Tipranavir (Aptivus; Boehringer Ingelheim) was given accelerated approval by the FDA for the treatment of HIV-1 infection in combination with other antiretroviral agents in June 2005. It is the first in a new class of non-peptidic HIV-1 protease inhibitors, and is active against HIV-1 strains that are resistant to other protease inhibitors.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 12 print issues and online access
$209.00 per year
only $17.42 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
References
Flexner, C. HIV-protease inhibitors N. Engl. J. Med. 338, 1281–1292 (1998).
De Clercq, E. Strategies in the design of antiviral drugs. Nature Rev. Drug Discov. 1, 13–25 (2002).
Turner, S. R. et al. Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. J. Med. Chem. 41, 3467–3476 (1998).
Poppe, S. M. et al. Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor. Antimicrob. Agents Chemother. 41, 1058–1063 (1997).
Chong, K. T. & Pagano, P. J. In vitro combination of PNU-140690, a human immunodeficiency virus type 1 protease inhibitor, with ritonavir against ritonavir-sensitive and -resistant clinical isolates. Antimicrob. Agents Chemother. 41, 2367–2373 (1997).
Rusconi, S. et al. Susceptibility to PNU-140690 (Tipranavir) of human immunodeficiency virus type 1 isolates derived from patients with multidrug resistance to other protease inhibitors. Antimicrob. Agents Chemother. 44, 1328–1332 (2000).
FDA labelling information [online], <http://www.fda.gov/cder/foi/label/2005/021814lbl.pdf> (2005).
Lalezari, J. P. et al. Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America. N. Engl. J. Med. 348, 2175–2185 (2003).
Lazzarin, A. et al. Efficacy of enfuvirtide in patients infected with drug-resistant HIV-1 in Europe and Australia. N. Engl. J. Med. 348, 2186–2195 (2003).
IMS Health Analysis, IMS Midas Quantum, MAT (June 2005).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Flexner, C., Bate, G. & Kirkpatrick, P. Tipranavir. Nat Rev Drug Discov 4, 955–956 (2005). https://doi.org/10.1038/nrd1907
Issue Date:
DOI: https://doi.org/10.1038/nrd1907
This article is cited by
-
Emerging principles in protease-based drug discovery
Nature Reviews Drug Discovery (2010)
