Efficacy and safety of muraglitazar: a double-blind, 24-week, dose-ranging study in patients with type 2 diabetes.
Muraglitazar is a dual (alpha/gamma) PPAR activator. Dual receptor activation may improve glycaemic and lipid profiles in patients with type 2 diabetes mellitus.This randomised double-blind trial in 1,477 drug-naive patients with type 2 diabetes compared the efficacy and safety of muraglitazar (0.5, 1.5, 5, 10, and 20 mg) with pioglitazone (15 mg). Endpoints included changes in HbA(1C) and plasma lipids, last observation carried forward over 24 weeks. At week 24, mean changes from baseline in HbA(1C) ranged from -0.25% to -1.76% with muraglitazar (p<or=0.0008, 0.5 mg versus each higher muraglitazar dose), compared with -0.57% with pioglitazone. At week 12, tri-glycerides decreased 4-41% with muraglitazar and 9% with pioglitazone. High-density lipoprotein cholesterol increased 6-23% with muraglitazar and 10% with pioglitazone. Oedema-related events occurred with muraglitazar in a dose-dependent incidence (range 9-40%), and at 14% with pioglitazone. Overall, muraglitazar produced simultaneous dose-dependent improvements in glycaemic and lipid parameters in drug-naive patients with type 2 diabetes mellitus.
Rubin
Cindy J
CJ
1Pharmaceutical Research Institute, Bristol-Myers Squibb, Princeton, New Jersey 08543, USA. cindy.rubin@bms.com
Viraswami-Appanna
Kalyanee
K
Fiedorek
Fred T
FT
D015415:Biomarkers / Q000097:blood; D001786:Blood Glucose / Q000378:metabolism; D002096:C-Peptide / Q000097:blood; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004487:Edema / Q000139:chemically induced; D005260:Female; D006442:Glycated Hemoglobin / Q000378:metabolism; D005998:Glycine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives*; D006801:Humans; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000009:adverse effects; D007328:Insulin / Q000097:blood; D008055:Lipids / Q000097:blood; D008297:Male; D008875:Middle Aged; D010080:Oxazoles / Q000008:administration & dosage* / Q000009:adverse effects; D047493:PPAR alpha / Q000819:agonists; D047495:PPAR gamma / Q000819:agonists; D000077205:Pioglitazone; D045162:Thiazolidinediones / Q000008:administration & dosage* / Q000009:adverse effects; D013997:Time Factors; D016896:Treatment Outcome; D015430:Weight Gain / Q000187:drug effects
D015415:Biomarkers; D001786:Blood Glucose; D002096:C-Peptide; D006442:Glycated Hemoglobin; D005998:Glycine; D007004:Hypoglycemic Agents; D007328:Insulin; D008055:Lipids; D010080:Oxazoles; D047493:PPAR alpha; D047495:PPAR gamma; D000077205:Pioglitazone; D045162:Thiazolidinediones; C517652:hemoglobin A1c protein, human; C500085:muraglitazar