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Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy
Raltegravir is the first licensed compound in 2007 of the new integrase inhibitor drug class. At the dose of 400 mg twice daily, raltegravir showed a potent antiviral action in antiretroviral-naïve patients when associated with tenofovir and emtricitabine. Raltegravir was also found to be highly act...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2010
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3108740/ https://www.ncbi.nlm.nih.gov/pubmed/21694899 http://dx.doi.org/10.2147/IDR.S8673 |
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author | Charpentier, Charlotte Weiss, Laurence |
author_facet | Charpentier, Charlotte Weiss, Laurence |
author_sort | Charpentier, Charlotte |
collection | PubMed |
description | Raltegravir is the first licensed compound in 2007 of the new integrase inhibitor drug class. At the dose of 400 mg twice daily, raltegravir showed a potent antiviral action in antiretroviral-naïve patients when associated with tenofovir and emtricitabine. Raltegravir was also found to be highly active in antiretroviral-experienced patients with virological failure and displaying multiresistant virus, as shown with the BENCHMRK and ANRS 139 TRIO trials. Finally, the use of raltegravir was assessed in the context of a switch strategy in antiretroviral-experienced patients with virological success [human immunodeficiency virus type 1 (HIV-1) RNA below detection limit], highlighting the following mandatory criteria in this strategy: the nucleoside reverse transcriptase inhibitors associated with raltegravir have to be fully active. In the different studies, raltegravir had a favorable safety and tolerability profile. In the clinical situation a switch in virologically suppressed patients receiving a protease inhibitor, an improvement of the lipid profile was observed. Overall, when analyzing the Phase II and III trials together, only a few patients on raltegravir discontinued for adverse events. The development of resistance to raltegravir mainly involved three resistance mutations in integrase gene: Q148H/K/R, N155H, and Y143C/H/R. In conclusion, raltegravir improved the clinical management of HIV-1 infection both in antiretroviral-naïve and in antiretroviral-experienced patients. |
format | Online Article Text |
id | pubmed-3108740 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-31087402011-06-21 Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy Charpentier, Charlotte Weiss, Laurence Infect Drug Resist Review Raltegravir is the first licensed compound in 2007 of the new integrase inhibitor drug class. At the dose of 400 mg twice daily, raltegravir showed a potent antiviral action in antiretroviral-naïve patients when associated with tenofovir and emtricitabine. Raltegravir was also found to be highly active in antiretroviral-experienced patients with virological failure and displaying multiresistant virus, as shown with the BENCHMRK and ANRS 139 TRIO trials. Finally, the use of raltegravir was assessed in the context of a switch strategy in antiretroviral-experienced patients with virological success [human immunodeficiency virus type 1 (HIV-1) RNA below detection limit], highlighting the following mandatory criteria in this strategy: the nucleoside reverse transcriptase inhibitors associated with raltegravir have to be fully active. In the different studies, raltegravir had a favorable safety and tolerability profile. In the clinical situation a switch in virologically suppressed patients receiving a protease inhibitor, an improvement of the lipid profile was observed. Overall, when analyzing the Phase II and III trials together, only a few patients on raltegravir discontinued for adverse events. The development of resistance to raltegravir mainly involved three resistance mutations in integrase gene: Q148H/K/R, N155H, and Y143C/H/R. In conclusion, raltegravir improved the clinical management of HIV-1 infection both in antiretroviral-naïve and in antiretroviral-experienced patients. Dove Medical Press 2010-10-13 /pmc/articles/PMC3108740/ /pubmed/21694899 http://dx.doi.org/10.2147/IDR.S8673 Text en © 2010 Charpentier and Weiss, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. |
spellingShingle | Review Charpentier, Charlotte Weiss, Laurence Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title | Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title_full | Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title_fullStr | Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title_full_unstemmed | Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title_short | Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy |
title_sort | extended use of raltegravir in the treatment of hiv-1 infection: optimizing therapy |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3108740/ https://www.ncbi.nlm.nih.gov/pubmed/21694899 http://dx.doi.org/10.2147/IDR.S8673 |
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