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Telotristat

Telotristat structure

CAS No:
1033805-28-5
Formula:
C25H22ClF3N6O3
Chemical Name:
Telotristat
Synonyms:
LP778902; (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)-phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid; (S)-2-amino-3-[4-(2-amino-6-{(R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy}pyrimidine-4-yl)phenyl]propionic acid; (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid; (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid;
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Telotristat is a phenylalanine derivative.|A tryptophan hydroxylase inhibitor. [Telotristat ethyl] (brand name Xermelo) is a prodrug of telotristat.|Telotristat is a Tryptophan Hydroxylase Inhibitor. The mechanism of action of telotristat is as a Tryptophan Hydroxylase Inhibitor.|Telotristat is an oral, small molecule inhibitor of tryptophan hydroxylase that is used in the treatment of symptoms of carcinoid syndrome. Telotristat is associated with modest rate of minor serum enzyme elevations during therapy but has not been linked to cases of clinically apparent liver injury.

Telotristat Basic Attributes

Molecular Weight：

546.92900

Exact Mass：

546.1394008

UNII：

381V4FCV2Z

DSSTox ID：

DTXSID60145805

ATC Code：

A - Alimentary tract and metabolism

Characteristics

PSA：

142.17000

XLogP3：

5.79160

Density：

1.50±0.1g/cm3

Water Solubility：

Sparingly Soluble (1.5E-3 g/L) (25 ºC), Calc.

Toxicity

Hepatotoxicity：

In small clinical trials of telotristat in patients with neuroendocrine tumors and symptomatic diarrhea despite stable doses of somatostatin analogues, transient, asymptomatic and mild serum elevations of ALT occurred in 4% to 5% and of GGT in 6% to 9% of treated subjects. Apparent liver injury with jaundice was not observed in the several prelicensure clinical trials and has not been reported in the limited clinical experience with this agent since its approval.

Drug Information

LiverTox Summary：

Telotristat is an oral, small molecule inhibitor of tryptophan hydroxylase that is used in the treatment of symptoms of carcinoid syndrome. Telotristat is associated with modest rate of minor serum enzyme elevations during therapy but has not been linked to cases of clinically apparent liver injury.

Drug Classes：

Antineoplastic Agents

MeSH Entry Terms：

LX1032

Computed Properties

Molecular Weight:546.9
XLogP3:2.1
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:11
Rotatable Bond Count:8
Exact Mass:546.1394008
Monoisotopic Mass:546.1394008
Topological Polar Surface Area:142
Heavy Atom Count:38
Complexity:790
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Telotristat 99% see COA Kanbei kanbei

CAS No.: 1033805-28-5

Grade: Industrial Grade

Content: 99%

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