HIV-1 Integrase Inhibitors: A Review of Their Chemical Development
Highly active antiretroviral therapy (HAART) significantly decreases plasma viral load, increases CD4+ T-cell counts in HIV-1-infected patients and has reduced progression to AIDS in developed countries. However, adverse side effects, and emergence of drug resistance, mean there is still a demand fo...
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| Veröffentlicht in: | Antiviral Chemistry and Chemotherapy 2011-12, Vol.22 (3), p.95-105 |
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| container_title | Antiviral Chemistry and Chemotherapy |
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| creator | Ingale, Kundan B Bhatia, Manish S |
| description | Highly active antiretroviral therapy (HAART) significantly decreases plasma viral load, increases CD4+ T-cell counts in HIV-1-infected patients and has reduced progression to AIDS in developed countries. However, adverse side effects, and emergence of drug resistance, mean there is still a demand for new anti-HIV agents. The HIV integrase (IN) is a target that has been the focus of rational drug design over the past decade. In 2007, raltegravir was the first IN inhibitor approved by the US Food and Drug Administration for antiretroviral combination therapy, while another IN inhibitor, elvitegravir, is currently in Phase III clinical trials. This article reviews the development and resistance profiling of small molecule HIV-1 IN inhibitors. |
| doi_str_mv | 10.3851/IMP1740 |
| format | Article |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection |
| subjects | Antiretroviral drugs CD4 antigen Clinical trials Drug development Drug Discovery Drug resistance Drug Resistance, Viral - drug effects Highly active antiretroviral therapy HIV HIV Infections - drug therapy HIV Infections - virology HIV Integrase - metabolism HIV Integrase Inhibitors - adverse effects HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacology Human immunodeficiency virus Humans Integrase Lymphocytes T |
| title | HIV-1 Integrase Inhibitors: A Review of Their Chemical Development |
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