Nonnucleoside Reverse Transcriptase Inhibitor Resistance and the Role of the Second-Generation Agents

2010 ◽  
Vol 44 (1) ◽  
pp. 157-165 ◽  
Author(s):  
Jessica Adams ◽  
Nimish Patel ◽  
Nancy Mankaryous ◽  
Mariam Tadros ◽  
Christopher D Miller
Keyword(s):  
Reverse Transcriptase ◽  
Second Generation ◽  
Transcriptase Inhibitor ◽  
Nonnucleoside Reverse Transcriptase Inhibitor ◽  
Inhibitor Resistance ◽  
Reverse Transcriptase Inhibitor

scholarly journals High nonnucleoside reverse transcriptase inhibitor resistance levels in HIV-1-infected Zambian mother–infant pairs

AIDS ◽  
2020 ◽  
Vol 34 (12) ◽  
pp. 1833-1842
Author(s):  
Sydney J. Bennett ◽  
Catherine Chunda-Liyoka ◽  
Lisa K. Poppe ◽  
Katie Meinders ◽  
Chisanga Chileshe ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Nonnucleoside Reverse Transcriptase Inhibitor ◽  
Inhibitor Resistance ◽  
Reverse Transcriptase Inhibitor ◽  
Hiv 1

scholarly journals Association of Virologic Failure and Nonnucleoside Reverse Transcriptase Inhibitor Resistance Found in Antiretroviral-Naive Children Infected With Human Immunodeficiency Virus and Given Efavirenz-Based Treatment

2019 ◽  
Vol 9 (2) ◽  
pp. 261-264
Author(s):  
Nikki Higa ◽  
Amy Pelz ◽  
Donald Birch ◽  
Ingrid A Beck ◽  
Tatiana Sils ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Reverse Transcriptase ◽  
Nucleoside Reverse Transcriptase Inhibitor ◽  
Virologic Failure ◽  
Transcriptase Inhibitor ◽  
Nnrti Resistance ◽  
Nonnucleoside Reverse Transcriptase Inhibitor ◽  
Immunodeficiency Virus ◽  
Inhibitor Resistance ◽  
Reverse Transcriptase Inhibitor

Abstract Among 66 antiretroviral-naive children aged <3 years with human immunodeficiency virus (HIV) or coinfected with HIV and tuberculosis and initiating efavirenz-based antiretroviral therapy (ART), non–nucleoside reverse transcriptase inhibitor (NNRTI) resistance was detected before ART in 5 (7.6%). Virologic failure occurred in 2 of these children; they were last tested at 16 and 24 weeks of ART. Pre-ART NNRTI resistance was not associated with virologic failure.

scholarly journals Pharmacokinetic and Safety Evaluation of BILR 355, a Second-Generation Nonnucleoside Reverse Transcriptase Inhibitor, in Healthy Volunteers

2008 ◽  
Vol 52 (12) ◽  
pp. 4300-4307 ◽  
Author(s):  
Fenglei Huang ◽  
Michael Koenen-Bergmann ◽  
Thomas R. MacGregor ◽  
Arne Ring ◽  
Susan Hattox ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Healthy Volunteers ◽  
Maximum Concentration ◽  
Second Generation ◽  
Dose Range ◽  
Transcriptase Inhibitor ◽  
Time Curve ◽  
Nonnucleoside Reverse Transcriptase Inhibitor ◽  
The Mean ◽  
Reverse Transcriptase Inhibitor

ABSTRACT BILR 355 is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) under clinical development for the treatment of human immunodeficiency virus infection, particularly in those who harbor virus resistant to the currently available NNRTIs. Two single-center, double-blinded, placebo-controlled, parallel dose-escalation studies were conducted to evaluate the pharmacokinetics and safety of oral BILR 355 administration alone and after coadministration with ritonavir (RTV) at 100 mg. Following a single dose of BILR 355 in oral solution, the mean half life (t 1/2) was 2 to 4 h, with peak concentrations occurring at 0.5 to 1 h postadministration. The mean apparent clearance (CL/F) ranged from 79.2 to 246 liters/h for administered doses of 12.5 mg to 100 mg. This observed nonlinearity in CL/F resulted from the increased bioavailability attributed to a saturated absorption and/or elimination process at higher doses. In contrast, after the coadministration of single doses of 5 mg to 87.5 mg of BILR 355 with RTV, the mean CL/F ranged from 5.88 to 8.47 liters/h. Over the dose range (5 to 87.5 mg) studied, systemic BILR 355 exposures were approximately proportional to the doses administered when they were coadministered with RTV. With RTV coadministration, the mean t 1/2 increased to 10 to 16 h, and the mean time of the maximum concentration in plasma lengthened to 1.5 to 5 h. Compared to the values for BILR 355 given alone, the mean area under the concentration-time curve from time zero to infinity, the maximum concentration in plasma, and the t 1/2 of BILR 355 achieved after coadministration with RTV increased 15- to 30-fold, 2- to 5-fold, and 3- to 5-fold, respectively. In both studies, BILR 355 appeared to be safe and well tolerated in healthy volunteers when the outcomes in the treated volunteers were compared with those in the placebo group.

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