Pemaglitazar
| Pemaglitazar.svg | |
Pemaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist that was investigated for the treatment of type 2 diabetes mellitus. It acts on both the PPAR-alpha and PPAR-gamma receptors, which are involved in the regulation of glucose and lipid metabolism.
Mechanism of Action[edit | edit source]
Pemaglitazar functions by activating PPAR-alpha and PPAR-gamma receptors. PPAR-alpha activation leads to increased fatty acid oxidation and improved lipid profiles, while PPAR-gamma activation enhances insulin sensitivity and glucose uptake in adipose tissue and muscle. This dual action was intended to provide comprehensive metabolic control in patients with type 2 diabetes.
Clinical Development[edit | edit source]
Pemaglitazar was developed by Bristol-Myers Squibb and underwent clinical trials to assess its efficacy and safety in managing type 2 diabetes. However, during the clinical trials, concerns about adverse effects, particularly related to cardiovascular safety, led to the discontinuation of its development.
Adverse Effects[edit | edit source]
The primary concern with pemaglitazar was its potential to cause cardiovascular events. Similar to other PPAR agonists, there was an increased risk of heart failure and other cardiovascular complications, which ultimately led to the cessation of its development.
Pharmacokinetics[edit | edit source]
Pemaglitazar is administered orally and undergoes hepatic metabolism. The pharmacokinetic profile includes a moderate half-life, allowing for once-daily dosing. However, detailed pharmacokinetic data were not fully published due to the early termination of its development.
Research and Development[edit | edit source]
Despite its potential, pemaglitazar's development was halted due to safety concerns. The lessons learned from its development have informed the design and testing of subsequent PPAR agonists, emphasizing the importance of cardiovascular safety in the development of antidiabetic medications.
Also see[edit | edit source]
- Type 2 diabetes mellitus
- Peroxisome proliferator-activated receptor
- PPAR-alpha
- PPAR-gamma
- Thiazolidinediones
- Cardiovascular disease
| PPAR Agonists | |
|---|---|
| Type | Example |
| PPAR-α | Fibrate |
| PPAR-γ | Thiazolidinedione |
| PPAR-δ | GW501516 |
| Dual/Triple Agonists | |
| PPAR-α/γ | Saroglitazar |
| PPAR-α/δ | Elafibranor |
| PPAR-γ/δ | Tesaglitazar |
| PPAR pan | Bezafibrate |
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Contributors: Prab R. Tumpati, MD
