Bictegravir in a fixed-dose tablet with emtricitabine and tenofovir alafenamide for the treatment of HIV infection: pharmacology and clinical implications

Coformulated bictegravir, emtricitabine, tenofovir alafenamide after initial treatment with bictegravir or dolutegravir and emtricitabine/tenofovir alafenamide

(2018) Paul E. Sax et al.   AIDS

HIV-1 integrase inhibitors that are broadly effective against drug-resistant mutants

(2018) Steven J. Smith et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Bictegravir: First Global Approval

(2018) Anthony Markham   DRUGS

Cabotegravir in the treatment and prevention of Human Immunodeficiency Virus-1

(2018) Tristan D. McPherson et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Where are we with injectables against HIV infection and what are the remaining challenges?

(2018) Said A. Hassounah et al.   Expert Review of Anti-Infective Therapy

Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals

(2018) Rebecca Begley et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Dolutegravir (DTG)-containing regimens after receiving raltegravir (RAL) or elvitegravir (EVG): Durability and virological response in a large Italian HIV drug resistance network (ARCA)

(2018) S. Rusconi et al.   JOURNAL OF CLINICAL VIROLOGY

HIV-1 Resistance Dynamics in Patients With Virologic Failure to Dolutegravir Maintenance Monotherapy

(2018) Ingeborg E A Wijting et al.   JOURNAL OF INFECTIOUS DISEASES

Accumulation of multiple mutations in vivo confers cross-resistance to new and existing integrase inhibitors

(2018) Wendy W Zhang et al.   JOURNAL OF INFECTIOUS DISEASES

The S230R Integrase Substitution Associated With Virus Load Rebound During Dolutegravir Monotherapy Confers Low-Level Resistance to Integrase Strand-Transfer Inhibitors

(2018) Hanh T Pham et al.   JOURNAL OF INFECTIOUS DISEASES

HIV-1 drug resistance before initiation or re-initiation of first-line antiretroviral therapy in low-income and middle-income countries: a systematic review and meta-regression analysis

(2018) Ravindra K Gupta et al.   LANCET INFECTIOUS DISEASES

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

(2018) Steven J. Smith et al.   Retrovirology

Creation of a long-acting nanoformulated dolutegravir

(2018) Brady Sillman et al.   Nature Communications

Fostemsavir

(2018) Pedro Cahn et al.   Current Opinion in HIV and AIDS

Cabotegravir

(2018) Hans-Jürgen Stellbrink et al.   Current Opinion in HIV and AIDS

Analyses of HIV-1 integrase sequences prior to South African national HIV-treatment program and availability of integrase inhibitors in Cape Town, South Africa

(2018) Dominik Brado et al.   Scientific Reports

Switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from dolutegravir plus abacavir and lamivudine in virologically suppressed adults with HIV-1: 48 week results of a randomised, double-blind, multicentre, active-controlled, phase 3, non-inferiority trial

(2018) Jean-Michel Molina et al.   Lancet HIV

Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentre, phase 3, non-inferiority trial

(2018) Eric S Daar et al.   Lancet HIV

Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults

(2018) Michael S. Saag et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Neural-Tube Defects with Dolutegravir Treatment from the Time of Conception

(2018) Rebecca Zash et al.   NEW ENGLAND JOURNAL OF MEDICINE

Ibalizumab in Multidrug-Resistant HIV — Accepting Uncertainty

(2018) Virginia Sheikh et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2018) Maureen Oliveira et al.   Retrovirology

Development and validation of LC-MS/MS method for quantification of bictegravir in human plasma and its application to an intracellular uptake study

(2018) Pavan Kumar Prathipati et al.   BIOMEDICAL CHROMATOGRAPHY

LB4. A Phase 3, Randomized, Controlled Clinical Trial of Bictegravir in a Fixed-Dose Combination, B/F/TAF, vs. ABC/DTG/3TC in Treatment-Naïve Adults at Week 96

(2018) David A Wohl et al.   Open Forum Infectious Diseases

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

Dolutegravir reshapes the genetic diversity of HIV-1 reservoirs

(2017) Pierre Gantner et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

HIV-1 strains belonging to large phylogenetic clusters show accelerated escape from integrase inhibitors in cell culture compared with viral isolates from singleton/small clusters

(2017) Bluma G. Brenner et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

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

Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380–1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial

(2017) Paul E Sax et al.   LANCET

Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3, randomised controlled non-inferiority trial

(2017) Joel Gallant et al.   LANCET

HIV drug resistance against strand transfer integrase inhibitors

(2017) Kaitlin Anstett et al.   Retrovirology

Dolutegravir as maintenance monotherapy for HIV (DOMONO): a phase 2, randomised non-inferiority trial

(2017) Ingeborg Wijting et al.   Lancet HIV

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

Lack of Clinically Relevant Effect of Bictegravir (BIC, B) on Metformin (MET) Pharmacokinetics (PK) and Pharmacodynamics (PD)

(2017) Joseph Custodio et al.   Open Forum Infectious Diseases

Tenofovir Alafenamide

(2016) Amanda K. Gibson et al.   ANNALS OF PHARMACOTHERAPY

Effect of dolutegravir functional monotherapy on HIV-1 virological response in integrase strand transfer inhibitor resistant patients

(2016) Lisa K Naeger et al.   ANTIVIRAL THERAPY

Dolutegravir as monotherapy in HIV-1-infected individuals with suppressed HIV viraemia

(2016) C. Katlama et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

The R263K substitution in HIV-1 subtype C is more deleterious for integrase enzymatic function and viral replication than in subtype B

(2015) Thibault Mesplède et al.   AIDS

Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors

(2015) Gabriel Birkus et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Twenty-eight day safety, antiviral activity, and pharmacokinetics of tenofovir alafenamide for treatment of chronic hepatitis B infection

(2015) Kosh Agarwal et al.   JOURNAL OF HEPATOLOGY

Dolutegravir Resistance Mutation R263K Cannot Coexist in Combination with Many Classical Integrase Inhibitor Resistance Substitutions

(2015) Kaitlin Anstett et al.   JOURNAL OF VIROLOGY

Formulation and pharmacology of long-acting cabotegravir

(2015) Christine Trezza et al.   Current Opinion in HIV and AIDS

Extremely High Mutation Rate of HIV-1 In Vivo

(2015) José M. Cuevas et al.   PLOS BIOLOGY

Dolutegravir versus placebo in subjects harbouring HIV-1 with integrase inhibitor resistance associated substitutions: 48-week results from VIKING-4, a randomized study

(2014) Bisher Akil et al.   ANTIVIRAL THERAPY

Tenofovir Alafenamide Vs. Tenofovir Disoproxil Fumarate in Single Tablet Regimens for Initial HIV-1 Therapy

(2014) Paul E. Sax et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

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

Resistance to HIV Integrase Strand Transfer Inhibitors Among Clinical Specimens in the United States, 2009–2012

(2013) Christopher B. Hurt et al.   CLINICAL INFECTIOUS DISEASES

A Randomized Double-Blind Comparison of Coformulated Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate Versus Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate for Initial Treatment of HIV-1 Infection

(2013) Andrew Zolopa et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

A Randomized, Double-Blind Comparison of Coformulated Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF vs Ritonavir-Boosted Atazanavir Plus Coformulated Emtricitabine and Tenofovir DF for Initial Treatment of HIV-1 Infection

(2013) Jürgen K. Rockstroh et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

A Randomized Phase 3 Study Comparing Once-Daily Elvitegravir With Twice-Daily Raltegravir in Treatment-Experienced Subjects With HIV-1 infection

(2013) Richard Elion et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

A Randomized, Double-Blind Comparison of Single-Tablet Regimen Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF Versus Single-Tablet Regimen Efavirenz/Emtricitabine/Tenofovir DF for Initial Treatment of HIV-1 Infection

(2013) David A. Wohl et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

A Randomized, Double-blind Comparison of Single-Tablet Regimen Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF vs Ritonavir-Boosted Atazanavir Plus Emtricitabine/Tenofovir DF for Initial Treatment of HIV-1 Infection

(2013) Nathan Clumeck et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

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 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

Clinical Use of HIV Integrase Inhibitors: A Systematic Review and Meta-Analysis

(2013) Peter Messiaen et al.   PLoS One

Broad Phenotypic Cross-Resistance to Elvitegravir in HIV-Infected Patients Failing on Raltegravir-Containing Regimens

(2012) Carolina Garrido et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

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

Substitutions at Amino Acid Positions 143, 148, and 155 of HIV-1 Integrase Define Distinct Genetic Barriers to Raltegravir Resistance In Vivo

(2012) S. Fransen et al.   JOURNAL OF VIROLOGY

Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143

(2011) Mathieu Métifiot et al.   AIDS

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

Natural Polymorphisms of integrase Among HIV Type 1-Infected South African Patients

(2010) Muhammad Q. Fish et al.   AIDS RESEARCH AND HUMAN RETROVIRUSES

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

Activity of Elvitegravir, a Once‐Daily Integrase Inhibitor, against Resistant HIV Type 1: Results of a Phase 2, Randomized, Controlled, Dose‐Ranging Clinical Trial

(2010) Andrew R. Zolopa et al.   JOURNAL OF INFECTIOUS DISEASES

Nature, Position, and Frequency of Mutations Made in a Single Cycle of HIV-1 Replication

(2010) M. E. Abram et al.   JOURNAL OF VIROLOGY

Raltegravir: The First HIV Type 1 Integrase Inhibitor

(2009) Charles Hicks et al.   CLINICAL INFECTIOUS DISEASES

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

Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection

(2008) Vincenzo Summa et al.   JOURNAL OF MEDICINAL CHEMISTRY