“Muraglitazar”的意思、由来-开放百科全书

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 sparse 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 HbA_1c (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 II and III clinical trials of muraglitazar revealed that it was associated with a greater incidence of myocardial infarction, stroke, transient ischemic attacks and congestive heart failure (CHF) when compared to placebo or pioglitazone.^[4]

References

1. ^{{cite journal|last1=Waites|first1=CR|last2=Dominick|first2=MA|last3=Sanderson|first3=TP|last4=Schilling|first4=BE|title=Nonclinical Safety Evaluation of Muraglitazar, a Novel PPARα/γ Agonist|journal=Toxicological Sciences|date=13 August 2007|volume=100|issue=1|pages=248–58|doi=10.1093/toxsci/kfm193|pmid=17675651|url=http://toxsci.oxfordjournals.org/content/100/1/248.full.pdf|accessdate=9 November 2016}}
2. ^¹{{cite journal|last1=Kendall|first1=DM|last2=Rubin|first2=CJ|last3=Mohideen|first3=P|last4=Ledeine|first4=JM|last5=Belder|first5=R|last6=Gross|first6=J|last7=Norwood|first7=P|last8=O'Mahony|first8=M|last9=Sall|first9=K|last10=Sloan|first10=G|last11=Roberts|first11=A|last12=Fiedorek|first12=FT|last13=DeFronzo|first13=RA|title=Improvement of Glycemic Control, Triglycerides, and HDL Cholesterol Levels with Muraglitazar, a Dual (α/γ) Peroxisome Proliferator–Activated Receptor Activator, in Patients with Type 2 Diabetes Inadequately Controlled with Metformin Monotherapy|journal=Diabetes Care|date=May 2006|volume=29|issue=5|pages=1016–23|doi=10.2337/diacare.2951016|pmid=16644631|url=http://care.diabetesjournals.org/content/diacare/29/5/1016.full.pdf|accessdate=9 November 2016}}
3. ^{{cite web|title=Bristol-Myers Squibb Announces Discontinuation of Development of Muraglitazar, an Investigational Oral Treatment for Type 2 Diabetes|url=http://www.prnewswire.com/news-releases/bristol-myers-squibb-announces-discontinuation-of-development-of-muraglitazar-an-investigational-oral-treatment-for-type-2-diabetes-56462702.html|publisher=PR Newswire from Bristol-Myers Squibb|accessdate=9 November 2016|date=May 18, 2006}}
4. ^{{cite journal|last1=Nissen|first1=SE|last2=Wolski|first2=K|last3=Topol|first3=EJ|title=Effect of Muraglitazar on Death and Major Adverse Cardiovascular Events in Patients with Type 2 Diabetes Mellitus|journal=Journal of the American Medical Association|date=23 November 2005|volume=294|issue=20|pages=2581–6|doi=10.1001/jama.294.20.joc50147|pmid=16239637}}

词条	Muraglitazar
释义	References {{Drugbox \| Verifiedfields = changed \| Watchedfields = changed \| verifiedrevid = 407806745 \| IUPAC_name = N-[(4-Methoxyphenoxy)carbonyl]-N-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzyl}glycine \| image = Muraglitazar.svg \| width = 315 \| tradename = \| pregnancy_AU = \| pregnancy_US = \| pregnancy_category = \| legal_AU = \| legal_CA = \| legal_UK = \| legal_US = \| legal_status = Development terminated \| routes_of_administration = \| bioavailability = \| protein_bound = \| metabolism = \| elimination_half-life = \| excretion = \| CAS_number_Ref = {{cascite\|correct\|??}} \| CAS_number = 331741-94-7 \| ATC_prefix = None \| ATC_suffix = \| PubChem = 206044 \| DrugBank_Ref = {{drugbankcite\|correct\|drugbank}} \| DrugBank = \| UNII_Ref = {{fdacite\|changed\|FDA}} \| UNII = W1MKM70WQI \| KEGG_Ref = {{keggcite\|correct\|kegg}} \| KEGG = D05091 \| ChEMBL_Ref = {{ebicite\|changed\|EBI}} \| ChEMBL = 557580 \| ChemSpiderID_Ref = {{chemspidercite\|changed\|chemspider}} \| ChemSpiderID = 178524 \| C=29 \| H=28 \| N=2 \| O=7 \| molecular_weight = 516.54 g/mol \| 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 \| StdInChI_Ref = {{stdinchicite\|changed\|chemspider}} \| StdInChI = 1S/C29H28N2O7/c1-20-26(30-28(37-20)22-6-4-3-5-7-22)16-17-36-24-10-8-21(9-11-24)18-31(19-27(32)33)29(34)38-25-14-12-23(35-2)13-15-25/h3-15H,16-19H2,1-2H3,(H,32,33) \| StdInChIKey_Ref = {{stdinchicite\|changed\|chemspider}} \| StdInChIKey = IRLWJILLXJGJTD-UHFFFAOYSA-N \| synonyms = 2-[(4-Methoxyphenoxy)carbonyl-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]amino]acetic acid }}Muraglitazar (proposed tradename Pargluva) is a dual 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 sparse 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 HbA_1c (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 II and III clinical trials of muraglitazar revealed that it was associated with a greater incidence of myocardial infarction, stroke, transient ischemic attacks and congestive heart failure (CHF) when compared to placebo or pioglitazone.^[4] References 1. ^{{cite journal\|last1=Waites\|first1=CR\|last2=Dominick\|first2=MA\|last3=Sanderson\|first3=TP\|last4=Schilling\|first4=BE\|title=Nonclinical Safety Evaluation of Muraglitazar, a Novel PPARα/γ Agonist\|journal=Toxicological Sciences\|date=13 August 2007\|volume=100\|issue=1\|pages=248–58\|doi=10.1093/toxsci/kfm193\|pmid=17675651\|url=http://toxsci.oxfordjournals.org/content/100/1/248.full.pdf\|accessdate=9 November 2016}} 2. ^¹{{cite journal\|last1=Kendall\|first1=DM\|last2=Rubin\|first2=CJ\|last3=Mohideen\|first3=P\|last4=Ledeine\|first4=JM\|last5=Belder\|first5=R\|last6=Gross\|first6=J\|last7=Norwood\|first7=P\|last8=O'Mahony\|first8=M\|last9=Sall\|first9=K\|last10=Sloan\|first10=G\|last11=Roberts\|first11=A\|last12=Fiedorek\|first12=FT\|last13=DeFronzo\|first13=RA\|title=Improvement of Glycemic Control, Triglycerides, and HDL Cholesterol Levels with Muraglitazar, a Dual (α/γ) Peroxisome Proliferator–Activated Receptor Activator, in Patients with Type 2 Diabetes Inadequately Controlled with Metformin Monotherapy\|journal=Diabetes Care\|date=May 2006\|volume=29\|issue=5\|pages=1016–23\|doi=10.2337/diacare.2951016\|pmid=16644631\|url=http://care.diabetesjournals.org/content/diacare/29/5/1016.full.pdf\|accessdate=9 November 2016}} 3. ^{{cite web\|title=Bristol-Myers Squibb Announces Discontinuation of Development of Muraglitazar, an Investigational Oral Treatment for Type 2 Diabetes\|url=http://www.prnewswire.com/news-releases/bristol-myers-squibb-announces-discontinuation-of-development-of-muraglitazar-an-investigational-oral-treatment-for-type-2-diabetes-56462702.html\|publisher=PR Newswire from Bristol-Myers Squibb\|accessdate=9 November 2016\|date=May 18, 2006}} 4. ^{{cite journal\|last1=Nissen\|first1=SE\|last2=Wolski\|first2=K\|last3=Topol\|first3=EJ\|title=Effect of Muraglitazar on Death and Major Adverse Cardiovascular Events in Patients with Type 2 Diabetes Mellitus\|journal=Journal of the American Medical Association\|date=23 November 2005\|volume=294\|issue=20\|pages=2581–6\|doi=10.1001/jama.294.20.joc50147\|pmid=16239637}} {{Oral hypoglycemics}}{{PPAR modulators}}{{gastrointestinal-drug-stub}} 5 : Abandoned drugs\|Oxazoles\|Carbamates\|Phenol ethers\|PPAR agonists
随便看	Jilbadji Land District Jilbania Jilbe language Jilbert's Dairy Jil Caplan JIL Church JIL (disambiguation) Jil (disambiguation) Jildo Irwa Jilebi Jileck Ji Lee Jilek Jilem (Havlickuv Brod District) Jilem (Havlíčkův Brod District) Jilem (Jindrichuv Hradec District) Jilem (Jindřichův Hradec District) Jiles Perry Richardson Jilga District Jili Jilian grace Jilib District Jili District Jili ffrwtan Ji-li Jiang