HIV-1 integrase strand transfer inhibitors: a review of current drugs, recent advances and drug resistance

Cabotegravir-Rilpivirine: The First Complete Long-Acting Injectable Regimen for the Treatment of HIV-1 Infection

(2021) Spencer H. Durham et al.   ANNALS OF PHARMACOTHERAPY

Efficacy and Safety of Switching to Dolutegravir/Lamivudine Fixed-Dose Two-Drug Regimen Versus Continuing a Tenofovir Alafenamide–Based Three- or Four-Drug Regimen for Maintenance of Virologic Suppression in Adults With HIV-1: Phase 3, Randomized, Non-inferiority TANGO Study

(2020) Jean van Wyk et al.   CLINICAL INFECTIOUS DISEASES

Structural basis of second-generation HIV integrase inhibitor action and viral resistance

(2020) Nicola J. Cook et al.   SCIENCE

Cabotegravir Plus Rilpivirine: First Approval

(2020) A. Markham   DRUGS

Greater Weight Gain in Treatment Naïve Persons Starting Dolutegravir-Based Antiretroviral Therapy

(2019) Kassem Bourgi et al.   CLINICAL INFECTIOUS DISEASES

Failure of Dolutegravir First-Line ART with Selection of Virus Carrying R263K and G118R

(2019) Nadine Lübke et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structural Insights on Retroviral DNA Integration: Learning from Foamy Viruses

(2019) Ga-Eun Lee et al.   Viruses-Basel

Two-drug regimens with dolutegravir plus rilpivirine or lamivudine in HIV-1 treatment-naïve, virologically-suppressed patients: latest evidences from the literature on their efficacy and safety

(2019) Valeria Cento et al.   Journal of Global Antimicrobial Resistance

Durable Efficacy of Dolutegravir Plus Lamivudine in Antiretroviral Treatment–Naive Adults With HIV-1 Infection

(2019) Pedro Cahn et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

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

(2018) Steven J. Smith et al.   Retrovirology

Comparative safety of dolutegravir-based or efavirenz-based antiretroviral treatment started during pregnancy in Botswana: an observational study

(2018) Rebecca Zash et al.   Lancet Global Health

Dolutegravir for first-line antiretroviral therapy in low-income and middle-income countries: uncertainties and opportunities for implementation and research

(2018) Jienchi Dorward et al.   Lancet HIV

Southern African HIV Clinicians Society Guidance on the use of dolutegravir in first-line antiretroviral therapy

(2018) Michelle A. Moorhouse et al.   SOUTHERN AFRICAN JOURNAL OF HIV MEDICINE

Investigational HIV integrase inhibitors in phase I and phase II clinical trials

(2017) Yingshan Han et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Dolutegravir-induced liver injury leading to sub-acute liver failure requiring transplantation: a case report and review of literature

(2017) Bo Wang et al.   INTERNATIONAL JOURNAL OF STD & AIDS

HIV drug resistance against strand transfer integrase inhibitors

(2017) Kaitlin Anstett et al.   Retrovirology

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

The benefits of integration

(2016) A. Ciuffi   CLINICAL MICROBIOLOGY AND INFECTION

Current status and prospects of HIV treatment

(2016) Tomas Cihlar et al.   Current Opinion in Virology

Comparison of Newly Assembled Full Length HIV-1 Integrase With Prototype Foamy Virus Integrase: Structure-Function Prospective

(2016) Mohammad Reza Dayer   Jundishapur Journal of Microbiology

Raltegravir: first in class HIV integrase inhibitor

(2016) Zelalem Temesgen   Therapeutics and Clinical Risk Management

Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence

(2015) Thibault Mesplède et al.   Viruses-Basel

Integrase strand transfer inhibitors in the management of HIV-positive individuals

(2014) Thibault Mesplède et al.   ANNALS OF MEDICINE

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

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

Pharmacokinetics, Safety, and Tolerability With Repeat Doses of GSK1265744 and Rilpivirine (TMC278) Long-Acting Nanosuspensions in Healthy Adults

(2014) William Spreen et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

GSK1265744 Pharmacokinetics in Plasma and Tissue After Single-Dose Long-Acting Injectable Administration in Healthy Subjects

(2014) William Spreen et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Dolutegravir in antiretroviral-naive adults with HIV-1

(2013) Hans-Jürgen Stellbrink et al.   AIDS

Clinical Pharmacokinetic, Pharmacodynamic and Drug-Interaction Profile of the Integrase Inhibitor Dolutegravir

(2013) Mackenzie L. Cottrell et al.   CLINICAL PHARMACOKINETICS

Pharmacokinetics, Safety, and Monotherapy Antiviral Activity of GSK1265744, an HIV Integrase Strand Transfer Inhibitor

(2013) W. Spreen et al.   HIV CLINICAL TRIALS

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

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 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

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

Clinical Pharmacokinetic and Pharmacodynamic Profile of the HIV Integrase Inhibitor Elvitegravir

(2011) Srinivasan Ramanathan et al.   CLINICAL PHARMACOKINETICS

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

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

Nucleoprotein Intermediates in HIV-1 DNA Integration Visualized by Atomic Force Microscopy

(2010) Svetlana Kotova et al.   JOURNAL OF MOLECULAR BIOLOGY

Dynamic Modulation of HIV-1 Integrase Structure and Function by Cellular Lens Epithelium-derived Growth Factor (LEDGF) Protein

(2008) Christopher J. McKee et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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