Korean J Med.  2014 Jul;87(1):19-25.

Peroxisome Proliferator-Activated Receptor (PPAR) alpha/gamma Agonist

• Lee J

Abstract

Peroxisome proliferator-activated receptor (PPAR) agonists improve glucose control and insulin sensitivity, reduce concentrations of atherogenic lipoproteins, and decrease circulating levels of inflammatory mediators. PPAR activation is considered an important pharmacologic target for patients with type 2 diabetes. However, the PPAR agonists in clinical use have undesirable side effects, including weight gain, heart failure, and bone fractures. PPAR alpha/gamma dual agonists each target one or more of the key cardiometabolic risk factors of diabetic dyslipidemia, insulin resistance, hyperglycemia, and inflammation; thus, combining their benefits to provide glucose control and ameliorate cardiovascular risks has emerged as an attractive treatment option. Aleglitazar, which was designed to balance the activation of PPAR alpha/gamma, proved efficacious in improving glycemic control and lipid homeostasis and is anticipated to minimize PPAR-related side effects. Whether the effects of aleglitazar on cardiometabolic risk factors translate into improved cardiovascular outcomes, particularly in high-risk patients, is currently being evaluated by AleCardio, a large, long-term, time-, and event-driven outcome study of type 2 diabetics with recent acute coronary syndrome.

Keyword

PPAR alpha/gamma agonist; Diabetic dyslipidemia; Insulin resistance; Aleglitazar

MeSH Terms

Acute Coronary Syndrome
Dyslipidemias
Fractures, Bone
Glucose
Heart Failure
Homeostasis
Humans
Hyperglycemia
Inflammation
Insulin Resistance
Lipoproteins
Outcome Assessment (Health Care)
Peroxisome Proliferator-Activated Receptors
Peroxisomes*
Risk Factors
Weight Gain
Glucose
Lipoproteins
Peroxisome Proliferator-Activated Receptors