title: Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular risk.
abstract: BACKGROUND
  In preliminary clinical studies, aleglitazar, a new dual PPAR-α-γ agonist, has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. This review will provide up-to-date information on the clinical safety and efficacy of aleglitazar, which is currently under Phase III clinical investigation for reduction of cardiovascular events in patients with type 2 diabetes and recent acute coronary syndrome.
  
  
  METHODS
  A PubMed literature search (January 1950 to February 2011) was conducted using the following search terms: aleglitazar, PPAR, PPAR α agonist, PPAR γ agonist and PPAR α/γ agonist. Additional articles were gathered using reference lists from sources obtained from the original literature search. This review summarizes available information pertaining to pharmacodynamics, pharmacokinetics, clinical studies and safety/tolerability of aleglitazar. The effects of this new drug are compared and contrasted with those of fibrates (PPAR-α agonists), thiazolidinediones (PPAR-γ agonists) and other dual PPAR-α-γ agonists.
  
  
  CONCLUSIONS
  Preliminary evidence from clinical studies with aleglitazar is promising, with reported improvements in glycemia, high-density lipoprotein-cholesterol, low-density lipoprotein-cholesterol, triglycerides, apolipoprotein B and blood pressure. However, PPAR-α- and -γ-associated side effects have been observed and additional large-scale, long-term clinical studies are necessary to better understand the clinical implications of these effects.
authors.affiliation: University of Maryland School of Medicine, Department of Medicine, Baltimore, MD 21201, USA.
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Younk
authors.forename: Lisa
authors.initials: L
authors.lastname: Uhl
authors.forename: Stephen N
authors.initials: SN
authors.lastname: Davis
mesh_terms: D001055:Apolipoproteins B / Q000097:blood; D001794:Blood Pressure; D002318:Cardiovascular Diseases / Q000517:prevention & control*; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004347:Drug Interactions; D058607:Fibric Acids / Q000627:therapeutic use; D006801:Humans; D007004:Hypoglycemic Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D010080:Oxazoles / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D047493:PPAR alpha / Q000819:agonists; D047495:PPAR gamma / Q000819:agonists; D045162:Thiazolidinediones / Q000627:therapeutic use; D013876:Thiophenes / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D014280:Triglycerides / Q000097:blood
chemical_list: D001055:Apolipoproteins B; D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D058607:Fibric Acids; D007004:Hypoglycemic Agents; D010080:Oxazoles; D047493:PPAR alpha; D047495:PPAR gamma; D045162:Thiazolidinediones; D013876:Thiophenes; D014280:Triglycerides; C542437:aleglitazar