Muraglitazar
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Also known as BMS-298585MK-0478MK0478SID170466259Muraglitizar
Summary
Muraglitazar (CHEMBL186179) is a phase-3 clinical-stage small molecule; indicated across 3 conditions including diabetes mellitus and type 2 diabetes mellitus.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 3 conditions
- Clinical trials: 10
- Chemistry: 516.5 Da · C29H28N2O7
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL186179 |
| Name | Muraglitazar |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 206044 |
| Molecular formula | C29H28N2O7 |
| Molecular weight | 516.5 |
| InChIKey | IRLWJILLXJGJTD-UHFFFAOYSA-N |
SMILES: CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=CC=C(C=C3)CN(CC(=O)O)C(=O)OC4=CC=C(C=C4)OC
IUPAC name: 2-[(4-methoxyphenoxy)carbonyl-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]amino]acetic acid
Also known as: BMS-298585, MK-0478, MK0478, Muraglitazar, muraglitazar, MURAGLITAZAR, SID170466259, Muraglitizar
Parent form; salt/anhydrous children: CHEMBL557580, CHEMBL3527055
Patent coverage: 444 distinct patent families (1,191 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: 2 (assay-derived). Sample: Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor alpha.
Bioactivity
ChEMBL activities: 25 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PPARG | 8.52 | EC50 | 3 | nM | CHEMBL_ACT_18346878 |
| PPARG | 7.8 | EC50 | 16 | nM | CHEMBL_ACT_26335916 |
| PPARG | 7.46 | EC50 | 35 | nM | CHEMBL_ACT_15159432 |
| PPARG | 7.46 | EC50 | 35 | nM | CHEMBL_ACT_2269627 |
| PPARG | 7.4 | EC50 | 40 | nM | CHEMBL_ACT_2173266 |
| PPARA | 7.3 | EC50 | 50 | nM | CHEMBL_ACT_26335917 |
| PPARG | 7.05 | EC50 | 90 | nM | CHEMBL_ACT_2503981 |
| PPARG | 7 | EC50 | 100 | nM | CHEMBL_ACT_12188774 |
| PPARG | 6.96 | EC50 | 110 | nM | CHEMBL_ACT_1518994 |
| PPARG | 6.92 | EC50 | 120 | nM | CHEMBL_ACT_1463604 |
| PPARG | 6.92 | IC50 | 120 | nM | CHEMBL_ACT_18758364 |
| PPARG | 6.82 | EC50 | 153 | nM | CHEMBL_ACT_2483469 |
| PPARA | 6.82 | EC50 | 150 | nM | CHEMBL_ACT_2503972 |
| PPARG | 6.72 | IC50 | 190 | nM | CHEMBL_ACT_1518993 |
| PPARA | 6.72 | IC50 | 190 | nM | CHEMBL_ACT_2173264 |
| PPARA | 6.62 | EC50 | 240 | nM | CHEMBL_ACT_1463603 |
| PPARA | 6.6 | IC50 | 250 | nM | CHEMBL_ACT_1518981 |
| PPARG | 6.6 | IC50 | 250 | nM | CHEMBL_ACT_2173265 |
| PPARA | 6.52 | EC50 | 300 | nM | CHEMBL_ACT_12188797 |
| PPARA | 6.5 | EC50 | 320 | nM | CHEMBL_ACT_1518991 |
| PPARA | 6.22 | EC50 | 595 | nM | CHEMBL_ACT_18346839 |
| PPARA | 5.85 | EC50 | 1410 | nM | CHEMBL_ACT_15160460 |
| PPARA | 5.85 | EC50 | 1410 | nM | CHEMBL_ACT_2173267 |
| PPARA | 5.85 | EC50 | 1410 | nM | CHEMBL_ACT_2269629 |
| PPARA | 5.39 | EC50 | 4110 | nM | CHEMBL_ACT_2483435 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
3 indications (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 |
|---|---|---|---|
| diabetes mellitus | 3 | MONDO:0005015 | EFO:0000400 |
| type 2 diabetes mellitus | 3 | MONDO:0005148 | MONDO:0005148 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 10.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 8 |
| PHASE2/PHASE3 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00094991 | PHASE3 | COMPLETED | Mechanism of Action and Efficacy of Muraglitazar in Type 2 Diabetes |
| NCT00095030 | PHASE3 | COMPLETED | Study Comparing Muraglitazar With Glimepiride in Type 2 Diabetics Who Are Not Controlled With Metformin Alone |
| NCT00106808 | PHASE3 | COMPLETED | Study of Muraglitazar Versus Pioglitazone in Type 2 Diabetes |
| NCT00130806 | PHASE3 | TERMINATED | An Investigational Drug Co-Administered With Insulin in Patients With Type 2 Diabetes (0478-065) |
| NCT00162175 | PHASE3 | COMPLETED | PPAR-COMBO With Sulfonylurea |
| NCT00162240 | PHASE3 | COMPLETED | PPAR - Combination With Metformin |
| NCT00240370 | PHASE3 | COMPLETED | A Study to Evaluate Combining Metformin With Muraglitazar or Pioglitazone in Type 2 Diabetics |
| NCT00240383 | PHASE2/PHASE3 | COMPLETED | Dose Ranging Study With LT, Monotherapy, PPAR |
| NCT00245388 | PHASE2/PHASE3 | COMPLETED | Efficacy and Safety of BMS-298585 Alone or in Combination With Pravastatin in Subjects With Mixed Dyslipidemia |
| NCT00246987 | PHASE3 | COMPLETED | A Trial to Evaluate BMS-298585 as Monotherapy in Subjects With Type 2 Diabetes Who Have Inadequate Glycemic Control |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: diabetes mellitus, type 2 diabetes mellitus