Englitazone

A thiazolidinedione drug

Englitazone
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Englitazone is a member of the thiazolidinedione class of drugs, which are primarily used as antidiabetic medications. These drugs function as insulin sensitizers, improving the body's response to insulin and thereby lowering blood glucose levels.

Mechanism of Action

Englitazone works by activating the peroxisome proliferator-activated receptor gamma (PPAR-_), a type of nuclear receptor. This activation leads to changes in the expression of genes involved in glucose and lipid metabolism. By enhancing insulin sensitivity, englitazone helps to control blood sugar levels in patients with type 2 diabetes mellitus.

Pharmacokinetics

The pharmacokinetic profile of englitazone includes its absorption, distribution, metabolism, and excretion. Englitazone is absorbed in the gastrointestinal tract and is subject to first-pass metabolism in the liver. It is primarily metabolized by the cytochrome P450 enzyme system and is excreted in the urine and feces.

Clinical Use

Englitazone was investigated for its potential use in the treatment of type 2 diabetes. However, like other thiazolidinediones, its development was halted due to concerns over safety and efficacy. The drug was never marketed, and its use remains limited to research settings.

Side Effects

Common side effects associated with thiazolidinediones, including englitazone, are weight gain, edema, and an increased risk of heart failure. These side effects are due to fluid retention and changes in fat distribution. Long-term use of thiazolidinediones has also been associated with an increased risk of bone fractures.

Related Pages

• Thiazolidinedione
• Type 2 diabetes mellitus
• Insulin sensitizer
• Peroxisome proliferator-activated receptor

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  Englitazone