Pioglitazone
From Proteopedia
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| - | < | + | <StructureSection load='' size='340' side='right' caption='Pioglitazone, also known as Actos' scene='Pioglitazone/Pioglitazone/1'> |
===Better Known as: Actos=== | ===Better Known as: Actos=== | ||
* Marketed By: Takeda Pharmaceuticals<br /> | * Marketed By: Takeda Pharmaceuticals<br /> | ||
* Major Indication: Hypoglycemia & Type 2 [[Diabetes]]<br /> | * Major Indication: Hypoglycemia & Type 2 [[Diabetes]]<br /> | ||
| - | * Drug Class: [[PPAR|PPAR-γ]] | + | * Drug Class: [[PPAR|PPAR-γ]] Agonist - Thiazolidinedione (Glitazones) |
* Date of FDA Approval (Patent Expiration): 1999 (2011)<br /> | * Date of FDA Approval (Patent Expiration): 1999 (2011)<br /> | ||
* 2009 Sales: $2.4 Billion <ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS</ref> | * 2009 Sales: $2.4 Billion <ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS</ref> | ||
| - | * | + | * Importance: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States. |
| - | * | + | * See [[Pharmaceutical Drugs]] for more information about other drugs and disorders |
| + | |||
| + | ===Mechanism of Action=== | ||
| + | Pioglitazone is a selective agonist for Peroxisome Proliferator-Activated Receptor Gamma ([[PPAR]]). When PPAR is not bound by ligand, it forms a complex with various co-repressors which possess histone deacetylation activity, maintaining tight chromatin structure and preventing gene transcription. This complex is released upon ligand binding (typical ligands are lipids), allowing various co-activators and co-activator-associated proteins to be recruited. Pioglitazone functions by by binding to the active site of PPARγ, causing the release of co-repressors and activation of the receptor. Activation of PPAR results in transcription of [[Molecular Playground/Insulin|insulin]] responsive genes involved in the control of glucose production, transport and utilization. This explains why the glitazones are referred to as "insulin sensitizers." <ref>PMID:9744270</ref> | ||
| + | </StructureSection> | ||
| + | ===Pharmacokinetics=== | ||
| + | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | ||
| + | <tr> | ||
| + | <td style="width:100%; vertical-align:top;border-width:0px; border-style:inset"> | ||
| + | <div style="height:100%; width: 100%"> | ||
| + | {{:Glitazone Pharmacokinetics}} | ||
| + | </div> | ||
| + | </td> | ||
| + | </tr> | ||
| + | </table> | ||
===References=== | ===References=== | ||
Current revision
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Pharmacokinetics
For Pharmacokinetic Data References, See: References |
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References
- ↑ http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS
- ↑ Nolte RT, Wisely GB, Westin S, Cobb JE, Lambert MH, Kurokawa R, Rosenfeld MG, Willson TM, Glass CK, Milburn MV. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature. 1998 Sep 10;395(6698):137-43. PMID:9744270 doi:10.1038/25931
