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Catalog: | HY-13055 |
Brand: | MCE |
CAS: | 1137608-69-5 |
MDL | MFCD22741520 |
---|---|
Molecular Weight | 754.15 |
Molecular Formula | C36H35ClF3N7O6 |
SMILES | O=C([C@H](CC1=CC=C(C=C1)C2=CC(O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(C)=N4)C(F)(F)F)=NC(N)=N2)N)OCC.O=C(C5=CC=CC=C5)NCC(O)=O |
Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation [1] . Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT04034745 | Andrew Hendifar, MD|Lexicon Pharmaceuticals|Cedars-Sinai Medical Center |
Pancreatic Cancer|Neuroendocrine Tumors|Cachexia; Cancer
|
October 2020 | |
NCT03423446 | Lexicon Pharmaceuticals |
Hepatic Impairment
|
November 28, 2017 | Phase 1 |
NCT02063659 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
March 11, 2014 | Phase 3 |
NCT02155205 | Lexicon Pharmaceuticals |
QT Interval
|
May 2014 | Phase 1 |
NCT02157584 | Lexicon Pharmaceuticals |
Healthy
|
June 2014 | Phase 1 |
NCT03442725 | Ipsen |
Renal Impairment
|
February 9, 2018 | Phase 1 |
NCT01104415 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
June 15, 2010 | Phase 2 |
NCT00853047 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
March 2009 | Phase 2 |
NCT04672876 | University of Chicago |
Neuroendocrine Tumors
|
January 2022 | Phase 2 |
NCT04810091 | M.D. Anderson Cancer Center|TerSera Therapeutics LLC |
Locally Advanced Neuroendocrine Neoplasm|Metastatic Neuroendocrine Neoplasm
|
May 18, 2021 | Phase 3 |
NCT03790111 | TerSera Therapeutics LLC |
Biliary Tract Cancer
|
March 13, 2019 | Phase 2 |
NCT02157558 | Lexicon Pharmaceuticals |
Drug Interactions
|
July 2014 | Phase 1 |
NCT04713202 | Chandrikha Chandrasekhara|TerSera Therapeutics LLC|Big Ten Cancer Research Consortium |
Neuroendocrine Tumors|Carcinoid Syndrome|Diarrhea
|
March 3, 2021 | Phase 2 |
NCT04776876 | M.D. Anderson Cancer Center |
Advanced Neuroendocrine Neoplasm|Carcinoid Syndrome
|
March 1, 2021 | Phase 2 |
NCT02026063 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
January 14, 2014 | Phase 3 |
NCT01456052 | Lexicon Pharmaceuticals |
Ulcerative Colitis
|
January 30, 2012 | Phase 2 |
NCT04065165 | European Organisation for Research and Treatment of Cancer - EORTC|Ipsen |
Small Intestinal NET|Carcinoid Heart Disease
|
April 2020 | Phase 3 |
NCT03302845 | Lexicon Pharmaceuticals |
Drug-drug Interaction
|
September 21, 2017 | Phase 1 |
NCT03453489 | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) |
Carcinoid Syndrome|Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm
|
June 20, 2018 | Phase 2 |
NCT03910387 | Emory University|TerSera Therapeutics LLC |
Locally Advanced Unresectable Pancreatic Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Recurrent Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer AJCC v8|Stage IV Pancreatic Cancer AJCC v8
|
April 17, 2019 | Phase 2 |
NCT01677910 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
January 8, 2013 | Phase 3 |
NCT02195635 | Lexicon Pharmaceuticals |
Drug Interactions
|
July 2014 | Phase 1 |
NCT02147808 | Lexicon Pharmaceuticals |
Drug Interactions
|
May 2014 | Phase 1 |
NCT02683577 | Ipsen |
Hepatic Impairment
|
February 2016 | Phase 1 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 200 mg/mL ( 265.20 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.3260 mL | 6.6300 mL | 13.2600 mL |
5 mM | 0.2652 mL | 1.3260 mL | 2.6520 mL |
10 mM | 0.1326 mL | 0.6630 mL | 1.3260 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 10 mg/mL (13.26 mM); Clear solution
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