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Tipranavir (Aptivus)
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Last Update:  March 12, 2010 
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Animal Studies
 
 
Metabolism mediated drug interactions associated with ritonavir-boosted tipranavir in mice.
Li F, Wang L, Guo GL, Ma X.
Drug Metab Dispos. 2010 Jan 26
 Abstract
General Reports
 
 
Trends in uptake of recently approved antiretrovirals within a national healthcare system.
 Belperio P, Mole L, Boothroyd D, Backus L.
HIV Med. 2009 Oct 23.
 Abstract

Multidrug-experienced HIV-1-infected women demonstrated similar virological and immunological
responses to tipranavir/ritonavir compared with men.
Walmsley SL, Squires K, Weiss L, et al
AIDS. 2008 Dec 24
 Abstract
 
Health-related quality of life and tolerability in treatment-experienced HIV-1-infected patients
on tipranavir versus comparator regimens.
Huang IC, Wu AW, Finnern HW, et al
Antivir Ther. 2008;13(1):15-25
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Tipranavir: the first nonpeptidic protease inhibitor for the treatment of protease
resistance.
Luna B, Townsend MU.
Clin Ther. 2007 Nov;29(11):2309-2318.
 Abstract
 
Tipranavir exhibits different effects on opportunistic pathogenic fungi.
Cenci E, Francisci D, Belfiori B, et a l 
J Infect. 2007 Sep 29;
Abstract
 
Tipranavir: a new option for the treatment of drug-resistant HIV infection.
Temesgen Z, Feinberg J. 
Clin Infect Dis. 2007 Sep 15;45(6):761-9.
Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Steady State Disposition of the Nonpeptidic Protease Inhibitor Tipranavir When Coadministered
with Ritonavir.
 Chen L, Sabo JP, Philip E, et al   
 Antimicrob Agents Chemother. 2007 May 7;
Abstract
 
Unique Thermodynamic Response of Tipranavir to HIV-1 Protease Drug Resistance Mutations.
Muzammil S, Armstrong AA, Kang LW, et al 
J Virol. 2007 Mar 14;
 Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Tipranavir: new drug. HIV protease inhibitor. A last resort.
[No authors listed]
 Prescrire Int. 2006 Dec;15(86):217-9.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Tipranavir: A Protease Inhibitor for HIV Salvage Therapy (CE) (July/August).
Dong BJ, Cocohoba JM. 
Ann Pharmacother. 2006 Jun 20;
 Abstract
 
Tipranavir: PNU 140690, tipranavir.
[No authors listed]
Drugs R D. 2006;7(1):55-62.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Practical perspectives on the use of tipranavir in combination with other medications: lessons
learned from pharmacokinetic studies.
Boffito M, Maitland D, Pozniak A.  
J Clin Pharmacol. 2006 Feb;46(2):130-9.
Abstract
 
Tipranavir: a protease inhibitor for multi-drug resistant HIV-1.
Best B, Haubrich R.  
Expert Opin Investig Drugs. 2006 Jan;15(1):59-70.
Abstract
 
Structure elucidation and total synthesis of a unique group of trace impurities in Tipranavir
Busacca CA, Campbell S, Saha A, 
Magn Reson Chem. 2005 Sep 5;
Abstract

Tipranavir: a novel non-peptidic protease inhibitor for the treatment of HIV infection.
Mehandru S, Markowitz M.
Expert Opin Investig Drugs. 2003 Nov;12(11):1821-8.
 Abstract
   
  Tipranavir: a protease inhibitor from a new class with distinct antiviral activity.
Yeni P.
J Acquir Immune Defic Syndr. 2003 Sep;34 Suppl 1:S91-4.
 Abstract
   
  Tipranavir inhibits broadly protease inhibitor-resistant HIV-1clinical samples.
Larder BA, Hertogs K, Bloor S, et al.
AIDS 2000 Sep 8;14(13):1943-1948
 Abstract
   
  FULL TEXT ARTICLE
 Susceptibility to PNU-140690 (Tipranavir) of human immunodeficiency virus type 1 isolates
derived from patients with multidrug resistance to other protease inhibitors.  
 Rusconi S, La Seta Catamancio S, Citterio P, et al.
Antimicrob Agents Chemother 2000 May;44(5):1328-1332
Paper
Safety
 

HIV/HCV Coinfection

 
Hepatic safety of tipranavir plus ritonavir (TPV/r)-based antiretroviral combinations:
effect of hepatitis virus co-infection and pre-existing fibrosis.
Macías J, Orihuela F, Rivero A, et al
J Antimicrob Chemother. 2008 Oct 24.
Abstract
Pharmacokinetics
 
 
Steady State Disposition of the Nonpeptidic Protease Inhibitor Tipranavir When Coadministered
with Ritonavir.
Chen L, Sabo JP, Philip E, et al   
Antimicrob Agents Chemother. 2007 May 7;
Abstract

Practical perspectives on the use of tipranavir in combination with other medications: lessons learned
from pharmacokinetic studies.
Boffito M, Maitland D, Pozniak A.
 J Clin Pharmacol. 2006 Feb;46(2):130-9.
Abstract
Drug/Drug Interactions
 
 
A Phenotype-Genotype Approach to Predicting CYP450 and P-Glycoprotein Drug
Interactions With the Mixed Inhibitor/Inducer Tipranavir/Ritonavir.
Dumond JB, Vourvahis M, Rezk NL, et al 
Clin Pharmacol Ther. 2010 Feb 10
 Abstract

A WEEK IN REVIEW FEATURED REPORT
Pharmacokinetic interactions between buprenorphine/naloxone and tipranavir/ritonavir in
HIV-negative subjects chronically receiving buprenorphine/naloxone.
Bruce RD, Altice FL, Moody DE, et al
Drug Alcohol Depend. 2009 Aug 31.
 Abstract

Interaction studies of tipranavir/ritonavir (TPV/r) with clarithromycin, fluconazole and rifabutin in healthy volunteers.
la Porte C, Sabo JP, Elgadi M, Cameron DW.
Antimicrob Agents Chemother. 2008 Nov 17
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Combined tipranavir and enfuvirtide use associated with higher plasma tipranavir concentrations
but not with increased hepatotoxicity: sub-analysis from RESIST.
 Raffi F, Battegay M, Rusconi S, et al 
AIDS. 2007 Sep;21(14):1977-1980.
 Abstract
 

A WEEK-IN-REVIEW FEATURED REPORT
Unexpected drug-drug interaction between tipranavir/ritonavir and enfuvirtide.
de Requena DG, Calcagno A, Bonora S, et al
AIDS. 2006 Oct 3;20(15):1977-1979.
 Abstract
Resistance
 
 
A WEEK-IN-REVIEW FEATURED REPORT
FULL-TEXT PDF ARTICLE
 Impact of first-line protease inhibitors on predicted resistance to tipranavir in HIV-1-infected
patients with virological failure.
Hsieh SM, Chang SY, Hung CC, et al
BMC Infect Dis. 2009 Sep 14;9(1):154.
Paper

A WEEK IN REVIEW FEATURED REPORT
Reversal of major genotypic tipranavir mutations under long-term treatment with tipranavir/ritonavir itself with
very limited optimized background, during deep salvage antiretroviral therapy.
Sabbatani S, Manfredi R, Fulgaro C, Bon I.
 Curr HIV Res. 2009 May;7(3):311-3.
 Abstract

A WEEK IN REVIEW FEATURED REPORT
Tipranavir/ritonavir genotypic resistance score in protease inhibitor-experienced patients.
Marcelin AG, Masquelier B, Descamps D, et al 
Antimicrob Agents Chemother. 2008 Jul 14.
Abstract

New resistance score for tipranavir .
Poveda E
AIDS Rev. 2008 Apr-Jun;10(2):127
 Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Evidence for different susceptibility to tipranavir and darunavir in patients infected with
distinct HIV-1 subtypes.
Poveda E, de Mendoza C, Parkin N, et al 
AIDS. 2008 Mar 12;22(5):611-6.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
 Unique Thermodynamic Response of Tipranavir to HIV-1 Protease Drug Resistance Mutations.
 Muzammil S, Armstrong AA, Kang LW, et al 
J Virol. 2007 Mar 14;
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Genotypic Changes in Human Immunodeficiency Virus-1 Protease Associated with Reduced
Susceptibility and Virologic Response to the Protease Inhibitor Tipranavir.
Baxter JD, Schapiro JM, Boucher CA, et al 
J Virol. 2006 Aug 23;
 Abstract

Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic
protease inhibitor tipranavir.
 Doyon L, Tremblay S, Bourgon L, et al
 Antiviral Res. 2005 Aug 22;
 Abstract
Diagnostics
          
  Use of different inhibitory quotients to predict early virological response to Tipranavir
in antiretroviral experienced HIV patients.
Morello J, De Mendoza C, Soriano V, et al 
Antimicrob Agents Chemother. 2009 Jul 13.
Abstract
 
Clinical validation and applicability of different tipranavir/ritonavir genotypic scores in
HIV-1 protease inhibitor-experienced patients.
Saracino A, Monno L, Tartaglia A,G. 
Curr HIV Res. 2009 Jul;7(4):425-33.
 Abstract
Viral Dynamics
          
  Short Communication: Association between Tipranavir Plasma Levels and Virological Response in
HIV-Infected Patients.
Morello J, Gascó PG, Rodriguez-Novoa S, et al
AIDS Res Hum Retroviruses. 2008 Mar;24(3):389-91.
 Abstract
Efficacy
 
 
Efficacy and safety of a salvage regimen based on tipranavir, enfuvirtide and three
nucleoside analogues in HIV1 infected patients with clinical progression: 96-week
evaluation.
Sozio F, Polilli E, D Annunzio M, Falconi L, et al
 Infez Med. 2009 Dec;17(4):228-35.
 Abstract

A WEEK IN REVIEW FEATURED REPORT
Successful virological outcome in an HIV-infected individual with a three-class resistant variant
and an insertion in the protease genome with a Tipranavir based regimen.
Panagopoulos P, Paraskevis D, Antoniadou A, et al 
Ir J Med Sci. 2008 Sep 10.
 Abstract
 
Efficacy, safety and tolerability of tipranavir coadministered with ritonavir in HIV-1-infected children
and adolescents.
Salazar JC, Cahn P, Yogev R, et al
AIDS. 2008 Sep 12;22(14):1789-98.
 Abstract
 
A WEEK IN REVIEW FEATURED REPORT
Tipranavir: A Review of its Use in the Management of HIV Infection.
Orman JS, Perry CM.
Drugs. 2008;68(10):1435-63.
 Abstract
 
Treatment response to ritonavir-boosted tipranavir versus ritonavir-boosted lopinavir in HIV-1
patients with higher lopinavir mutation scores.
Walmsley SL, Cotte L, Rusconi S, et al
AIDS. 2007 Oct;21(16):2245-2248.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Tipranavir/T20-based salvage regimens highly effective and durable against HIV-1 with evidence
for genotypic predictability of response in clinical practice.
Gupta RK, Loveday C, Kalidindi U, et al 
Int J STD AIDS. 2007 Sep;18(9):630-2.
 Abstract
 
Review of tipranavir in the treatment of drug-resistant HIV.
 Streeck H, Rockstroh JK.
Ther Clin Risk Manag. 2007 Aug;3(4):641-51.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Long-Term Efficacy and Safety of Tipranavir Boosted With Ritonavir in HIV-1-Infected Patients
Failing Multiple Protease Inhibitor Regimens: 80-Week Data From a Phase 2 Study.
Markowitz M, Slater LN, Schwartz R, et al
J Acquir Immune Defic Syndr. 2007 May 31;
 
A WEEK-IN-REVIEW FEATURED REPORT
Tipranavir: a new protease inhibitor for the treatment of antiretroviral-experienced
HIV-infected patients.
de Mendoza C, Morello J, Garcia-Gasco P, et al 
Expert Opin Pharmacother. 2007 Apr;8(6):839-50.
 Abstract
 
A WEEK IN REVIEW FEATURED  REPORT
Doses of Tipranavir Boosted with Ritonavir in Treatment-Experienced HIV Type 1-Infected
Patients.
Gathe JC, Pierone G, Piliero P, et al
AIDS Res Hum Retroviruses. 2007 Jan 1;
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Ritonavir-Boosted Tipranavir Demonstrates Superior Efficacy to Ritonavir-Boosted Protease
Inhibitors in Treatment-Experienced HIV-Infected Patients: 24-Week Results of the RESIST-2
Trial.
Cahn P, Villacian J, Lazzarin A, etal 
Clin Infect Dis. 2006 Nov 15;43(10):1347-56.
 Abstract
 
A WEEK-IN-REVIEW FEATURED REPORT
Efficacy of the Protease Inhibitors Tipranavir plus Ritonavir in Treatment-Experienced Patients:
24-Week Analysis from the RESIST-1 Trial.
Gathe J, Cooper DA, Farthing C, Jayaweera D, et al
Clin Infect Dis. 2006 Nov 15;43(10):1337-46.
 Abstract
 
Durable efficacy of tipranavir-ritonavir in combination with an optimised background regimen of antiretroviral
drugs for treatment-experienced HIV-1-infected patients at 48 weeks in the Randomized Evaluation of
Strategic Intervention in multi-drug resistant patients with Tipranavir (RESIST) studies: an analysis of
combined data from two randomised open-label trials.
Hicks CB, Cahn P, Cooper DA, Walmsley SL 
Lancet. 2006 Aug 5;368(9534):466-75.
Abstract 

A 14-Day Dose-Response Study of the Efficacy, Safety, and Pharmacokinetics of the Nonpeptidic
Protease Inhibitor Tipranavir in Treatment-Naive HIV-1-Infected Patients.
McCallister S, Valdez H, Curry K,et al
J Acquir Immune Defic Syndr. 2004 Apr 20;35(4):376-382
 Abstract

Diagnostics/Monitoring
 
A liquid chromatography-tandem mass spectrometry assay for quantification of nevirapine,
indinavir, atazanavir, amprenavir, saquinavir, ritonavir, lopinavir, efavirenz, tipranavir, darunavir
and maraviroc in the plasma of patients infected with HIV.
 Martin J, Deslandes G, Dailly E, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Aug 3
 Abstract

Low trough levels of tipranavir in a combination antiretroviral therapy of tipranavir/ritonavir and tenofovir
require therapeutic drug monitoring.
Langmann P, Winzer R, Schirmer D, et al
Eur J Med Res. 2008 Oct 27;13(10):469-71.
 Abstract
 
High Performance Liquid Chromatographic Method for the Determination of HIV-1 Protease
Inhibitor Tipranavir in Plasma of Patients during Highly Active Antiretroviral Therapy.
 Langmann P, Heinz W, Klinker H, et al
 Eur J Med Res. 2008 Feb 25;13(2):52-8.
 Abstract
 
A simple and sensitive assay for determining plasma tipranavir concentration in the clinical
setting by new HPLC method.
D'Avolio A, Sciandra M, Siccardi M, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Nov 6;
 Abstract
 
Determination of Tipranavir in Human Plasma by Reverse Phase Liquid Chromatography With
UV Detection Using Photodiode Array.
Keil K, Difrancesco R, Morse GD. 
Ther Drug Monit. 2006 Aug;28(4):512-6.
 Abstract
 
Liquid chromatographic assay for the non-peptidic protease inhibitor tipranavir in plasma.
Sparidans RW, Dost F, Crommentuyn KM, et al 
Biomed Chromatogr. 2006 Jun 23;
 Abstract
 
A simple high performance liquid chromatography assay for monitoring plasma concentrations
of tipranavir in HIV infected patients.
Dailly E, Reliquet V, Victorri-Vigneau C, et al 
J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Feb 21;
 Abstract

Simultaneous quantification of the new HIV protease inhibitors atazanavir and tipranavir in
human plasma by high-performance liquid chromatography coupled with electrospray ionization
tandem mass spectrometry.
 Crommentuyn KM, Rosing H, Hillebrand MJ, et al
J Chromatogr B Analyt Technol Biomed Life Sci. 2004 May 25;804(2):359-67.
Abstract
Adverse Events
 
 
FULL-TEXT PDF ARTICLE
 Hepatic profile analyses of tipranavir in Phase II and III clinical trials.
Mikl J, Sulkowski MS, Benhamou Y, et al
BMC Infect Dis. ;9(1):203.
 Paper

A WEEK IN REVIEW FEATURED REPORT
Intracranial Hemorrhage and Liver-Associated Deaths Associated with Tipranavir/Ritonavir:
Review of Cases from the FDA's Adverse Event Reporting System.
Chan-Tack KM, Struble KA, Birnkrant DB. 
AIDS Patient Care STDS. 2008 Nov;22(11):843-50.
 Abstract
 
Effects of boosted tipranavir and lopinavir on body composition, insulin sensitivity and
adipocytokines in antiretroviral-naive adults.
Carr A, Ritzhaupt A, Zhang W, et al
AIDS. 2008 Nov 12;22(17):2313-2321
 Abstract
 
Drug toxicity, HIV progression, or comorbidity of aging: does tipranavir use increase the risk of
intracranial hemorrhage?
Justice AC, Zingmond DS, Gordon KS, et al 
Clin Infect Dis. 2008 Nov 1;47(9):1226-30.
 Abstract

Intracranial haemorrhage possibly related to Tipranavir in an HIV-1 patient with cryptococcal meningitis.
Chrysos G, Gerakari S, Stasini F, et al
 J Infect. 2008 Feb 29
 Abstract
Therapeutic Strategies
 
 
The Benefit of Simplification From Tipranavir/Ritonavir 500/200 bid to 500/100 bid
Guided by Therapeutic Drug Monitoring.
Morello J, Rodríguez-Novoa S, Blanco F,  et al
Ther Drug Monit. 2010 Mar 4
 Abstract

Efficacy and safety of a salvage regimen based on tipranavir, enfuvirtide and three nucleoside
analogues in HIV1 infected patients with clinical progression: 96-week evaluation.
Sozio F, Polilli E, D Annunzio M,  et al
Infez Med. 2009 Dec;17(4):228-35.
 Abstract
Economics
 
 
Cost-effectiveness of Tipranavir in Treatment-Experienced HIV Patients in the United States.
Simpson KN, Roberts G, Hicks CB, Finnern HW.
HIV Clin Trials. 2008 Jul-Aug;9(4):225-37.
 Abstract

FULL TEXT PDF ARTICLE
 Cost-effectiveness of tipranavir versus comparator protease inhibitor regimens in HIV infected
patients previously exposed to antiretroviral therapy in the Netherlands.
Hubben GA, Bos JM, Veltman-Starkenburg CA,et al 
Cost Eff Resour Alloc. 2007 Nov 22;5(1):15
Paper

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