Glitazars are dual peroxisome proliferator-activated receptors (PPAR) alpha/gamma agonists that improve the lipid profile and exert an antidiabetic action — similar to a combination of a fibrate and a thiazolidinedione. In May 2006 the two glitazars most advanced in development, muraglitazar (Pargluva) and tesaglitazar (Galida) were discontinued. Muraglitazar was associated with an increased incidence of heart failure and tesaglitazar was associated with decreased glomerular filtration.
Staels B.The clinical significance of PPARα and γ agonism. Br J Diabetes Vasc Dis2002;2(suppl 1):S28-S31.
2.
Pershadsingh HADual peroxisome proliferator-activated receptor-alpha/gamma agonists: in the treatment of type 2 diabetes mellitus and the metabolic syndrome . Treat Endocrinol2006;5:89-99.
3.
Bailey CJNew drugs for the treatment of diabetes mellitus. In international textbook of diabetes mellitus, 3rd edn. RA DeFronzo, E Ferrannini , H Keen , P Zimmet (eds). Chichester: John Wiley, 2004, 951-79.
Kendall DM, Rubin CJ, Mohideen P. et al. 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 Care2006;29:1016-23.
6.
Nissen SE, Wolski K., Topol EJEffect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus. JAMA2005;294:2581-6.
7.
Fagerberg B. , Edwards S., Halmos T. et al. Tesaglitazar, a novel dual peroxisome proliferators-ativated receptor α/γ agonist, dose-dependently improves the metabolic abnormalities associated with insuln resistance in a non-diabetic population. Diabetologia2005;48:1716-25.
8.
Goldstein BJ , Rosenstock J., Anzalone D. et al. Tesaglitazar improves glucose and lipid abnormalities in patients with type 2 diabetes . Diabetes2005;54(suppl 1):83-OR.
9.
The FIELD study investigators.Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study), a randomised controlled trial. Lancet2005;366:1849-61.
10.
Dormandy JA , Charbonnel B., Eckland DJA et al. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive study (prospective pioglitazone clinical trial in macrovascular events): a randomised controlled trial. Lancet2005;366:1279-89.
