Telotristat ethyl (USAN, brand name Xermelo) is a prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase. It is formulated as telotristat etiprate — a hippurate salt of telotristat ethyl.[3]
On February 28, 2017, the U.S. Food and Drug Administration (FDA) approved telotristat ethyl in combination with somatostatin analog (SSA) therapy for the treatment of adults with diarrhea associated with carcinoid syndrome that SSA therapy alone has inadequately controlled.[5][6] Telotristat ethyl was approved for use in the European Union in September 2017.[4]
The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[7]
^"Summary Basis of Decision (SBD) for Xermelo". Health Canada. 23 October 2014. Retrieved 29 May 2022.
^"Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
^ abc"Xermelo- telotristat ethyl tablet". DailyMed. 30 October 2020. Retrieved 11 November 2020.
^ ab"Xermelo EPAR". European Medicines Agency (EMA). Retrieved 17 April 2020.
^"FDA Approves Xermelo for Carcinoid Syndrome Diarrhea" (Press release). U.S. Food and Drug Administration (FDA). February 28, 2017. Retrieved 1 March 2017.
^"Xermelo (telotristat ethyl) Tablets". U.S. Food and Drug Administration (FDA). 4 April 2017. Retrieved 17 April 2020.
^New Drug Therapy Approvals 2017 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2018. Retrieved 16 September 2020.
Telotristatethyl (USAN, brand name Xermelo) is a prodrug of telotristat, which is an inhibitor of tryptophan hydroxylase. It is formulated as telotristat...
refractory, mTOR inhibitors such as everolimus. The TPH inhibitor telotristatethyl may be useful in controlling diarrhea associated with the carcinoid...
of irritable bowel syndrome and other gastrointestinal disorders; telotristatethyl (LX1032) for the treatment of the symptoms associated with carcinoid...
condition. His research studies led to the development and approval of telotristatethyl, a tryptophan hydroxylase inhibitor, for the treatment of patients...
at elevated temperatures, while another uses acyloin condensation of the ethyl ester of pimelic acid the acyloin again followed by oxidation by bromine...
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