Englitazone: Difference between revisions

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'''Englitazone''' is a [[thiazolidinedione]] derivative, which is a type of [[antidiabetic drug]]. It was developed by [[Eli Lilly and Company]] but was never marketed.
{{Short description|A thiazolidinedione drug}}
{{Drugbox
| image = Englitazone.svg
| image_size = 200px
| image_alt = Structural formula of Englitazone
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== Mechanism of Action ==
'''Englitazone''' is a member of the [[thiazolidinedione]] class of drugs, which are primarily used as [[antidiabetic medication]]s. These drugs function as [[insulin sensitizer]]s, improving the body's response to insulin and thereby lowering [[blood glucose]] levels.
Englitazone works by activating [[peroxisome proliferator-activated receptors]] (PPARs), specifically PPARγ. PPARs are a group of [[nuclear receptor]] proteins that function as transcription factors regulating the expression of genes. PPARγ activation results in an increase in the transcription of [[insulin-responsive genes]], leading to better cellular response to insulin.


== Pharmacokinetics ==
==Mechanism of Action==
The [[pharmacokinetics]] of englitazone, like other thiazolidinediones, involves absorption in the [[gastrointestinal tract]] after oral administration. It is extensively metabolized in the liver and excreted in the urine and feces.
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]].


== Side Effects ==
==Pharmacokinetics==
Potential side effects of englitazone include [[weight gain]], [[edema]], and potential increase in [[cardiovascular disease]] risk. It may also cause or exacerbate [[congestive heart failure]] in some patients.
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.


== Development and Marketing ==
==Clinical Use==
Englitazone was developed by Eli Lilly and Company but was never marketed. The reasons for this are not publicly disclosed, but may be related to the side effect profile or market competition.
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.


== See Also ==
==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]]
* [[Thiazolidinedione]]
* [[Peroxisome proliferator-activated receptors]]
* [[Type 2 diabetes mellitus]]
* [[Insulin resistance]]
* [[Insulin sensitizer]]
* [[Type 2 diabetes]]
* [[Peroxisome proliferator-activated receptor]]


[[Category:Thiazolidinediones]]
[[Category:Thiazolidinediones]]
[[Category:Abandoned drugs]]
[[Category:Experimental drugs]]
[[Category:Antidiabetic drugs]]
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Latest revision as of 01:50, 20 February 2025

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[edit]

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[edit]

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[edit]

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[edit]

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[edit]