Tesaglitazar

Summary

Tesaglitazar (CHEMBL282686) is a phase-3 clinical-stage small molecule; indicated across 1 condition including type 2 diabetes mellitus.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 17
• Chemistry: 408.5 Da · C20H24O7S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL282686
Name	Tesaglitazar
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	208901
Molecular formula	C20H24O7S
Molecular weight	408.5
InChIKey	CXGTZJYQWSUFET-IBGZPJMESA-N

SMILES: CCO[C@@H](CC1=CC=C(C=C1)OCCC2=CC=C(C=C2)OS(=O)(=O)C)C(=O)O

IUPAC name: (2S)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid

Also known as: AR-H-039242, AR-H039242XX, Az-242, AZ-242, BR-44608, Galida, Tesaglitazar, (S)-tesaglitazar, tesaglitazar, TESAGLITAZAR

Patent coverage: 1,771 distinct patent families (7,488 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor gamma.

Bioactivity

ChEMBL activities: 27 potent at pChembl ≥ 5 of 27 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PPARG	7.89	EC50	13	nM	CHEMBL_ACT_2257760
PPARG	7.75	Ki	18	nM	CHEMBL_ACT_2080378
PPARA	7.43	EC50	37	nM	CHEMBL_ACT_2080409
PPARG	6.89	EC50	130	nM	CHEMBL_ACT_26335923
P37238	6.7	Ki	200	nM	CHEMBL_ACT_1463471
P37238	6.6	EC50	250	nM	CHEMBL_ACT_1463473
P37238	6.6	EC50	250	nM	CHEMBL_ACT_18102609
PPARA	6.54	EC50	290	nM	CHEMBL_ACT_26335924
PPARG	6.46	IC50	350	nM	CHEMBL_ACT_1001264
PPARG	6.44	EC50	360	nM	CHEMBL_ACT_18102589
PPARA	6.38	EC50	414	nM	CHEMBL_ACT_2080387
PPARG	6.15	EC50	704	nM	CHEMBL_ACT_2371601
PPARG	6.15	EC50	704	nM	CHEMBL_ACT_2483470
PPARA	6.09	EC50	820	nM	CHEMBL_ACT_2257754
PPARA	6	Ki	1000	nM	CHEMBL_ACT_1463470
PPARA	5.92	EC50	1200	nM	CHEMBL_ACT_1001261
PPARA	5.92	EC50	1200	nM	CHEMBL_ACT_12188796
PPARG	5.89	EC50	1300	nM	CHEMBL_ACT_1001262
PPARG	5.89	EC50	1300	nM	CHEMBL_ACT_12188773
PPARA	5.77	EC50	1700	nM	CHEMBL_ACT_1463472
P23204	5.77	EC50	1700	nM	CHEMBL_ACT_18102608
PPARA	5.51	EC50	3120	nM	CHEMBL_ACT_2483436
PPARA	5.5	EC50	3124	nM	CHEMBL_ACT_2371665
PPARG	5.45	EC50	3528	nM	CHEMBL_ACT_1893422
PPARA	5.42	IC50	3800	nM	CHEMBL_ACT_1001263
PPARA	5.42	EC50	3800	nM	CHEMBL_ACT_18102577
PPARA	5.01	EC50	9798	nM	CHEMBL_ACT_1893447

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 17.

Phase distribution

Phase	Trials
PHASE3	13
PHASE2	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00214565	PHASE3	TERMINATED	GALLANT 6 Tesaglitazar vs. Pioglitazone
NCT00214591	PHASE3	TERMINATED	GALLANT 5 Tesaglitazar Versus Metformin
NCT00226330	PHASE3	TERMINATED	GALLEX 6: Study to Evaluate the Safety and Tolerability of Tesaglitazar in Patients With Type 2 Diabetes Mellitus
NCT00229710	PHASE3	TERMINATED	GALLEX 9: Safety and Tolerability of Oral Tesaglitazar When Added to Insulin Therapy in Patients With Type 2 Diabetes
NCT00242372	PHASE3	TERMINATED	GALLANT 9 Tesaglitazar vs. Placebo in Combination With Insulin
NCT00251940	PHASE3	TERMINATED	GALLANT 7 Tesaglitazar Add-on to Sulphonylurea
NCT00251953	PHASE3	TERMINATED	GALLANT 8 Tesaglitazar Add-on to Metformin
NCT00252772	PHASE3	TERMINATED	GALLANT 2 Tesaglitazar vs. Placebo
NCT00252837	PHASE3	TERMINATED	GALLANT 22 Tesaglitazar vs. Placebo
NCT00252876	PHASE3	TERMINATED	GALLEX 1 - Long Term Extension Study in Patients With Type 2 Diabetes
NCT00255541	PHASE3	TERMINATED	GALLANT 4 Tesaglitazar vs. Glibenclamide
NCT00261352	PHASE3	TERMINATED	GALLANT 14 Tesaglitazar vs. Metformin and Fenofibrate
NCT00300105	PHASE3	TERMINATED	GALLEX 4 - Long-Term Extension Study to Evaluate Tesaglitazar Therapy in Patients With Type 2 Diabetes
NCT00229684	PHASE2	TERMINATED	ARMOR (Analyzing Renal Mechanisms of Creatinine Excretion in Patients On tesaglitazaR)
NCT00261417	PHASE2	TERMINATED	Dose Response Study in Japanese Patients
NCT00263965	PHASE2	TERMINATED	ARAMIS: Actions of tesaglitazaR on fAt Metabolism and Insulin Sensitivity
NCT00280865	PHASE2	COMPLETED	GLAD: Dose-Finding, Efficacy, and Safety of AZ 242 (Tesaglitazar) in Subjects With Type 2 Diabetes

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).