telotristat ethyl + lanreotide

This combination therapy consists of **telotristat ethyl**, an oral tryptophan hydroxylase inhibitor, and **lanreotide**, a long-acting somatostatin analog. It is primarily being investigated in the Phase III TELEFIRST trial (sponsored by the European Organisation for Research and Treatment of Cancer - EORTC) for the first-line treatment of advanced well-differentiated small intestinal neuroendocrine tumours (siNET) associated with highly-functioning carcinoid syndrome. Telotristat ethyl reduces peripheral serotonin production by inhibiting tryptophan hydroxylase-1 (TPH1), the rate-limiting enzyme in serotonin biosynthesis. Lanreotide acts as an agonist at somatostatin receptors (primarily SSTR2 and SSTR5) to suppress the secretion of various hormones and peptides, including serotonin, thereby controlling symptoms like diarrhea and flushing.

Brand names

XermeloSomatuline

Other names

Telotristat etiprateTELEFIRST