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Tipranavir is a protease inhibitor used to treat HIV-1 resistant to more than 1 protease inhibitor. Tipranavir is a sulfonamide-containing dyhydropyrone and a nonpeptidic protease inhibitor that targets the HIV protease.
- Mechanism
- Curator reviewed
Tipranavir (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions. Two mechanisms are suggested in regards to the potency of tipranavir: 1. Tipravanir may bind to the active site of the protease enzyme with fewer hydrogen bonds than peptidic protease inhibitors, which results in increased flexibility, allowing it to fit into the active site of the enzyme in viruses that have become resistance to other protease inhibitors. This also enables tipranavir to adjust to amino acid substitutions at the active site. 2. Tipranavir's strong hydrogen bonding interaction with the amide backbone of the protease active site Asp30 may lead to its activity against resistant viruses.
- Primary indication
- For combination antiretroviral treatment of HIV-1 infected adult patients with evidence of viral replication, who are highly treatment-experienced or have HIV-1 strains resistant to multiple protease inhibitors.Curator reviewed · 1 structured indication
- Formula / weight
- C31H33F3N2O5S · 602.664 g/mol (avg)
- First approval
- Canada, 2005 · United States, 2005 · European Union, 2022
- Brand names
- Aptivus
Resolves to
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Which drugs share a target with Tipranavir, and which of those have an active Phase 3 trial?