Efficacies of Cabotegravir and Bictegravir against drug-resistant HIV-1 integrase mutants

Novel secondary mutations C56S and G149A confer resistance to HIV-1 integrase strand transfer inhibitors

(2018) Tomokazu Yoshinaga et al.   ANTIVIRAL RESEARCH

Antiviral Activity, Safety, and Pharmacokinetics of Bictegravir as 10-Day Monotherapy in HIV-1–Infected Adults

(2017) Joel E. Gallant et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Structure-Guided Optimization of HIV Integrase Strand Transfer Inhibitors

(2017) Xue Zhi Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Long-acting intramuscular cabotegravir and rilpivirine in adults with HIV-1 infection (LATTE-2): 96-week results of a randomised, open-label, phase 2b, non-inferiority trial

(2017) David A Margolis et al.   LANCET

Cryo-EM structures and atomic model of the HIV-1 strand transfer complex intasome

(2017) Dario Oliveira Passos et al.   SCIENCE

Bictegravir versus dolutegravir, each with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection: a randomised, double-blind, phase 2 trial

(2017) Paul E Sax et al.   Lancet HIV

Safety and tolerability of long-acting cabotegravir injections in HIV-uninfected men (ECLAIR): a multicentre, double-blind, randomised, placebo-controlled, phase 2a trial

(2017) Martin Markowitz et al.   Lancet HIV

HIV-1 Integrase Strand Transfer Inhibitors with Reduced Susceptibility to Drug Resistant Mutant Integrases

(2016) Xue Zhi Zhao et al.   ACS Chemical Biology

Transmitted HIV Drug Resistance Is High and Longstanding in Metropolitan Washington, DC

(2016) Seble G. Kassaye et al.   CLINICAL INFECTIOUS DISEASES

Drug resistant integrase mutants cause aberrant HIV integrations

(2016) Janani Varadarajan et al.   Retrovirology

Rilpivirine analogs potently inhibit drug-resistant HIV-1 mutants

(2016) Steven J. Smith et al.   Retrovirology

Will drug resistance against dolutegravir in initial therapy ever occur?

(2015) Mark A. Wainberg et al.   Frontiers in Pharmacology

Antiviral Characteristics of GSK1265744, an HIV Integrase Inhibitor Dosed Orally or by Long-Acting Injection

(2014) Tomokazu Yoshinaga et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Addition of E138K to R263K in HIV integrase increases resistance to dolutegravir, but fails to restore activity of the HIV integrase enzyme and viral replication capacity

(2014) T. Mesplede et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Dolutegravir in Antiretroviral-Experienced Patients With Raltegravir- and/or Elvitegravir-Resistant HIV-1: 24-Week Results of the Phase III VIKING-3 Study

(2014) A. Castagna et al.   JOURNAL OF INFECTIOUS DISEASES

4-Amino-1-hydroxy-2-oxo-1,8-naphthyridine-Containing Compounds Having High Potency against Raltegravir-Resistant Integrase Mutants of HIV-1

(2014) Xue Zhi Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bicyclic 1-Hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide-Containing HIV-1 Integrase Inhibitors Having High Antiviral Potency against Cells Harboring Raltegravir-Resistant Integrase Mutants

(2014) Xue Zhi Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naive adults with HIV-1 infection (FLAMINGO): 48 week results from the randomised open-label phase 3b study

(2014) Bonaventura Clotet et al.   LANCET

Biochemical Analysis of the Role of G118R-Linked Dolutegravir Drug Resistance Substitutions in HIV-1 Integrase

(2013) Peter K. Quashie et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

What if HIV were unable to develop resistance against a new therapeutic agent?

(2013) Mark A Wainberg et al.   BMC Medicine

Dolutegravir: First Global Approval

(2013) Anita D. Ballantyne et al.   DRUGS

Carbamoyl Pyridone HIV-1 Integrase Inhibitors 3. A Diastereomeric Approach to Chiral Nonracemic Tricyclic Ring Systems and the Discovery of Dolutegravir (S/GSK1349572) and (S/GSK1265744)

(2013) Brian A. Johns et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2013) Pedro Cahn et al.   LANCET

Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study

(2013) Francois Raffi et al.   LANCET

Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naive adults with HIV-1 infection (SPRING-2 study): 96 week results from a randomised, double-blind, non-inferiority trial

(2013) François Raffi et al.   LANCET INFECTIOUS DISEASES

Dolutegravir plus Abacavir–Lamivudine for the Treatment of HIV-1 Infection

(2013) Sharon L. Walmsley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Dolutegravir: A New Integrase Strand Transfer Inhibitor for the Treatment of HIV

(2013) Bhavik M. Shah et al.   PHARMACOTHERAPY

Treatment with suboptimal doses of raltegravir leads to aberrant HIV-1 integrations

(2013) Janani Varadarajan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Safety and Efficacy of Dolutegravir in Treatment-Experienced Subjects With Raltegravir-Resistant HIV Type 1 Infection: 24-Week Results of the VIKING Study

(2012) Joseph J. Eron et al.   JOURNAL OF INFECTIOUS DISEASES

Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks

(2012) Paul E Sax et al.   LANCET

Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of dolutegravir as 10-day monotherapy in HIV-1-infected adults

(2011) Sherene Min et al.   AIDS

MK-0536 Inhibits HIV-1 Integrases Resistant to Raltegravir

(2011) Mathieu Métifiot et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4

(2011) Nicolas A. Margot et al.   ANTIVIRAL RESEARCH

Characterization of the R263K Mutation in HIV-1 Integrase That Confers Low-Level Resistance to the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir

(2011) P. K. Quashie et al.   JOURNAL OF VIROLOGY

Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial

(2011) Joseph J Eron et al.   LANCET INFECTIOUS DISEASES

Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial

(2011) Jan van Lunzen et al.   LANCET INFECTIOUS DISEASES

Structural and Functional Analyses of the Second-Generation Integrase Strand Transfer Inhibitor Dolutegravir (S/GSK1349572)

(2011) S. Hare et al.   MOLECULAR PHARMACOLOGY

In VitroAntiretroviral Properties of S/GSK1349572, a Next-Generation HIV Integrase Inhibitor

(2010) Masanori Kobayashi et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Long‐Term Efficacy and Safety of Raltegravir Combined with Optimized Background Therapy in Treatment‐Experienced Patients with Drug‐Resistant HIV Infection: Week 96 Results of the BENCHMRK 1 and 2 Phase III Trials

(2010) Roy T. Steigbigel et al.   CLINICAL INFECTIOUS DISEASES

Retroviral intasome assembly and inhibition of DNA strand transfer

(2010) Stephen Hare et al.   NATURE

Resistance to Integrase Inhibitors

(2010) Mathieu Métifiot et al.   Viruses-Basel

Loss of Raltegravir Susceptibility by Human Immunodeficiency Virus Type 1 Is Conferred via Multiple Nonoverlapping Genetic Pathways

(2009) S. Fransen et al.   JOURNAL OF VIROLOGY

Mutations Associated with Failure of Raltegravir Treatment Affect Integrase Sensitivity to the Inhibitor In Vitro

(2008) I. Malet et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Resistance Mutations in Human Immunodeficiency Virus Type 1 Integrase Selected with Elvitegravir Confer Reduced Susceptibility to a Wide Range of Integrase Inhibitors

(2008) O. Goethals et al.   JOURNAL OF VIROLOGY

Subgroup and Resistance Analyses of Raltegravir for Resistant HIV-1 Infection

(2008) David A. Cooper et al.   NEW ENGLAND JOURNAL OF MEDICINE