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Telotristat ethyl (Xermelo) is a tablet that cuts the serotonin that neuroendocrine tumours pour out, easing the constant diarrhoea of carcinoid syndrome when somatostatin analogue injections are not enough.
Telotristat ethyl was approved by the FDA in February 2017 and authorised in the EU in September 2017 for carcinoid syndrome diarrhoea in combination with somatostatin analogue therapy in adults inadequately controlled by that therapy, on the TELESTAR phase 3 trial (135 patients) in which the 250 mg three-times-daily dose reduced daily bowel movements more than placebo, a statistically significant difference, and lowered urinary 5-HIAA. It is the first oral drug for carcinoid syndrome and the first tryptophan hydroxylase inhibitor approved for any indication. Nausea, headache, raised liver enzymes, depression and constipation are the main adverse effects. Marketed by TerSera in the US and SERB in Europe.
Prodrug of telotristat, which inhibits tryptophan hydroxylase, the rate-limiting enzyme of peripheral serotonin synthesis in neuroendocrine tumour cells, lowering urinary 5-HIAA and bowel frequency without crossing into the brain.
1.Telotristat ethyl slips into a pocket on its target.
Compare all products across the US, EU, UK, Japan, China and Australia →
| Region | Year | Indication |
|---|---|---|
| US | 2017 | Carcinoid syndrome diarrhoea with somatostatin analogue therapy in adults inadequately controlled by SSA alone |
| EU | 2017 | Same (Xermelo) |
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Query for this drug: (TITLE:"Telotristat ethyl" OR ABSTRACT:"Telotristat ethyl" OR TITLE:"Xermelo" OR ABSTRACT:"Xermelo" OR TITLE:"LX1032" OR ABSTRACT:"LX1032" OR TITLE:"Telotristat etiprate" OR ABSTRACT:"Telotristat etiprate") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Telotristat ethyl, not a curated reading list.
Shares SERB Pharmaceuticals and the tag supportive.
Shares SERB Pharmaceuticals and the tag supportive.
Shares TerSera Therapeutics and the tag supportive.
Shares Tryptophan hydroxylase 1, Somatostatin analogues (octreotide, lanreotide), Small intestinal neuroendocrine tumours, Neuroendocrine tumours.
Shares Somatostatin analogues (octreotide, lanreotide), Small intestinal neuroendocrine tumours, Neuroendocrine tumours.
Shares Somatostatin analogues (octreotide, lanreotide), Small intestinal neuroendocrine tumours, Neuroendocrine tumours.
Shares Somatostatin analogues (octreotide, lanreotide), Small intestinal neuroendocrine tumours, Neuroendocrine tumours.
Shares Somatostatin analogues (octreotide, lanreotide), Neuroendocrine tumours.