Reglitazar
| Reglitazar_structure.png | |
Reglitazar is a pharmaceutical compound that was investigated for its potential use as a thiazolidinedione (TZD) class drug, primarily targeting the treatment of type 2 diabetes mellitus. It functions as a dual peroxisome proliferator-activated receptor (PPAR) agonist, specifically targeting both the PPAR-alpha and PPAR-gamma subtypes. This dual action was hypothesized to provide benefits in both glucose metabolism and lipid regulation.
Mechanism of Action[edit | edit source]
Reglitazar acts by activating PPAR-alpha and PPAR-gamma receptors, which are nuclear hormone receptors that regulate the expression of genes involved in glucose and lipid metabolism. Activation of PPAR-gamma enhances insulin sensitivity in adipose tissue, muscle, and liver, while PPAR-alpha activation leads to increased fatty acid oxidation and improved lipid profiles.
Clinical Development[edit | edit source]
Reglitazar underwent several phases of clinical trials to evaluate its efficacy and safety in patients with type 2 diabetes. However, like many other drugs in the TZD class, concerns about potential adverse effects, such as cardiovascular disease and hepatotoxicity, led to a reevaluation of its risk-benefit profile.
Adverse Effects[edit | edit source]
The development of Reglitazar was halted due to concerns over adverse effects, which included potential cardiovascular risks and liver toxicity. These concerns are common among TZD drugs, as seen with other members of this class such as rosiglitazone and pioglitazone.
Current Status[edit | edit source]
As of the latest updates, Reglitazar is not approved for clinical use and remains a compound of interest primarily in research settings. Its development has been discontinued, and it is not available on the market.
Also see[edit | edit source]
- Thiazolidinedione
- Peroxisome proliferator-activated receptor
- Type 2 diabetes mellitus
- Rosiglitazone
- Pioglitazone
| 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
