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Resistance to newly approved and investigational protease inhibitors

Resistance to newly approved and investigational protease inhibitors Resistance to newly approved and investigational protease inhibitors Andrea De Luca Abbreviations Purpose of review The aim of this paper was to review recent literature on the IC 50% inhibitory concentration OBT optimized background therapy HIV-1 genotypic and phenotypic resistance determinants of therapeutic response to newly approved protease inhibitors and the viral resistance pathways to these and to 2007 Lippincott Williams & Wilkins 1746-630X investigational protease inhibitors. Recent findings Published papers and conference abstracts highlighting Introduction HIV drug resistance selection and response to tipranavir Inhibitors of HIV-1 protease have represented the and darunavir, as well as to investigational protease cornerstone of highly active antiretroviral therapy. The inhibitors brecanavir, PL-100 and SP-256, were reviewed. antiviral potency and high genetic barrier to drug resist- Tipranavir and darunavir exhibit a high genetic barrier to ance of the agents of this class, used in combination with resistance, and demonstrate significant antiviral efficacy in nucleoside reverse transcriptase inhibitors, have made a patients carrying multidrug-resistant HIV. Drugs activities major contribution to the reduction of morbidity and are affected by partly distinct patterns of resistance mortality in HIV-infected individuals [1]. mutations. Investigational agents show promising in-vitro activity against viral strains resistant to other protease Limitations of http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Current Opinion in HIV and Aids Wolters Kluwer Health

Resistance to newly approved and investigational protease inhibitors

De Luca, Andrea
Current Opinion in HIV and Aids , Volume 2 (2) – Mar 1, 2007
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ISSN
1746-630X
eISSN
1746-6318
DOI
10.1097/COH.0b013e3280287a38
pmid
19372878
Publisher site
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Abstract

Resistance to newly approved and investigational protease inhibitors Andrea De Luca Abbreviations Purpose of review The aim of this paper was to review recent literature on the IC 50% inhibitory concentration OBT optimized background therapy HIV-1 genotypic and phenotypic resistance determinants of therapeutic response to newly approved protease inhibitors and the viral resistance pathways to these and to 2007 Lippincott Williams & Wilkins 1746-630X investigational protease inhibitors. Recent findings Published papers and conference abstracts highlighting Introduction HIV drug resistance selection and response to tipranavir Inhibitors of HIV-1 protease have represented the and darunavir, as well as to investigational protease cornerstone of highly active antiretroviral therapy. The inhibitors brecanavir, PL-100 and SP-256, were reviewed. antiviral potency and high genetic barrier to drug resist- Tipranavir and darunavir exhibit a high genetic barrier to ance of the agents of this class, used in combination with resistance, and demonstrate significant antiviral efficacy in nucleoside reverse transcriptase inhibitors, have made a patients carrying multidrug-resistant HIV. Drugs activities major contribution to the reduction of morbidity and are affected by partly distinct patterns of resistance mortality in HIV-infected individuals [1]. mutations. Investigational agents show promising in-vitro activity against viral strains resistant to other protease Limitations of

Journal

Current Opinion in HIV and Aids – Wolters Kluwer Health

Published: Mar 1, 2007

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