Tipranavir (TPV) is a nonpeptidic protease inhibitor with potent in vitro activity against most HIV-1 strains resistant to other protease inhibitors. In vitro data have shown that resistance to TPV develops slowly. When coadministered with ritonavir (RTV) as a booster, TPV has shown potent antiviral activity in multiple antiretroviral-experienced patients. In the RESIST-1 and RESIST-2 studies, the efficacy and safety of TPV/RTV (500/200 mg twice daily) in highly treatment-experienced HIV-1-positive patients was assessed. Analysis at 48 weeks showed that TPV/RTV-containing regimens significantly improved immune and virological responses compared with a RTV-boosted comparator protease inhibitor plus optimized background regimen. TPV is generally well tolerated; nevertheless, clinical hepatitis and liver decompensation have been associated to its use, together with an indication of an increased risk of intracranial hemorrhage. Extensive listing of drug-drug interactions have been reported with TPV.
Tipranavir : a novel protease inhibitor for HIV therapy / S. Rusconi. - In: EXPERT REVIEW OF CLINICAL PHARMACOLOGY. - ISSN 1751-2433. - 2:2(2009), pp. 147-153. [10.1586/17512433.2.2.147]
Tipranavir : a novel protease inhibitor for HIV therapy
S. RusconiPrimo
2009
Abstract
Tipranavir (TPV) is a nonpeptidic protease inhibitor with potent in vitro activity against most HIV-1 strains resistant to other protease inhibitors. In vitro data have shown that resistance to TPV develops slowly. When coadministered with ritonavir (RTV) as a booster, TPV has shown potent antiviral activity in multiple antiretroviral-experienced patients. In the RESIST-1 and RESIST-2 studies, the efficacy and safety of TPV/RTV (500/200 mg twice daily) in highly treatment-experienced HIV-1-positive patients was assessed. Analysis at 48 weeks showed that TPV/RTV-containing regimens significantly improved immune and virological responses compared with a RTV-boosted comparator protease inhibitor plus optimized background regimen. TPV is generally well tolerated; nevertheless, clinical hepatitis and liver decompensation have been associated to its use, together with an indication of an increased risk of intracranial hemorrhage. Extensive listing of drug-drug interactions have been reported with TPV.Pubblicazioni consigliate
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