Literature DB >> 28382568

Telotristat Ethyl: First Global Approval.

Anthony Markham1.   

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.

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Year:  2017        PMID： 28382568     DOI： 10.1007/s40265-017-0737-x

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   9.546


  4 in total

1.  Telotristat etiprate for carcinoid syndrome: a single-arm, multicenter trial.

Authors:  Marianne Pavel; Dieter Hörsch; Martyn Caplin; John Ramage; Thomas Seufferlein; Juan Valle; Phillip Banks; Pablo Lapuerta; Arthur Sands; Brian Zambrowicz; Douglas Fleming; Bertram Wiedenmann
Journal:  J Clin Endocrinol Metab       Date:  2015-01-30       Impact factor: 5.958

2.  Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical- and infection-induced intestinal inflammation.

Authors:  Janice J Kim; Huaqing Wang; Joshua D Terc; Brian Zambrowicz; Qi M Yang; Waliul I Khan
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2015-07-23       Impact factor: 4.052

3.  Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome.

Authors:  Matthew H Kulke; Dieter Hörsch; Martyn E Caplin; Lowell B Anthony; Emily Bergsland; Kjell Öberg; Staffan Welin; Richard R P Warner; Catherine Lombard-Bohas; Pamela L Kunz; Enrique Grande; Juan W Valle; Douglas Fleming; Pablo Lapuerta; Phillip Banks; Shanna Jackson; Brian Zambrowicz; Arthur T Sands; Marianne Pavel
Journal:  J Clin Oncol       Date:  2016-10-28       Impact factor: 44.544

4.  Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide.

Authors:  Matthew H Kulke; Thomas O'Dorisio; Alexandria Phan; Emily Bergsland; Linda Law; Phillip Banks; Joel Freiman; Kenny Frazier; Jessica Jackson; James C Yao; Larry Kvols; Pablo Lapuerta; Brian Zambrowicz; Douglas Fleming; Arthur Sands
Journal:  Endocr Relat Cancer       Date:  2014-07-10       Impact factor: 5.678
  4 in total
  11 in total

Review 1.  Carcinoid-syndrome: recent advances, current status and controversies.

Authors:  Tetsuhide Ito; Lingaku Lee; Robert T Jensen
Journal:  Curr Opin Endocrinol Diabetes Obes       Date:  2018-02       Impact factor: 3.243

Review 2.  Supportive therapy in gastroenteropancreatic neuroendocrine tumors: Often forgotten but important.

Authors:  Xi-Feng Jin; Matilde P Spampatti; Christine Spitzweg; Christoph J Auernhammer
Journal:  Rev Endocr Metab Disord       Date:  2018-06       Impact factor: 6.514

3.  Fluorine-18-Labeled PET Radiotracers for Imaging Tryptophan Uptake and Metabolism: a Systematic Review.

Authors:  Flóra John; Otto Muzik; Sandeep Mittal; Csaba Juhász
Journal:  Mol Imaging Biol       Date:  2020-08       Impact factor: 3.488

Review 4.  Emerging Roles for Serotonin in Regulating Metabolism: New Implications for an Ancient Molecule.

Authors:  Julian M Yabut; Justin D Crane; Alexander E Green; Damien J Keating; Waliul I Khan; Gregory R Steinberg
Journal:  Endocr Rev       Date:  2019-08-01       Impact factor: 19.871

5.  Identification of New Non-BBB Permeable Tryptophan Hydroxylase Inhibitors for Treating Obesity and Fatty Liver Disease.

Authors:  Suvarna H Pagire; Haushabhau S Pagire; Kun-Young Park; Eun Jung Bae; Kwang-Eun Kim; Minhee Kim; Jihyeon Yoon; Saravanan Parameswaran; Jun-Ho Choi; Sungmi Park; Jae-Han Jeon; Jin Sook Song; Myung Ae Bae; In-Kyu Lee; Hail Kim; Jae Myoung Suh; Jin Hee Ahn
Journal:  Molecules       Date:  2022-05-25       Impact factor: 4.927

6.  Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone.

Authors:  Samantha R Weaver; Hannah P Fricke; Cynthia Xie; Robert J Aiello; Julia F Charles; Laura L Hernandez
Journal:  Am J Physiol Endocrinol Metab       Date:  2018-10-23       Impact factor: 4.310

Review 7.  Practical management of toxicities associated with targeted therapies for advanced gastroenteropancreatic neuroendocrine tumors.

Authors:  Pieter-Jan Cuyle; Hans Prenen
Journal:  Ann Gastroenterol       Date:  2018-01-08

8.  Inhibition of Tryptophan Hydroxylases and Monoamine Oxidase-A by the Proton Pump Inhibitor, Omeprazole-In Vitro and In Vivo Investigations.

Authors:  Nibal Betari; Kristoffer Sahlholm; Xavier Morató; Héctor Godoy-Marín; Olga Jáuregui; Knut Teigen; Francisco Ciruela; Jan Haavik
Journal:  Front Pharmacol       Date:  2020-11-26       Impact factor: 5.810

Review 9.  Spotlight on telotristat ethyl for the treatment of carcinoid syndrome diarrhea: patient selection and reported outcomes.

Authors:  Cristina Saavedra; Jorge Barriuso; Mairéad G McNamara; Juan W Valle; Angela Lamarca
Journal:  Cancer Manag Res       Date:  2019-08-08       Impact factor: 3.989

Review 10.  One Key and Multiple Locks: Substrate Binding in Structures of Tryptophan Dioxygenases and Hydroxylases.

Authors:  Andrea Mammoli; Alessandra Riccio; Elisa Bianconi; Alice Coletti; Emidio Camaioni; Antonio Macchiarulo
Journal:  ChemMedChem       Date:  2021-07-16       Impact factor: 3.466
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