General
Preferred name
TELOTRISTAT ETHYL
Synonyms
LX1606 (Hippurate) ()
LX 1606 Hippurate ()
LX1606 ()
TELOTRISTAT ETIPRATE ()
LX1606 (Hippurate)LX 1606 Hippurate ()
LX 1606 ()
LX1032 ()
Telotristat Etiprate (LX 1606 Hippurate) ()
LX1606 hippurate ()
LX1032 HIPPURATE ()
Telotristat ethyl hippurate ()
Xermelo ()
LX-1032 ()
LX-1606 ()
LX 1032 ()
P&D ID
PD056960
CAS
1137608-69-5
1033805-22-9
Tags
available
prodrug
drug
Approved by
EMA
FDA
First approval
2017
Drug Status
investigational
approved
Drug indication
Carcinoid syndrome
Carcinoid syndrome diarrhea
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Telotristat ethyl is an oral tryptophan hydroxylase inhibitor. Telotristat ethyl is the USAN, the INN is telotristat (represented in PubChem CID 25025298. (GtoPdb)
PHARMACODYNAMICS Activity is mainly in the gastrointestinal tract, with minimal effects reported on the brain and cardiovascular system, accompanied by an excellent safety profile.; In normal mice, telotristat etiprate (administered once daily for 4 days at doses of 15–300 mg/kg/day) was found to reduce serotonin levels throughout the gastrointestinal tract. These reductions occurred in a dose dependent fashion with maximal effects observed with doses of telotristat etiprate ≥150 mg/kg. No significant change in brain serotonin or 5-hydroxyindoleacetic acid (5-HIAA, a serotonin metabolite) was observed. Similar findings were seen in Sprague-Dawley rats. Gastrointestinal motility studies were conducted in rats using the charcoal meal test. There was a significant dose-related delay in both gastrointestinal transit and gastric emptying, associated with a reduction in blood serotonin levels and proximal colon serotonin.; A quantitative whole-body autoradiography study was conducted to assess the absorption, distribution and excretion of radioactivity in rats following a single oral dose of telotristat etiprate labeled with carbon 14. Rats were administered either 30 mg/kg or 100 mg/kg of the compound. The distribution of radioactivity was limited to tissues of the hepatic and renal system and the contents of the GI tract. There was no measurable radioactivity in the brain at any dose tested.
Compound Sets
20
AdooQ Bioactive Compound Library
A10542
A11785
Cayman Chemical Bioactives
25342
ChEMBL Approved Drugs
CHEMBL3348963
CHEMBL2105695
ChEMBL Drugs
CHEMBL3348963
CHEMBL2105695
Concise Guide to Pharmacology 2017/18
9490
Concise Guide to Pharmacology 2019/20
9490
Concise Guide to Pharmacology 2021/22
9490
Concise Guide to Pharmacology 2023/24
9490
Drug Repurposing Hub
DrugBank
DB12095
DrugBank Approved Drugs
DB12095
DrugCentral
5214
DrugCentral Approved Drugs
5214
DrugMAP
DMDIYFZ
DrugMAP Approved Drugs
DMDIYFZ
Guide to Pharmacology
9490
MedChem Express Bioactive Compound Library
HY-13055
HY-13055A
ReFrame library
Selleckchem Bioactive Compound Library
telotristat-etiprate-lx-1606-hippurate
TargetMol Bioactive Compound Library
T6044
T11897
External IDs
48
Properties
(calculated by RDKit )
Molecular Weight
574.17
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
2
Rotatable Bonds
9
Ring Count
4
Aromatic Ring Count
4
cLogP
4.99
TPSA
131.17
Fraction CSP3
0.26
Chiral centers
2.0
Largest ring
6.0
QED
0.27
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Metabolism
Metabolic Enzyme/Protease
Target
Tryptophan hydroxylase
TPH1
hydroxylase
Indication
diarrhea
MOA
tryptophan hydroxylase inhibitor
Source data