Telotristat etiprateProduct ingredient for Telotristat ethyl

Telotristat ethyl is a prodrug of telotristat that was approved by the FDA in March 2017 as Xermelo.⁸ It was previously referred to as telotristat etiprate, the hippurate salt form; however, the FDA recommends the use of the name of the neutral form rather than that of the salt.^4,5 Currently, telotristat ethyl is used to treat carcinoid syndrome diarrhea from neuroendocrine tumors that are inadequately controlled by short-acting somatostatin analog (SSA) treatment.⁸

Neuroendocrine cells are cells that secrete regulatory peptides and biogenic amines in response to chemical, neural, or other types of stimuli.⁶ Neuroendocrine tumors (NET) arising from these cells can therefore secrete chemical mediators into the bloodstream to cause side effects in distant sites, a phenomenon called carcinoid syndrome.⁶ The most common peptides and amines secreted by NET are histamines, tachykinins, kallikrein, and serotonin.¹² Overexposure to serotonin can cause severe diarrhea, one of the main clinical symptoms of carcinoid syndrome.⁴ Serotonin is metabolized in the urinary metabolite 5-hydroxy indole acetic acid (u5-HIAA), and high levels of u5-HIAA is associated with poor survival outcome in patients with NET.⁴ The first line treatment of carcinoid syndrome diarrhea is SSA, but symptoms still reoccur over the course of the disease.⁴

ChemSpider

25027411

ChEMBL

CHEMBL3348963

Wikipedia

Telotristat_ethyl