Skip to main content
Log in

Telotristat Ethyl: First Global Approval

  • AdisInsight Report
  • Published:
Drugs Aims and scope Submit manuscript

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Lexicon Pharmaceuticals. XERMELO (telotristat ethyl): US prescribing information. 2017. http://xermelo.com/Media/Default/pdfs/Product_Info_telotristat_etiprate.pdf. Accessed 2 Mar 2017.

  2. Lexicon P. Lexicon and Ipsen enter into ex-North America/Japan licensing and commercialization agreement for telotristat etiprate [media release]. 22 Oct 2014. http://www.lexpharma.com.

  3. Lexicon P, Ipsen. Lexicon and Ipsen expand their licensing and commercialization agreement for telotristat etiprate to include Canada [media release]. 18 Mar 2015. http://www.lexpharma.com.

  4. Lexicon Pharmaceuticals I. Lexicon Pharmaceuticals announces two agreements to finance long-term drug development strategy [media release]. 17 June 2007. http://www.lexpharma.com.

  5. Lexicon Pharmaceuticals I. Lexicon Pharmaceuticals announces reacquisition of all rights to Symphony Icon programs [media release]. 02 Aug 2010. http://www.lexpharma.com.

  6. Lexicon Pharmaceuticals. Lexicon Pharmaceuticals announces agreement to buy out remaining obligations to Symphony Icon [media release]. 05 Oct 2016. http://www.lexpharma.com.

  7. Kim JJ, Wang H, Terc JD, et al. Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical- and infection-induced intestinal inflammation. Am J Physiol Gastrointest Liver Physiol. 2015;309(6):G455–65.

    Article  CAS  PubMed  Google Scholar 

  8. Oravecz T, Jhaver K, Yang QM, et al. LX1606 (Aka LX1032), a peripheral inhibitor of serotonin synthesis, alleviates development of inflammatory bowel disease in a preclinical model [abstract no. Mo2021]. Gastroenterology. 2012;142(5 Supplement 1):S722.

  9. Pappas SC, Brown P, Turnage A, et al. LX1032: a potential new therapy for chronic diarrhea in carcinoid syndrome (CS) [abstract no. 352]. Gastroenterology. 2009;136(5 Supplement 1):A56.

  10. Kulke MH, Horsch D, Caplin ME, et al. Telotristat ethyl, a tryptophan hydroxylase inhibitor for the treatment of carcinoid syndrome. J Clin Oncol. 2017;35(1):14–23.

    Article  PubMed  Google Scholar 

  11. Pavel M, Gross D, Benavent M, et al. Efficacy and safety results of telotristat ethyl in patients with carcinoid syndrome during the double-blind treatment period of the TELECAST phase 3 clinical trial. In: North American Neuroendocrine Tumor Society Meeting. 2016.

  12. Pavel M, Benavent M, Perros P, et al. Telotristat ethyl in carcinoid syndrome: safety and efficacy results of an open-label extension of the TELECAST phase 3 clinical trial [abstract no. 1942 plus poster]. In: European Neuroendocrine Tumor Society (ENETS) Conference. 2017.

  13. Kulke MH, O’Dorisio T, Phan A, et al. Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide. Endocr Relat Cancer. 2014;21(5):705–14.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  14. Pavel M, Horsch D, Caplin M, et al. Telotristat etiprate for carcinoid syndrome: a single-arm, multicenter trial. J Clin Endocrinol Metab. 2015;100(4):1511–9.

    Article  CAS  PubMed  Google Scholar 

  15. Kulke M, Horsch D, Caplin M, et al. Integrated placebo-controlled safety analysis from clinical studies of telotristat ethyl for the treatment of carcinoid syndrome [abstract no. 422PD]. Ann Oncol. 2016;27(Suppl 6):vi136–vi48.

Download references

Disclosure

The preparation of this review was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. A. Markham is a contracted employee of Adis, Springer SBM.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Anthony Markham.

Additional information

This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Markham, A. Telotristat Ethyl: First Global Approval. Drugs 77, 793–798 (2017). https://doi.org/10.1007/s40265-017-0737-x

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-017-0737-x

Keywords

Navigation