Imiglitazar
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Imiglitazar 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]
Imiglitazar functions by activating PPAR-alpha and PPAR-gamma receptors. These receptors are nuclear hormone receptors that regulate the expression of genes involved in glucose and lipid metabolism. Activation of PPAR-alpha leads to increased fatty acid oxidation and improved lipid profiles, while activation of PPAR-gamma enhances insulin sensitivity and glucose uptake in adipose tissue and muscle.
Clinical Development[edit | edit source]
Imiglitazar was developed as a potential treatment for type 2 diabetes due to its dual action on PPAR-alpha and PPAR-gamma. However, its development was halted during clinical trials. The reasons for discontinuation included concerns about safety and efficacy, as well as the emergence of adverse effects that outweighed the potential benefits.
Pharmacokinetics[edit | edit source]
The pharmacokinetic profile of imiglitazar includes its absorption, distribution, metabolism, and excretion. It is absorbed orally and undergoes hepatic metabolism. The exact metabolic pathways and the half-life of the drug were subjects of investigation during its clinical trials.
Adverse Effects[edit | edit source]
During clinical trials, imiglitazar was associated with several adverse effects. These included weight gain, edema, and potential cardiovascular risks, which are common concerns with PPAR-gamma agonists. The safety profile was a significant factor in the decision to discontinue its development.
Research and Development[edit | edit source]
Research into PPAR agonists like imiglitazar continues, as these compounds hold promise for the treatment of metabolic disorders. However, the challenge remains to develop drugs that provide therapeutic benefits without significant adverse effects.
Also see[edit | edit source]
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