NCIt definition : A tryptophan hydroxylase (TPH) inhibitor, with potential anti-serotonergic activity.
Upon administration, telotristat binds to and inhibits the activity of TPH. This may
result in a reduction in peripheral serotonin (5-HT) production and improvement of
serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting
enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.;