Abstract
Telotristat ethyl (Xermelo™) is a peripheral tryptophan hydroxylase (TPH) inhibitor that was developed by Lexicon Pharmaceuticals, Inc. for the treatment of carcinoid syndrome. Many neuroendocrine tumours secrete serotonin (5-HT) into the blood stream, resulting in a number of symptoms, notably diarrhoea. Telotristat ethyl inhibits TPH, thereby reducing the production of 5-HT. In February 2017, telotristat ethyl was approved in the USA for the treatment of carcinoid syndrome diarrhoea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy. This article summarizes the milestones in the development of telotristat ethyl leading to this first global approval.
MeSH terms
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Animals
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Diarrhea / drug therapy*
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Drug Approval
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Drug Therapy, Combination
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Humans
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Malignant Carcinoid Syndrome / drug therapy*
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Neuroendocrine Tumors / complications
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Neuroendocrine Tumors / drug therapy*
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Phenylalanine / administration & dosage
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Phenylalanine / adverse effects
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Phenylalanine / analogs & derivatives*
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Phenylalanine / pharmacokinetics
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Pyrimidines / administration & dosage*
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Pyrimidines / adverse effects
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Pyrimidines / pharmacokinetics
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Randomized Controlled Trials as Topic
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Somatostatin / analogs & derivatives
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Tryptophan Hydroxylase / antagonists & inhibitors*
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United States
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United States Food and Drug Administration
Substances
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Pyrimidines
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telotristat
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Phenylalanine
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Somatostatin
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Tryptophan Hydroxylase