Elvitegravir

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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Elvitegravir/Elvitegravir/1" align="right" caption="The Investigational New Drug, Elvitegravir, ([[3l2u]])"/>
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<StructureSection load='' size='340' side='right' caption='The Investigational Drug, Elvitegravir, ([[3l2u]])' scene='Elvitegravir/Elvitegravir/1'>
===Better Known as: N/A===
===Better Known as: N/A===
* Marketed By: Gilead Sciences
* Marketed By: Gilead Sciences
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* Projected 2013 Sales: $460 Million
* Projected 2013 Sales: $460 Million
* Importance: It is expected to be the next effective HIV treatment to come to market. Expected to be the second [[Retroviral Integrase]] inhibitor approved. Currently in phase III clinical trials. Results from phase II trials indicate that the once-daily treatment was more effective than current [[HIV Protease]] inhibitor combinations.<ref>PMID:17977962</ref>
* Importance: It is expected to be the next effective HIV treatment to come to market. Expected to be the second [[Retroviral Integrase]] inhibitor approved. Currently in phase III clinical trials. Results from phase II trials indicate that the once-daily treatment was more effective than current [[HIV Protease]] inhibitor combinations.<ref>PMID:17977962</ref>
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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===
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===Pharmacokinetics===
===Pharmacokinetics===
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{| class="wikitable" border="1" width="60%" style="text-align:center"
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<table style="background: cellspacing="0px" align="" cellpadding="0px" width="50%">
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|-
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<tr>
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! colspan="4" align="center"| Retroviral Integrase Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]]<ref>A Gaur, et al. Pharmacokinetics and Safety of Once-Daily Elvitegravir in HIV-Infected Adolescents. 17th Conference on Retroviruses. Poster Number: 874.</ref><ref>doi: 10.1128/AAC.01543-07</ref>
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<td style="width:auto; vertical-align:top;border-width:0px; border-style:inset">
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|-
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<div style="height:100%; width: 100%">
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! Parameter
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{{:Retroviral Integrase Inhibitor Pharmacokinetics}}
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! [[Raltegravir]]
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</div>
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! [[Elvitegravir]]
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</td>
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! [[MK-2048]]
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</tr>
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|-
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</table>
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! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
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! 1.8
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! 2-4
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! N/A
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|-
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! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
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! 4253
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! 2070
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! N/A
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|-
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! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
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! 32
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! ~30
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! N/A
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|-
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! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
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! 83
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! N/A
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! N/A
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|-
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! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 10.8
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! 7.6
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! N/A
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|-
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! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 10168
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! 21200
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! N/A
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! Dosage (mg)
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! 400
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! 150
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! N/A
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|-
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! Metabolism
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! Hepatic - (UGT1A1)
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! Hepatic - (CYP3A4)
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! N/A
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|}
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</StructureSection>
===References===
===References===
<references/>
<references/>
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Current revision

The Investigational Drug, Elvitegravir, (3l2u)

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References

  1. ↑ Shimura K, Kodama E, Sakagami Y, Matsuzaki Y, Watanabe W, Yamataka K, Watanabe Y, Ohata Y, Doi S, Sato M, Kano M, Ikeda S, Matsuoka M. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74. Epub 2007 Oct 31. PMID:17977962 doi:10.1128/JVI.01534-07
  2. ↑ Savarino A. A historical sketch of the discovery and development of HIV-1 integrase inhibitors. Expert Opin Investig Drugs. 2006 Dec;15(12):1507-22. PMID:17107277 doi:10.1517/13543784.15.12.1507
  3. ↑ Hare S, Gupta SS, Valkov E, Engelman A, Cherepanov P. Retroviral intasome assembly and inhibition of DNA strand transfer. Nature. 2010 Mar 11;464(7286):232-6. Epub 2010 Jan 31. PMID:20118915 doi:10.1038/nature08784
  4. ↑ Hare S, Vos AM, Clayton RF, Thuring JW, Cummings MD, Cherepanov P. Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A. 2010 Oct 28. PMID:21030679 doi:10.1073/pnas.1010246107


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David Canner, Alexander Berchansky

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