ALEGLITAZAR

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H23NO5S
Molecular Weight	437.508
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CO[C@@H](CC1=C2SC=CC2=C(OCCC3=C(C)OC(=N3)C4=CC=CC=C4)C=C1)C(O)=O

InChI

InChIKey=DAYKLWSKQJBGCS-NRFANRHFSA-N

InChI=1S/C24H23NO5S/c1-15-19(25-23(30-15)16-6-4-3-5-7-16)10-12-29-20-9-8-17(14-21(28-2)24(26)27)22-18(20)11-13-31-22/h3-9,11,13,21H,10,12,14H2,1-2H3,(H,26,27)/t21-/m0/s1

HIDE SMILES / InChI

Description

Aleglitazar is a dual agonist of PPARalpha/PPARgamma which was developed by Hoffmann-La Roche for the treatment of type 2 diabetes. Aleglitazar activates PPAR receptors with EC50 in nanomolar range and exerts a cardioprotective effect in vitro. The drug is currently in phase III of clinical trials.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Peroxisome proliferator-activated receptor alpha 62	Agonist 2,752		5.0 nM [EC50]
Peroxisome proliferator-activated receptor gamma 118	Agonist 2,752		9.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262	Primary		Phase III 665	Unknown

C_max

Value	Dose	Analyte	Population
1.1 ng/mL	20 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
3.05 ng/mL	50 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
28.9 ng/mL	600 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
5.91 ng/mL	100 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
16.8 ng/mL	300 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
49.2 ng/mL	900 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
8.66 ng × h/mL	20 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
26 ng × h/mL	50 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
204 ng × h/mL	600 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
41.8 ng × h/mL	100 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
141 ng × h/mL	300 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
402 ng × h/mL	900 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
6.04 h	20 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
7.77 h	50 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
13.4 h	600 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
8.2 h	100 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
11.9 h	300 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens
16.4 h	900 μg 1 times / day steady-state, oral	ALEGLITAZAR plasma	Homo sapiens

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
001 Chemical	DY105513	https://www.001chemical.com/chem/search?q=DY105513
1PlusChem LLC	1P00DBLC	https://www.1pchem.com/search?query=1P00DBLC
AK Scientific	3431AH	https://aksci.com/item_detail.php?cat=3431AH
AstaTech	42161	http://astatechinc.com/CPSResult.php?CRNO=42161
BOC Sciences	475479-34-6	http://www.bocsci.com/description.asp?cas=475479-34-6

Showing 1 to 5 of 19 entries

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PubMed

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Title	Date	PubMed
Effect of the dual peroxisome proliferator-activated receptor-alpha/gamma agonist aleglitazar on risk of cardiovascular disease in patients with type 2 diabetes (SYNCHRONY): a phase II, randomised, dose-ranging study.	2009 Jul 11	19515415
PPAR-alpha and PPAR-gamma agonists for type 2 diabetes.	2009 Jul 11	19515412
A cardiologic approach to non-insulin antidiabetic pharmacotherapy in patients with heart disease.	2009 Jul 20	19619327
Therapeutic potential of aleglitazar, a new dual PPAR-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus.	2010	20653327
Pharmacokinetics, pharmacodynamics, and tolerability of aleglitazar in patients with type 2 diabetes: results from a randomized, placebo-controlled clinical study.	2010 Aug	20336066

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Patents

Sample Use Guides

In Vivo Use Guide

Patients receive 150 mcg orally daily.

Route of Administration: Oral

In Vitro Use Guide

Aleglitazar increased cell viability and reduced apoptosis in human cardiomyocytes at concentrations of 150-600 nM.

Show entries

Name

Type

Language

R-1439

Preferred Name

English

ALEGLITAZAR

Official Name

English

aleglitazar [INN]

Common Name

English

ALEGLITAZAR [USAN]

Common Name

English

Aleglitazar [WHO-DD]

Common Name

English

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Classification Tree

Code System

Code

Anti-diabetic Agent

NCI_THESAURUS

C98233

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Code System

Code

Type

Description

DRUG BANK

DB08915

PRIMARY

FDA UNII

41T4OAG59U

PRIMARY

USAN

TT-44

PRIMARY

ChEMBL

CHEMBL519504

PRIMARY

WIKIPEDIA

ALEGLITAZAR

PRIMARY

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ACTIVE MOIETY


					41T4OAG59U

ALEGLITAZAR

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2