Aleglitazar

Aleglitazar

Chemical structure of Aleglitazar

Aleglitazar is a pharmaceutical drug that was developed as a dual peroxisome proliferator-activated receptor (PPAR) agonist, targeting both the PPAR_ and PPAR_ subtypes. It was investigated for its potential use in the treatment of type 2 diabetes mellitus and associated cardiovascular disease.

Mechanism of Action

Aleglitazar functions by activating the PPAR_ and PPAR_ receptors, which play key roles in the regulation of lipid metabolism and glucose homeostasis. Activation of PPAR_ leads to increased fatty acid oxidation and improved lipid profile, while PPAR_ activation enhances insulin sensitivity and glucose uptake in adipose tissue.

Development and Clinical Trials

Aleglitazar was developed by Hoffmann-La Roche and underwent several phases of clinical trials. The drug showed promise in early studies by improving glycemic control and lipid parameters in patients with type 2 diabetes. However, later-stage trials raised concerns about its safety profile, particularly regarding heart failure and renal impairment.

Safety and Efficacy

The safety concerns observed in clinical trials included an increased risk of congestive heart failure, bone fractures, and renal dysfunction. These adverse effects led to the discontinuation of its development for the treatment of type 2 diabetes.

Conclusion

Despite its initial promise as a dual PPAR agonist, Aleglitazar's development was halted due to safety concerns. The case of Aleglitazar highlights the challenges in developing drugs that target multiple pathways and the importance of thorough safety evaluations in the drug development process.

Related Pages

• Type 2 diabetes mellitus
• Peroxisome proliferator-activated receptor
• Insulin resistance
• Cardiovascular disease