[CAS NO. 1033805-28-5] Telotristat

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PRODUCTS SPECIFICATIONS [1033805-28-5]

Catalog

HY-13055B

Brand

MCE

CAS

1033805-28-5

DESCRIPTION [1033805-28-5]

Overview

MDL	MFCD20528907
Molecular Weight	546.93
Molecular Formula	C25H22ClF3N6O3
SMILES	N[C@@H](CC1=CC=C(C2=NC(N)=NC(O[C@H](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1)C(O)=O

For research use only. We do not sell to patients.

Summary

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC ₅₀ of 0.028 μM.

IC50 & Target

IC50: 0.028 μM (tryptophan hydroxylase) ^[1]

In Vitro

Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03453489	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)	Carcinoid Syndrome\|Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm	June 20, 2018	Phase 2
NCT02147808	Lexicon Pharmaceuticals	Drug Interactions	May 2014	Phase 1
NCT01104415	Lexicon Pharmaceuticals	Carcinoid Syndrome	June 15, 2010	Phase 2
NCT02155205	Lexicon Pharmaceuticals	QT Interval	May 2014	Phase 1
NCT02063659	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 11, 2014	Phase 3
NCT04776876	M.D. Anderson Cancer Center	Advanced Neuroendocrine Neoplasm\|Carcinoid Syndrome	March 1, 2021	Phase 2
NCT04034745	Andrew Hendifar, MD\|Lexicon Pharmaceuticals\|Cedars-Sinai Medical Center	Pancreatic Cancer\|Neuroendocrine Tumors\|Cachexia; Cancer	October 2020
NCT03302845	Lexicon Pharmaceuticals	Drug-drug Interaction	September 21, 2017	Phase 1
NCT04065165	European Organisation for Research and Treatment of Cancer - EORTC\|Ipsen	Small Intestinal NET\|Carcinoid Heart Disease	April 2020	Phase 3
NCT02157584	Lexicon Pharmaceuticals	Healthy	June 2014	Phase 1
NCT02683577	Ipsen	Hepatic Impairment	February 2016	Phase 1
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
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
NCT02195635	Lexicon Pharmaceuticals	Drug Interactions	July 2014	Phase 1
NCT03442725	Ipsen	Renal Impairment	February 9, 2018	Phase 1
NCT02026063	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 14, 2014	Phase 3
NCT03423446	Lexicon Pharmaceuticals	Hepatic Impairment	November 28, 2017	Phase 1
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
NCT03790111	TerSera Therapeutics LLC	Biliary Tract Cancer	March 13, 2019	Phase 2
NCT04543955	Aman Chauhan\|TerSera Therapeutics LLC\|University of Kentucky	Neuroendocrine Tumors	July 19, 2021	Phase 2
NCT01677910	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 8, 2013	Phase 3
NCT01456052	Lexicon Pharmaceuticals	Ulcerative Colitis	January 30, 2012	Phase 2
NCT00853047	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL ( 60.94 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8284 mL	9.1419 mL	18.2839 mL
5 mM	0.3657 mL	1.8284 mL	3.6568 mL
10 mM	0.1828 mL	0.9142 mL	1.8284 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

* All of the co-solvents are available by MCE.