نتایج جستجو برای: integrase inhibitors

تعداد نتایج: 191203  

Journal: :Journal of Antimicrobial Chemotherapy 2017

2014
Sophie M. Bastarache Thibault Mesplède Daniel A. Donahue Richard D. Sloan Mark A. Wainberg

Both the presence of latently infected cells and cell-to-cell viral transmission are means whereby HIV can partially evade the inhibitory activities of antiretroviral drugs. The clinical use of a novel integrase inhibitor, dolutegravir (DTG), has established hope that this compound may limit HIV persistence, since no treatment-naïve patient treated with DTG has yet developed resistance against ...

Journal: :Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 2008
Marian Iwamoto Larissa A Wenning Goutam C Mistry Amelia S Petry Sarah Y Liou Kaylan Ghosh Sheila Breidinger Neal Azrolan Maria J Gutierrez William E Bridson Julie A Stone Keith M Gottesdiener John A Wagner

Raltegravir is an HIV integrase inhibitor that is metabolized through glucuronidation by uridine diphosphate glucuronosyltransferase 1A1, and its use is anticipated in combination with atazanavir (a uridine diphosphate glucuronosyltransferase 1A1 inhibitor). Two pharmacokinetic studies of healthy subjects assessed the effect of multiple-dose atazanavir or ritonavir-boosted atazanavir on raltegr...

Journal: :The Journal of antimicrobial chemotherapy 2010
Carolina Garrido Vincent Soriano Carmen de Mendoza

Raltegravir (Isentress) is the first approved HIV integrase inhibitor. Agents in this class target a different viral enzyme compared with agents inhibiting reverse transcriptase and protease. A wide number of patients are currently susceptible to integrase inhibitors, including heavily antiretroviral-experienced patients harbouring drug-resistant viruses. The good tolerability and convenience o...

Journal: :The Journal of infectious diseases 2011
Filippo Canducci Elisa R Ceresola Enzo Boeri Vincenzo Spagnuolo Francesca Cossarini Antonella Castagna Adriano Lazzarin Massimo Clementi

Novel integrase inhibitors are in advanced clinical development, and cross-resistance data are needed to consider the possibility to plan a sequential usage within this class of antiretroviral drugs. Ex vivo phenotypic assays were conducted on 11 wild-type and 27 fully replicating recombinant viruses obtained from 11 patients failing previous raltegravir-containing regimens. Dolutegravir mainta...

2013
Mark A Wainberg Thibault Mesplède Francois Raffi

BACKGROUND The HIV integrase inhibitor, Dolutegravir (DTG), was recently approved by the Food and Drug Administration in the United States and is the only HIV drug that has not selected for resistance mutations in the clinic when used as part of first-line therapy. This has led to speculation that DTG might have a higher genetic barrier for the development of drug resistance than the other comp...

2010
J Eron JM Livrozet P Morlat A Lazzarin C Katlama T Hawkins T Fujiwara R Cuffe C Vavro J Santiago M Ait-Khaled S Min JM Yeo

Background S/GSK1349572(572) showed potent activity in Phase 2 studies in INI-naive HIV-infected subjects and limited cross-resistance to raltegravir (RAL) and elvitegravir in vitro. VIKING is an ongoing 24-week Phase 2b pilot study assessing 572 in subjects with RAL-resistant HIV. A good antiviral response during the functional monotherapy phase (through Day 11) of this pilot study was observe...

Journal: :Drug discovery today 2007
Nathan Ford Alexandra Calmy Tido von Schoen-Angerer

At the 2006 International AIDS Conference (http://www.aids2006.org/), an impressive range of new therapeutic developments for HIV/AIDS were described. Several new drugs, and new drug classes (entry and fusion inhibitors, integrase inhibitors, and maturation antagonists) are offering great hope for more effective treatment [1]. At the same time, however, the conference also saw unrest among trea...

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