Tipranavir: Difference between revisions

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* 2009 Sales: N/A
* 2009 Sales: N/A
* Importance: It was the ninth [[HIV Protease]] inhibitor approved by the FDA for treatment of HIV. It is a very potent inhibitor, and is often recommended for patients who have become resistant to other treatments, but also has a relatively harsh side-effect profile.  
* Importance: It was the ninth [[HIV Protease]] inhibitor approved by the FDA for treatment of HIV. It is a very potent inhibitor, and is often recommended for patients who have become resistant to other treatments, but also has a relatively harsh side-effect profile.  
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
* See [[Pharmaceutical Drugs]] for more information about other drugs and diseases.


===Mechanism of Action===
===Mechanism of Action===
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{| class="wikitable" border="1" width="52%" style="text-align:center"
{| class="wikitable" border="1" width="52%" style="text-align:center"
|-
|-
!  colspan="12" align="center"| HIV Protease Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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>
!  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>
|-
|-
! Parameter
! Parameter
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! [[Nelfinavir]]
! [[Nelfinavir]]
|-
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)  
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)  
! 4.4
! 4.4
! ~3
! ~3
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! 3.1
! 3.1
|-
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)  
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)  
! 13120
! 13120
! 14600
! 14600
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! 4701
! 4701
|-
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! --
! --
! --
! --
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! 20-80
! 20-80
|-
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! 99
! 99
! >99
! >99
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! 98
! 98
|-
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 4.8
! 4.8
! 4.2
! 4.2
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! 3.3
! 3.3
|-
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 128100
! 128100
! 46500
! 46500
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! 31906
! 31906
|-
|-
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h)
! [[Pharmacokinetics#Clearance_.28Cl.29|Clearance]] (L/h)
! ~8.4
! ~8.4
! 32.4
! 32.4

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky