telotristat; telotristat ethyl (Xermelo)
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Indications
- carcinoid syndrome diarrhea in combination with somatostatin analog
Dosage
Tablets: 250 mg
Pharmacokinetics
- telotristat ethyl (marketed form) is a precursor to telotristat
- protein-binding 99% (both telotristat ethyl & telotristat)
- hydrolysis via carboxylesterases
- 1/2 life 0.6 hours telotristat ethyl, 5 hours telotristat
- 93% excreted into the feces[3]
Adverse effects
- nausea, constipation, anorexia
- increased serum transaminases, edema
- fever
- headache
Mechanism of action
- inhibits tryptophan hydroxylase
More general terms
References
- ↑ RxNorm
- ↑ Radke J FDA Approves Xermelo (telotristat ethyl) for Carcinoid Syndrome. Rare Disease Report, Feb 28, 2017 http://www.raredr.com/news/fda-approves-xermelo
Windle ML. FDA New Drug and Biologic Approvals -- 2017 Year-in-Review Medscape - Jan 11, 2018. https://reference.medscape.com/viewarticle/890871
U.S. Food and Drug Administration. Novel Drug Approvals for 2017. https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DrugInnovation/ucm537040.htm - ↑ 3.0 3.1 Wikipedia: Telotristat ethyl https://en.wikipedia.org/wiki/Telotristat_ethyl
- ↑ Kulke MH, Horsch D, Caplin ME et al Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome. J Clin Oncol. 2017 Jan;35(1):14-23. Epub 2016 Oct 28. PMID: https://www.ncbi.nlm.nih.gov/pubmed/27918724
- ↑ 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 Oct;21(5):705-14. Epub 2014 Jul 10. PMID: https://www.ncbi.nlm.nih.gov/pubmed/25012985 Free PMC Article