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Version: 17.06d (Release date: 2017-06-26)
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Telotristat Etiprate (Code C81941)

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Terms & Properties

Preferred Name: Telotristat Etiprate

Definition: An orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor prodrug, with potential antiserotonergic activity. Upon administration, telotristat etiprate is converted to its active moiety, telotristat (LP-778902), which binds to and blocks the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.

Display Name: Telotristat Etiprate

Label: Telotristat Etiprate

NCI Thesaurus Code: C81941 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3853880  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Ethyl 4-(2-amino-6-((1r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pryrimidin-4-yl)-l-phenylalaninate N-benzoylglycinate (1:1)
LX1032 Hippurate
LX1606 Hippurate
Telotristat Etiprate
TPH Inhibitor LX1606
Tryptophan Hydroxylase Inhibitor LX1032
Tryptophan Hydroxylase Inhibitor LX1606

External Source Codes: 
CAS Registry Number 1137608-69-5 (see NLM ChemIDplus info)
FDA UNII Code 3T25U84H4U
PDQ Closed Trial Search ID 639514
PDQ Closed Trial Search ID 662188
PDQ Open Trial Search ID 639514 (check for NCI PDQ open clinical trial info)
PDQ Open Trial Search ID 662188 (check for NCI PDQ open clinical trial info)
UMLS CUI C3853880

Other Properties:
     Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For Carcinoid Syndrome, Ulcerative Colitis
Chemical_Formula C27H26ClF3N6O3.C9H9NO3
code C81941
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name TPH_Inhibitor_LX1032
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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