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Saquinavir

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<applet load="" size="480" color="" frame="true" spin="on" Scene ="Saquinavir/Saquinavir/1" align="right" caption="Saquinavir, better known as Invirase, ([[3d1y]])"/>
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<StructureSection load='' size='340' side='right' caption='Saquinavir, better known as Invirase, ([[3d1y]])' scene='Saquinavir/Saquinavir/1'>
===Better Known as: Invirase or Fortovase===
===Better Known as: Invirase or Fortovase===
* Marketed By: Roche<br />
* Marketed By: Roche<br />
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===Drug Resistance===
===Drug Resistance===
The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]]
The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]]
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</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
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{| class="wikitable" border="1" width="52%" style="text-align:center"
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<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">
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|-
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<tr>
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! colspan="12" align="center"| HIV Protease Inhibitor [[Pharmacokinetics]]<ref>PMID:20400409</ref><ref>Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.</ref><ref>L. Veronese et al. Single-Dose Pharmacokinetics of Amprenavir, a Human Immunodeficiency Virus Type 1 Protease Inhibitor, in Subjects with Normal or Impaired Hepatic Function. Antimicrob Agents Chemother. 2000 April; 44(4): 821–826.</ref><ref>J. Ford, et al. Intracellular and Plasma Pharmacokinetics of Saquinavir-Ritonavir, Administered at 1,600/100 Milligrams Once Daily in Human Immunodeficiency Virus-Infected Patients. Antimicrob Agents Chemother. 2004 July; 48(7): 2388–2393.</ref><ref>PMID:10620574</ref><ref>PMID:16086644</ref><ref>PMID:19131522</ref><ref>PMID: 10952482</ref><ref>PMID:16338276</ref><ref>PMID:19729375</ref><ref>PMID:12668574</ref><ref>PMID:17255144</ref><ref>PMID:10858338</ref>
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<td style="width:100%; 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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{{:HIV Protease Inhibitor Pharmacokinetics}}
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! [[Ritonavir]]
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</div>
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! [[Tipranavir]]
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</td>
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! [[Indinavir]]
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</tr>
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! [[Saquinavir]]
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</table>
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! [[Amprenavir]]
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! [[Fosamprenavir]]
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! [[Lopinavir]]
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! [[Darunavir]]
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! [[Atazanavir]]
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! [[Nelfinavir]]
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|-
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! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
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! 4.4
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! ~3
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! 1.5
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! 3.7
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! .98
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! 1.5-4
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! 2
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! .5
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! 2-4
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! 3.1
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|-
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! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
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! 13120
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! 14600
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! 8100
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! 2297
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! 4901
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! 4820
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! 11.9
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! 2730
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! ~4393
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! 4701
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|-
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! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
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! --
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! --
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! 65
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! 4
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! --
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! --
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! --
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! --
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! 68
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! 20-80
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|-
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! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
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! 99
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! >99
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! 61
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! 98
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! 90
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! 90
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! 99
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! 95
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! 86
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! 98
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|-
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! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 4.8
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! 4.2
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! 1.2
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! 4.5
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! 5.5
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! 7.7
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! 6.1
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! 29.4
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! 5.3
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! 3.3
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|-
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! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 128100
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! 46500
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! 20900
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! 13467
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! 11999
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! 35000
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! 117600
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! 4746
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! ~26045
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! 31906
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|-
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! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
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! ~8.4
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! 32.4
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! 49.5
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! 36.7
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! 56.8
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! 84.4
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! 1.7
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! 32.8
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! 13.6
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! 37.3
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|-
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! Dosage (mg)
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! 600
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! 600
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! 800
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! 1000
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! 600
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! 1400
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! 280
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! 400
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! 400
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! 1250
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|-
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! Metabolism
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! Hepatic (CYP3A4 & CYP2C19)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4 & CYP3A5)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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|}
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===References===
===References===

Current revision

Saquinavir, better known as Invirase, (3d1y)

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Pharmacokinetics

HIV Protease Inhibitor Pharmacokinetics
Parameter Ritonavir Tipranavir Indinavir Saquinavir Amprenavir Fosamprenavir Lopinavir Darunavir Atazanavir Nelfinavir
Tmax (hr) 4.4 ~3 1.5 3.7 .98 1.5-4 2 .5 2-4 3.1
Cmax (ng/ml) 13120 14600 8100 2297 4901 4820 11.9 2730 ~4393 4701
Bioavailability (%) -- -- 65 4 -- -- -- -- 68 20-80
Protein Binding (%) 99 >99 61 98 90 90 99 95 86 98
T1/2 (hr) 4.8 4.2 1.2 4.5 5.5 7.7 6.1 29.4 5.3 3.3
AUC (ng/ml/hr) 128100 46500 20900 13467 11999 35000 117600 4746 ~26045 31906
Clearance (L/h) ~8.4 32.4 49.5 36.7 56.8 84.4 1.7 32.8 13.6 37.3
Dosage (mg) 600 600 800 1000 600 1400 280 400 400 1250
Metabolism Hepatic (CYP3A4 & CYP2C19) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4 & CYP3A5) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4)

For Pharmacokinetic Data References, See: References

References

  1. ↑ Spinelli S, Liu QZ, Alzari PM, Hirel PH, Poljak RJ. The three-dimensional structure of the aspartyl protease from the HIV-1 isolate BRU. Biochimie. 1991 Nov;73(11):1391-6. PMID:1799632
  2. ↑ Tie Y, Kovalevsky AY, Boross P, Wang YF, Ghosh AK, Tozser J, Harrison RW, Weber IT. Atomic resolution crystal structures of HIV-1 protease and mutants V82A and I84V with saquinavir. Proteins. 2007 Apr 1;67(1):232-42. PMID:17243183 doi:10.1002/prot.21304


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David Canner, Alexander Berchansky

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