Bictegravir/emtricitabine/tenofovir alafenamide: a review in HIV-1 infection

ED Deeks - Drugs, 2018 - Springer
Bictegravir is a new integrase strand transfer inhibitor (INSTI) with a high genetic barrier to
the development of HIV-1 resistance. The drug is co-formulated with the nucleos (t) ide …

Long-acting injectable cabotegravir for HIV prevention: what do we know and need to know about the risks and consequences of cabotegravir resistance?

UM Parikh, CA Koss, JW Mellors - Current HIV/AIDS Reports, 2022 - Springer
Abstract Purpose of Review Cabotegravir is a potent integrase strand transfer inhibitor
(INSTI) recently approved as a long-acting injectable formulation for HIV prevention (CAB …

Selective resistance profiles emerging in patient-derived clinical isolates with cabotegravir, bictegravir, dolutegravir, and elvitegravir

M Oliveira, RI Ibanescu, K Anstett, T Mésplède… - Retrovirology, 2018 - Springer
Background Integrase strand transfer inhibitors (INSTIs) are recommended for first-line HIV
therapy based on their relatively high genetic barrier to resistance. Although raltegravir …

Efficacies of cabotegravir and bictegravir against drug-resistant HIV-1 integrase mutants

SJ Smith, XZ Zhao, TR Burke, SH Hughes - Retrovirology, 2018 - Springer
Background Integrase strand transfer inhibitors (INSTIs) are the class of antiretroviral (ARV)
drugs most recently approved by the FDA for the treatment of HIV-1 infections. INSTIs block …

Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir

N Gautam, JEM McMillan, D Kumar, AN Bade… - Nature …, 2021 - nature.com
A once every eight-week cabotegravir (CAB) long-acting parenteral is more effective than
daily oral emtricitabine and tenofovir disoproxil fumarate in preventing human …

Mechanisms underlying of antiretroviral drugs in different cellular reservoirs with a focus on macrophages

S Aquaro, A Borrajo, M Pellegrino, V Svicher - Virulence, 2020 - Taylor & Francis
Ongoing with current combinations of antiretroviral drugs for the treatment of Human
Immunodeficiency Virus (HIV) infection can successfully maintain long-term suppression of …

Long dissociation of bictegravir from HIV-1 integrase-DNA complexes

KL White, N Osman, E Cuadra-Foy… - Antimicrobial Agents …, 2021 - Am Soc Microbiol
The HIV integrase (IN) strand transfer inhibitor (INSTI) bictegravir (BIC) has a long
dissociation half-life (t 1/2) from wild-type IN-DNA complexes: BIC 163 h> dolutegravir (DTG) …

Pharmacokinetics and pharmacodynamics of cabotegravir, a long-acting HIV integrase strand transfer inhibitor

D Cattaneo, C Gervasoni - European journal of drug metabolism and …, 2019 - Springer
Available antiretroviral drugs have demonstrated effectiveness in both pre-exposure
prophylaxis and treatment of HIV infection. However, some concerns still persist regarding …

Genetic features of HIV-1 integrase sub-subtype A6 predominant in Russia and predicted susceptibility to INSTIs

A Kirichenko, I Lapovok, P Baryshev… - Viruses, 2020 - mdpi.com
The increasing use of the integrase strand transfer inhibitor (INSTI) class for the treatment of
HIV-infection has pointed to the importance of analyzing the features of HIV-1 subtypes for …

Pretreatment drug resistance in a large countrywide Ethiopian HIV-1C cohort: a comparison of Sanger and high-throughput sequencing

NF Telele, AW Kalu, S Gebre-Selassie, D Fekade… - Scientific reports, 2018 - nature.com
Baseline plasma samples of 490 randomly selected antiretroviral therapy (ART) naïve
patients from seven hospitals participating in the first nationwide Ethiopian HIV-1 cohort …