The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance

The use of highly active antiretroviral therapy (HAART) involves combinations of drugs to achieve maximal virological response and reduce the potential for the emergence of antiviral resistance. There are two broad classes of reverse transcriptase inhibitors, the nucleoside reverse transcriptase inh...

Full description

Saved in:
Bibliographic Details
Main Author: Mark A. Wainberg
Format: Article
Language:English
Published: Wiley 2012-01-01
Series:Scientifica
Online Access:http://dx.doi.org/10.6064/2012/238278
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1832559453166108672
author Mark A. Wainberg
author_facet Mark A. Wainberg
author_sort Mark A. Wainberg
collection DOAJ
description The use of highly active antiretroviral therapy (HAART) involves combinations of drugs to achieve maximal virological response and reduce the potential for the emergence of antiviral resistance. There are two broad classes of reverse transcriptase inhibitors, the nucleoside reverse transcriptase inhibitors (NRTIs) and nonnucleoside reverse transcriptase inhibitors (NNRTIs). Since the first classes of such compounds were developed, viral resistance against them has necessitated the continuous development of novel compounds within each class. This paper considers the NRTIs and NNRTIs currently in both preclinical and clinical development or approved for second line therapy and describes the patterns of resistance associated with their use, as well as the underlying mechanisms that have been described. Due to reasons of both affordability and availability, some reverse transcriptase inhibitors with low genetic barrier are more commonly used in resource-limited settings. Their use results to the emergence of specific patterns of antiviral resistance and so may require specific actions to preserve therapeutic options for patients in such settings. More recently, the advent of integrase strand transfer inhibitors represents another major step forward toward control of HIV infection, but these compounds are also susceptible to problems of HIV drug resistance.
format Article
id doaj-art-dc4b84a1aae94405b8da22d9d12fcd4e
institution Kabale University
issn 2090-908X
language English
publishDate 2012-01-01
publisher Wiley
record_format Article
series Scientifica
spelling doaj-art-dc4b84a1aae94405b8da22d9d12fcd4e2025-02-03T01:30:01ZengWileyScientifica2090-908X2012-01-01201210.6064/2012/238278238278The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug ResistanceMark A. Wainberg0Lady Davis Institute, McGill University AIDS Centre, Jewish General Hospital, Montreal, QC, H3T 1E2, CanadaThe use of highly active antiretroviral therapy (HAART) involves combinations of drugs to achieve maximal virological response and reduce the potential for the emergence of antiviral resistance. There are two broad classes of reverse transcriptase inhibitors, the nucleoside reverse transcriptase inhibitors (NRTIs) and nonnucleoside reverse transcriptase inhibitors (NNRTIs). Since the first classes of such compounds were developed, viral resistance against them has necessitated the continuous development of novel compounds within each class. This paper considers the NRTIs and NNRTIs currently in both preclinical and clinical development or approved for second line therapy and describes the patterns of resistance associated with their use, as well as the underlying mechanisms that have been described. Due to reasons of both affordability and availability, some reverse transcriptase inhibitors with low genetic barrier are more commonly used in resource-limited settings. Their use results to the emergence of specific patterns of antiviral resistance and so may require specific actions to preserve therapeutic options for patients in such settings. More recently, the advent of integrase strand transfer inhibitors represents another major step forward toward control of HIV infection, but these compounds are also susceptible to problems of HIV drug resistance.http://dx.doi.org/10.6064/2012/238278
spellingShingle Mark A. Wainberg
The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
Scientifica
title The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
title_full The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
title_fullStr The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
title_full_unstemmed The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
title_short The Need for Development of New HIV-1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance
title_sort need for development of new hiv 1 reverse transcriptase and integrase inhibitors in the aftermath of antiviral drug resistance
url http://dx.doi.org/10.6064/2012/238278
work_keys_str_mv AT markawainberg theneedfordevelopmentofnewhiv1reversetranscriptaseandintegraseinhibitorsintheaftermathofantiviraldrugresistance
AT markawainberg needfordevelopmentofnewhiv1reversetranscriptaseandintegraseinhibitorsintheaftermathofantiviraldrugresistance