Muraglitazar

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Muraglitazar
Muraglitazar.png
Systematic (IUPAC) name
N-[(4-methoxyphenoxy)carbonyl]-N-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzyl}glycine
Clinical data
Legal status
?
Identifiers
CAS number 331741-94-7 YesY
ATC code None
PubChem CID 206044
ChemSpider 178524 N
UNII W1MKM70WQI N
KEGG D05091 YesY
ChEMBL CHEMBL557580 N
Synonyms 2-[(4-Methoxyphenoxy)carbonyl-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]amino]acetic acid
Chemical data
Formula C29H28N2O7 
Mol. mass 516.54 g/mol
 N (what is this?)  (verify)

Muraglitazar (proposed tradename Pargluva) is a peroxisome proliferator-activated receptor agonist with affinity to PPARα and PPARγ.[1]

The drug had completed phase III clinical trials,[2] however in May, 2006 Bristol-Myers Squibb announced that it had discontinued further development.[3]

Data on muraglitazar is relatively less due to the recent introduction of this agent. One double-blind randomized clinical trial[2] comparing muraglitazar and pioglitazone found that the effects of the former were favourable in terms of HDL-C increase, decrease in total cholesterol, apolipoprotein B, triglycerides and a greater reduction in HbA1c (P<0.0001 for all comparisons). However, the muraglitazar group had a higher all-cause mortality, greater incidence of edema and heart failure and more weight gain compared to the pioglitazone group. A meta-analysis of the phase 2 and 3 clinical trials of muraglitazar revealed that it was associated with a greater incidence of myocardial infarction, stroke, transient ischemic attacks and CHF when compared to placebo or pioglitazone.[4]

References[edit]

  1. ^ Waites CR, Dominick MA, Sanderson TP, Schilling BE (2007). "Nonclinical safety evaluation of muraglitazar, a novel PPARalpha/gamma agonist". Toxicol. Sci. 100 (1): 248–58. doi:10.1093/toxsci/kfm193. PMID 17675651. 
  2. ^ a b Kendall DM, Rubin CJ, Mohideen P, Ledeine JM, Belder R, Gross J, Norwood P, O'Mahony M, Sall K, Sloan G, Roberts A, Fiedorek FT, DeFronzo RA (2006). "Improvement of glycemic control, triglycerides, and HDL cholesterol levels with muraglitazar, a dual (alpha/gamma) peroxisome proliferator-activated receptor activator, in patients with type 2 diabetes inadequately controlled with metformin monotherapy: A double-blind, randomized, pioglitazone-comparative study". Diabetes Care 29 (5): 1016–23. doi:10.2337/diacare.2951016. PMID 16644631. 
  3. ^ "Bristol-Myers Squibb Announces Discontinuation of Development of Muraglitazar, an Investigational Oral Treatment for Type 2 Diabetes". Bristol-Myers Squibb. 2006-05-18. Retrieved 2008-03-18. 
  4. ^ Nissen SE, Wolski K, Topol EJ (November 2005). "Effect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus". JAMA 294 (20): 2581–6. doi:10.1001/jama.294.20.joc50147. PMID 16239637.