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Pioglitazone

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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/>
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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 />
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* 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.
* Importance: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States.
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* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
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* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders
===Mechanism of Action===
===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>
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>
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</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
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<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
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{| class="wikitable" border="1" width="40%" style="text-align:center"
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<tr>
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<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
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! colspan="6" align="center"| Glitazone [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>doi: 10.1111/j.1365-2125.2007.02986.x</ref><ref>PMID:18997160</ref><ref>PMID: 9454824</ref><ref>PMID: 17594391</ref>
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<div style="height:100%; width: 100%">
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|-
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{{:Glitazone Pharmacokinetics}}
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! Parameter
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</div>
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! [[Pioglitazone]] (Actos)
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</td>
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! [[Rosiglitazone]] (Avandia)
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</tr>
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</table>
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|-
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! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
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! 1.8
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! 1
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! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
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! 617
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! 361
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! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
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! 83
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! 99
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! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
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! 99
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! 99
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! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 3-8
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! 3-4
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! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 6244
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! 2024
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! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
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! 360
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! 10
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! Equivalent Dosage (mg)
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! 30
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! 4
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! Metabolism
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! Hepatic <br/>(CYP2C8)
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! Hepatic <br/>(CYP2C8)
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===References===
===References===

Current revision

Pioglitazone, also known as Actos

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Pharmacokinetics

Glitazone Pharmacokinetics Comparison at Equivalent Dosages
Parameter Pioglitazone (Actos) Rosiglitazone (Avandia)
Tmax (hr) 1.8 1
Cmax (ng/ml) 617 361
Bioavailability (%) 83 99
Protein Binding (%) 99 99
T1/2 (hr) 3-8 3-4
AUC (ng/ml/hr) 6244 2024
IC50 (nM) 360 10
Equivalent Dosage (mg) 30 4
Metabolism Hepatic
(CYP2C8) 		Hepatic
(CYP2C8)

For Pharmacokinetic Data References, See: References

References

  1. ↑ http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS
  2. ↑ 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


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David Canner, Alexander Berchansky

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