Synonyms: LX-1606 | LX1606 | Xermelo®
telotristat ethyl is an approved drug (FDA (2017))
Compound class:
Synthetic organic
Comment: Telotristat ethyl is an oral tryptophan hydroxylase inhibitor. Telotristat ethyl is the USAN, the INN is telotristat (represented in PubChem CID 25025298.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bae EJ, Choi WG, Pagire HS, Pagire SH, Parameswaran S, Choi JH, Yoon J, Choi WI, Lee JH, Song JS et al.. (2021)
Peripheral Selective Oxadiazolylphenyl Alanine Derivatives as Tryptophan Hydroxylase 1 Inhibitors for Obesity and Fatty Liver Disease. J Med Chem, 64 (2): 1037-1053. [PMID:33417443] |
2. Kim JJ, Wang H, Terc JD, Zambrowicz B, Yang QM, Khan WI. (2015)
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, 309 (6): G455-65. [PMID:26206858] |
3. Kulke MH, Hörsch D, Caplin ME, Anthony LB, Bergsland E, Öberg K, Welin S, Warner RR, Lombard-Bohas C, Kunz PL et al.. (2017)
Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome. J Clin Oncol, 35 (1): 14-23. [PMID:27918724] |
4. Lamarca A, Barriuso J, McNamara MG, Hubner RA, Valle JW. (2016)
Telotristat ethyl: a new option for the management of carcinoid syndrome. Expert Opin Pharmacother, 17 (18): 2487-2498. [PMID:27817224] |
5. Margolis KG, Stevanovic K, Li Z, Yang QM, Oravecz T, Zambrowicz B, Jhaver KG, Diacou A, Gershon MD. (2014)
Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 63 (6): 928-37. [PMID:23749550] |