Cevoglitazar

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Cevoglitazar_structure.png



Cevoglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist that has been investigated for its potential use in 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]

Cevoglitazar functions by activating PPAR-alpha and PPAR-gamma receptors.

  • PPAR-alpha activation leads to increased fatty acid oxidation and improved lipid profiles, which can help reduce triglyceride levels and increase HDL cholesterol.
  • PPAR-gamma activation enhances insulin sensitivity and glucose uptake in adipose tissue and muscle, thereby lowering blood glucose levels.

The dual activation of these receptors is intended to provide a comprehensive approach to managing the metabolic abnormalities associated with type 2 diabetes.

Clinical Development[edit | edit source]

Cevoglitazar has undergone various stages of clinical trials to evaluate its efficacy and safety in patients with type 2 diabetes. However, like many dual PPAR agonists, its development has faced challenges due to concerns about potential side effects, including cardiovascular risks and weight gain.

Potential Benefits[edit | edit source]

The dual action of cevoglitazar on both PPAR-alpha and PPAR-gamma receptors offers several potential benefits:

  • Improved glycemic control
  • Reduction in triglyceride levels
  • Increase in HDL cholesterol
  • Potential weight management benefits

Safety and Side Effects[edit | edit source]

The safety profile of cevoglitazar is a critical aspect of its clinical evaluation. Common side effects associated with PPAR agonists include:

  • Weight gain
  • Edema
  • Cardiovascular risks

The balance between efficacy and safety is a key consideration in the development of cevoglitazar as a therapeutic agent.

Research and Future Directions[edit | edit source]

Research into cevoglitazar and other dual PPAR agonists continues, with a focus on optimizing their therapeutic benefits while minimizing adverse effects. Future studies may explore combination therapies or novel formulations to enhance the drug's safety and efficacy.

Also see[edit | edit source]



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