesis of peripheral serotonin in the intestine by inhibiting tryptophan hydroxylase. Serotonin is formed from the amino acid tryptophan. In patients with carcinoid syndrome, it is overproduced and plays an important role in disease development. Telotristat does not cross the blood–brain barrier into the central nervous system and therefore does not inhibit the synthesis of the neurotransmitter serotonin. It has a half-life of approximately 6 hours.
Indications
For the treatment of diarrhea associated with carcinoid syndrome in combination with a somatostatin analog.
Dosage
According to the SmPC. Film-coated tablets are taken three times daily with a meal.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects include nausea, headache, elevation of GGT, depression, flatulence, decreased appetite, peripheral edema, and fever.
