Clinical pharmacokinetic, pharmacodynamic and drug-interaction profile of the integrase inhibitor dolutegravir

ML Cottrell, T Hadzic, ADM Kashuba - Clinical pharmacokinetics, 2013 - Springer
Dolutegravir is a second-generation integrase strand transfer inhibitor (INSTI) currently
under review by the US Food and Drug Administration for marketing approval. The in vitro …

Genetic barrier to resistance for dolutegravir.

JM Llibre, F Pulido, F García, M Garcia Deltoro… - AIDS …, 2015 - search.ebscohost.com
Dolutegravir is a novel integrase strand-transfer inhibitor that displays potent in vitro activity
and a remarkably different resistance profile. Its robust pharmacokinetic/pharmacodynamic …

FUBAR: a fast, unconstrained bayesian approximation for inferring selection

B Murrell, S Moola, A Mabona, T Weighill… - Molecular biology …, 2013 - academic.oup.com
Abstract Model-based analyses of natural selection often categorize sites into a relatively
small number of site classes. Forcing each site to belong to one of these classes places …

Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non …

P Cahn, AL Pozniak, H Mingrone, A Shuldyakov… - The Lancet, 2013 - thelancet.com
Summary Background Dolutegravir (GSK1349572), a once-daily HIV integrase inhibitor, has
shown potent antiviral response and a favourable safety profile. We evaluated safety …

Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved resistance profile

M Tsiang, GS Jones, J Goldsmith… - Antimicrobial agents …, 2016 - Am Soc Microbiol
ABSTRACT Bictegravir (BIC; GS-9883), a novel, potent, once-daily, unboosted inhibitor of
HIV-1 integrase (IN), specifically targets IN strand transfer activity (50% inhibitory …

Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING Study

JJ Eron, B Clotet, J Durant, C Katlama… - The Journal of …, 2013 - academic.oup.com
Abstract Background. Dolutegravir (DTG; S/GSK1349572), a human immunodeficiency virus
type 1 (HIV-1) integrase inhibitor, has limited cross-resistance to raltegravir (RAL) and …

Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection

T Yoshinaga, M Kobayashi, T Seki, S Miki… - Antimicrobial agents …, 2015 - Am Soc Microbiol
ABSTRACT GSK1265744 is a new HIV integrase strand transfer inhibitor (INSTI)
engineered to deliver efficient antiviral activity with a once-daily, low-milligram dose that …

Integrase inhibitor resistance mechanisms and structural characteristics in antiretroviral therapy-experienced, integrase inhibitor-naive adults with HIV-1 infection …

M Underwood, J Horton, K Nangle… - Antimicrobial Agents …, 2022 - Am Soc Microbiol
At week 48 in the phase IIIb DAWNING study, the integrase strand transfer inhibitor (INSTI)
dolutegravir plus 2 nucleoside reverse transcriptase inhibitors demonstrated superiority to …

Carbamoyl pyridone HIV-1 integrase inhibitors. 2. Bi-and tricyclic derivatives result in superior antiviral and pharmacokinetic profiles

T Kawasuji, BA Johns, H Yoshida… - Journal of Medicinal …, 2013 - ACS Publications
This work is a continuation of our initial discovery of a potent monocyclic carbamoyl pyridone
human immunodeficiency virus type-1 (HIV-1) integrase inhibitor that displayed favorable …

Emergence of resistance in HIV-1 integrase with dolutegravir treatment in a pediatric population from the IMPAACT P1093 study

C Vavro, T Ruel, A Wiznia, N Montañez… - Antimicrobial agents …, 2022 - Am Soc Microbiol
ABSTRACT P1093 is a multicenter, open-label, phase I/II study of pharmacokinetics, safety,
and tolerability of dolutegravir plus an optimized background regimen in pediatric …