tcsc2408 Telotristat

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

IC50 & Target: IC50: 0.028 μM (tryptophan hydroxylase)^[1]

In Vitro: Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome^[1].

In Vivo: Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional^[1].