Aleglitazar

Summary

Aleglitazar (CHEMBL519504) 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: 22
• Chemistry: 437.5 Da · C24H23NO5S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL519504
Name	Aleglitazar
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10274777
Molecular formula	C24H23NO5S
Molecular weight	437.5
InChIKey	DAYKLWSKQJBGCS-NRFANRHFSA-N

SMILES: CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=C4C=CSC4=C(C=C3)C[C@@H](C(=O)O)OC

IUPAC name: (2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid

Also known as: Aleglitazar, R-1439, R1439, RO-0728804, RO0728804, Ro-0728804, ALEGLITAZAR

Patent coverage: 400 distinct patent families (1,072 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,063 (99%) of the total. 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: 5 (assay-derived). Sample: Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor alpha, Peroxisome proliferator-activated receptor delta.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PPARG	7.72	IC50	19	nM	CHEMBL_ACT_2509111
PPARG	7.68	EC50	21	nM	CHEMBL_ACT_2509177
PPARA	7.42	IC50	38	nM	CHEMBL_ACT_2509078
PPARA	7.3	EC50	50	nM	CHEMBL_ACT_2509144
PPARD	7.28	EC50	53	nM	CHEMBL_ACT_2525519
P37230	5.65	EC50	2260	nM	CHEMBL_ACT_2525538
P23204	5.63	EC50	2340	nM	CHEMBL_ACT_2525539

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: 22.

Phase distribution

Phase	Trials
PHASE3	8
PHASE1	8
PHASE2	6

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01042769	PHASE3	COMPLETED	A Study With Aleglitazar in Patients With a Recent Acute Coronary Syndrome and Type 2 Diabetes Mellitus
NCT01691755	PHASE3	COMPLETED	A Study of Aleglitazar in Patients With Type 2 Diabetes Mellitus Who Have Not Previously Received Anti-Hyperglycemic Therapy
NCT01691846	PHASE3	COMPLETED	A Study of Aleglitazar in Combination With Metformin in Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled With Metformin Alone
NCT01691989	PHASE3	COMPLETED	A Study of Aleglitazar in Combination With Metformin in Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled With Sulfonylurea Alone or Sulfonylurea Plus Metformin Therapy
NCT01715818	PHASE3	COMPLETED	A Study on The Potential of Aleglitazar to Reduce Cardiovascular Risk in Patients With Stable Cardiovascular Disease and Glucose Abnormalities
NCT01871415	PHASE3	COMPLETED	A Study of Aleglitazar in Combination With Metformin in Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled With Metformin Monotherapy
NCT01871428	PHASE3	COMPLETED	A Study of Aleglitazar in Monotherapy in Patients With Type 2 Diabetes Mellitus Who Are Drug-Naïve to Anti-Hyperglycemic Therapy
NCT01893242	PHASE3	WITHDRAWN	A Study of Alegitazar in Patients With Type 2 Diabetes And Chronic Kidney Disease (Alerenal Study)
NCT00388518	PHASE2	COMPLETED	A Study of Aleglitazar in Patients With Type 2 Diabetes
NCT00461006	PHASE2	COMPLETED	A Comparison of the Effects of Aleglitazar and Actos on Renal Function on Patients With Type 2 Diabetes.
NCT00461058	PHASE2	COMPLETED	A Comparative Study of Aleglitazar and Actos in Patients With Type 2 Diabetes Mellitus and New York Heart Association (NYHA) Class II Heart Failure.
NCT01043029	PHASE2	COMPLETED	A Study of Aleglitazar in Type 2 Diabetes Patients With Moderate Renal Impairment
NCT01680978	PHASE2	COMPLETED	A Study to Evaluate the Effect of Aleglitazar on Cardiac Energetics and Function in Patients With Type 2 Diabetes Mellitus and no History of Coronary Artery Disease
NCT01729403	PHASE2	COMPLETED	A Study of The Effect of Aleglitazar on Insulin Sensitivity in Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled With Metformin
NCT01188304	PHASE1	COMPLETED	A Study of Aleglitazar in Combination With Aspirin in Healthy Volunteers
NCT01188317	PHASE1	COMPLETED	A Study of Aleglitazar in Combination With Ibuprofen in Healthy Volunteers
NCT01197911	PHASE1	COMPLETED	A Study of The Effect of Hepatic Impairment on The Pharmacokinetics of Aleglitazar
NCT01398267	PHASE1	COMPLETED	A Pharmacodynamic/Pharmacokinetic Study of Aleglitazar in Patients With Type 2 Diabetes Mellitus on Treatment With Lisinopril
NCT01615354	PHASE1	COMPLETED	A Study of Aleglitazar in Combination With Oral Contraceptive Healthy Volunteers
NCT01679639	PHASE1	COMPLETED	A Study to Investigate the Effects of Rifampicin on the Pharmacokinetics of Aleglitazar in Healthy Volunteers
NCT01701739	PHASE1	COMPLETED	A Pharmacokinetics Study of Aleglitazar in Combination With Digoxin in Healthy Volunteers
NCT01711775	PHASE1	COMPLETED	A Pharmacokinetic Study of Aleglitazar in Healthy Chinese Volunteers

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).