Telotristat etiprate
- telotristat etiprate An orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor prodrug, with potential antiserotonergic activity.
Mechanism of action of Telotristat etiprate[edit source]
Upon administration, telotristat etiprate is converted to its active moiety, telotristat (LP-778902), which binds to and blocks 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.
Clinical Trials Using Telotristat etiprate[edit source]
Check for ACTIVE CLINICAL TRIALS
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Contributors: Prab R. Tumpati, MD