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https://www.readbyqxmd.com/read/29349445/discovery-of-novel-diarylpyrimidines-as-potent-hiv-1-nnrtis-by-investigating-the-chemical-space-of-a-less-explored-hydrophobic-channel
#1
Zhongxia Zhou, Tao Liu, Dongwei Kang, Zhipeng Huo, Gaochan Wu, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu
A new series of diarylpyrimidines (DAPYs) were designed, synthesized and evaluated as novel HIV-1 NNRTIs to further explore the chemical space surrounding the "hydrophobic channel" of the NNRTI binding pocket (NNIBP), guided by the comprehensive analysis of X-ray structural biology data of HIV-1 RT/NNRTI complexes and molecular modeling. Encouragingly, most of the synthesized DAPYs were found to be active against the HIV-1 wild-type (WT) strain with EC50 values ranging from 3 nM to 63 nM, and displayed significantly reduced cytotoxicity compared with etravirine (ETV) and rilpivirine (RPV)...
January 19, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29335895/pharmacokinetics-antiviral-activity-and-safety-of-rilpivirine-in-pregnant-women-with-hiv-1-infection-results-of-a-phase-3b-multicenter-open-label-study
#2
Olayemi Osiyemi, Salih Yasin, Carmen Zorrilla, Ceyhun Bicer, Vera Hillewaert, Kimberley Brown, Herta M Crauwels
INTRODUCTION: Physiologic changes during pregnancy may impact the pharmacokinetics of drugs. In addition, efficacy and safety/tolerability concerns have been identified for some antiretroviral agents. METHODS: Human immunodeficiency virus (HIV)-1-infected pregnant women (18-26 weeks gestation) receiving the non-nucleoside reverse transcriptase inhibitor rilpivirine 25 mg once daily were enrolled in this phase 3b, open-label study examining the impact of pregnancy on the pharmacokinetics of rilpivirine when it is given in combination with other antiretroviral agents...
January 15, 2018: Infectious Diseases and Therapy
https://www.readbyqxmd.com/read/29318459/incidence-and-predictors-of-single-drug-discontinuation-according-to-the-presence-of-hcv-coinfection-in-hiv-patients-from-the-icona-foundation-cohort-study
#3
Sebastiano Leone, Milensu Shanyinde, Alessandro Cozzi Lepri, Fiona C Lampe, Pietro Caramello, Andrea Costantini, Andrea Giacometti, Andrea De Luca, Antonella Cingolani, Francesca Ceccherini Silberstein, Massimo Puoti, Andrea Gori, Antonella d'Arminio Monforte
To evaluate incidence rates of and predictors for any antiretroviral (ART) drug discontinuation by HCV infection status in a large Italian cohort of HIV infected patients. All patients enrolled in ICONA who started combination antiretroviral therapy (cART) containing abacavir or tenofovir or emtricitabine or lamivudine plus efavirenz or rilpivirine or atazanavir/r or darunavir/r (DRV/r) or lopinavir/r or dolutegravir or elvitegravir or raltegravir were included. Multivariate Poisson regression models were used to determine factors independently associated with single ART drug discontinuation...
January 9, 2018: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/29317618/development-of-an-oral-once-weekly-drug-delivery-system-for-hiv-antiretroviral-therapy
#4
Ameya R Kirtane, Omar Abouzid, Daniel Minahan, Taylor Bensel, Alison L Hill, Christian Selinger, Anna Bershteyn, Morgan Craig, Shirley S Mo, Hormoz Mazdiyasni, Cody Cleveland, Jaimie Rogner, Young-Ah Lucy Lee, Lucas Booth, Farhad Javid, Sarah J Wu, Tyler Grant, Andrew M Bellinger, Boris Nikolic, Alison Hayward, Lowell Wood, Philip A Eckhoff, Martin A Nowak, Robert Langer, Giovanni Traverso
The efficacy of antiretroviral therapy is significantly compromised by medication non-adherence. Long-acting enteral systems that can ease the burden of daily adherence have not yet been developed. Here we describe an oral dosage form composed of distinct drug-polymer matrices which achieved week-long systemic drug levels of the antiretrovirals dolutegravir, rilpivirine and cabotegravir in a pig. Simulations of viral dynamics and patient adherence patterns indicate that such systems would significantly reduce therapeutic failures and epidemiological modelling suggests that using such an intervention prophylactically could avert hundreds of thousands of new HIV cases...
January 9, 2018: Nature Communications
https://www.readbyqxmd.com/read/29310899/efficacy-safety-and-tolerability-of-dolutegravir-rilpivirine-for-the-maintenance-of-virological-suppression-in-adults-with-hiv-1-phase-3-randomised-non-inferiority-sword-1-and-sword-2-studies
#5
Josep M Llibre, Chien-Ching Hung, Cynthia Brinson, Francesco Castelli, Pierre-Marie Girard, Lesley P Kahl, Elizabeth A Blair, Kostas Angelis, Brian Wynne, Kati Vandermeulen, Mark Underwood, Kim Smith, Martin Gartland, Michael Aboud
BACKGROUND: Lifelong HIV antiretroviral therapy (ART) has prompted an interest in two-drug regimens to minimise cumulative drug exposure and toxicities. The safety, tolerability, and efficacy of dolutegravir and rilpivirine suggest potential compatibility and effectiveness as a two-drug regimen. We aimed to investigate this two-drug regimen in a phase 3 study. METHODS: We identically designed SWORD-1 and SWORD-2, which were open-label, parallel-group, multicentre, phase 3, randomised, non-inferiority studies in 12 countries evaluating efficacy and safety of once-daily dolutegravir 50 mg plus rilpivirine 25 mg versus current ART regimen (CAR)...
January 5, 2018: Lancet
https://www.readbyqxmd.com/read/29304154/experiences-with-long-acting-injectable-art-a-qualitative-study-among-plhiv-participating-in-a-phase-ii-study-of-cabotegravir-rilpivirine-latte-2-in-the-united-states-and-spain
#6
Deanna Kerrigan, Andrea Mantsios, Miguel Gorgolas, Maria-Luisa Montes, Federico Pulido, Cynthia Brinson, Jerome deVente, Gary J Richmond, Sarah W Beckham, Paige Hammond, David Margolis, Miranda Murray
Challenges with adherence to daily oral antiretroviral therapy (ART) among people living with HIV (PLHIV) have stimulated development of injectable long-acting (LA) regimens. We conducted 39 in-depth interviews with participants and providers in a Phase IIb study (LATTE-2) evaluating an injectable LA regimen in the U.S. and Spain. Interviews exploring participant and provider attitudes and experiences with LA versus oral ART were audiotaped, transcribed and analyzed using thematic content analysis. Participants described the convenience of LA injections versus daily pills and emotional benefits such as minimized potential for HIV disclosure and eliminating the "daily reminder of living with HIV...
2018: PloS One
https://www.readbyqxmd.com/read/29246084/dolutegravir-plus-rilpivirine-dual-therapy-in-treating-hiv-1-infection
#7
Amedeo F Capetti, Maria V Cossu, Laura Paladini, Giuliano Rizzardini
In industrialized countries, the HIV-infected population is aging and consequently comorbidities and polypharmacological regimens are increasing. This has led researchers to evaluate the efficacy, safety and durability of dual therapies as a switch option in subjects who have achieved stable virologic suppression to reduce toxicity and drug intake. Initially effective dual combinations relied on protease inhibitors but when dolutegravir, the first integrase inhibitor to display a high genetic barrier, became commercially available, many physicians began to use it in a variety of dual regimens even before randomized clinical trials showed non-inferiority of such regimens towards triple therapies...
December 15, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29244143/impact-of-hiv-1-minority-variants-on-the-virus-response-to-a-rilpivirine-based-first-line-regimen
#8
Stéphanie Raymond, Florence Nicot, Coralie Pallier, Pantxika Bellecave, Anne Maillard, Mary Anne Trabaud, Laurence Morand-Joubert, Audrey Rodallec, Corinne Amiel, Thomas Mourez, Laurence Bocket, Agnès Beby-Defaux, Magali Bouvier-Alias, Sidonie Lambert-Niclot, Charlotte Charpentier, Brice Malve, Audrey Mirand, Julia Dina, Hélène Le Guillou-Guillemette, Stéphanie Marque-Juillet, Anne Signori-Schmuck, Francis Barin, Ali Si-Mohamed, Véronique Avettand Fenoel, Catherine Roussel, Vincent Calvez, Karine Saune, Anne Geneviève Marcelin, Christophe Rodriguez, Diane Descamps, Jacques Izopet
Background: Minority resistant variants of HIV-1 could influence the virological response to treatment based on non-nucleoside reverse transcriptase (RT) inhibitors. Data on minority rilpivirine-resistant variants are scarce. This study used next-generation sequencing (NGS) to identify patients harbouring minority resistant variants to nucleos(t)ide and non-nucleoside RT inhibitors and to assess their influence on the virological response (VR). Methods: All the subjects, 541 HIV-1-infected patients being treated at 24 French virology laboratories, started their first line regimen containing rilpivirine between 2012 and 2015...
December 13, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29239893/switch-from-tenofovir-disoproxil-fumarate-combination-to-dolutegravir-plus-rilpivirine-improves-parameters-of-bone-health
#9
Grace A Mccomsey, Sergio Lupo, David Parks, Mónica Coronado Poggio, Joseph De Wet, Lesley P Kahl, Kostas Angelis, Brian Wynne, Kati Vandermeulen, Martin Gartland, Michael Cupo, Michael Aboud
OBJECTIVE: Bone mineral density (BMD) loss, a risk factor for osteoporosis, has been attributed to HIV infection and antiretroviral therapy (ART), including regimens containing tenofovir disoproxil fumarate. DESIGN: Study 202094 is an open-label, parallel-group, sub-study of the phase III SWORD-1 and SWORD-2 studies (ClincialTrials.gov identifier, NCT02478632). METHODS: HIV-1-infected adults with HIV-1 RNA < 50 copies per mL who received ART containing tenofovir disoproxil fumarate for ≥6 months were randomized to receive dolutegravir+rilpivirine or continue current ART regimen...
December 12, 2017: AIDS
https://www.readbyqxmd.com/read/29239232/effectiveness-of-single-and-multiple-tablet-antiretroviral-regimens-in-correctional-setting-for-treatment-experienced-hiv-patients
#10
Andrew Merker, Melissa Badowski, Thomas Chiampas, Sarah E Pérez, Mahesh Patel, Jeremy Young, Ryan Werner
Minimal information is available regarding antiretroviral prescribing patterns and outcomes for HIV patients in correctional systems. This study analyzes single- (STR) and multiple- (MTR) tablet regimen effectiveness in patients receiving HIV telemedicine care through the Illinois Department of Corrections (IDOC). This study involves a retrospective review of HIV-positive adult patients in IDOC on either an STR (efavirenz, rilpivirine, elvitegravir based) or an MTR (emtricitabine/tenofovir with atazanavir/ritonavir, darunavir/ritonavir, or raltegravir)...
January 1, 2017: Journal of Correctional Health Care
https://www.readbyqxmd.com/read/29216682/simultaneous-determination-and-validation-of-emtricitabine-rilpivirine-and-tenofovir-from-biological-samples-using-lc-and-ce-methods
#11
Mehmet Gumustas, Mehmet Gokhan Caglayan, Feyyaz Onur, Sibel A Ozkan
A combination of antiretroviral agents is frequently used in effective treatment of the Human Immunodeficiency Virus infection. In this study, two different separation methods are presented for the simultaneous determination of emtricitabine, rilpivirine, and tenofovir from raw materials and urine samples. Developed liquid chromatography and capillary electrophoresis methods were thoroughly optimized for high analytical performances. Optimization of multiple variables at the same time by performing a minimum number of experiments was achieved by the Box-Behnken design, which is an experimental design in Response Surface Methodology, in capillary electrophoresis...
December 7, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29210830/tenofovir-associated-nephrotoxicity-among-a-us-national-historical-cohort-of-hiv-infected-veterans-risk-modification-by-concomitant-antiretrovirals
#12
Joanne LaFleur, Adam P Bress, Stephen Esker, Kristin Knippenberg, Jacob Crook, Heather Nyman, Roger Bedimo, Pablo Tebas, Lisa Rosenblatt
BACKGROUND: Tenofovir disoproxil fumarate (TDF) has been associated with renal complications. The third agent in TDF-containing antiretroviral regimens may modify that risk. We compared renal adverse outcomes among treatment-naïve HIV-infected patients initiating TDF-containing regimens including efavirenz (EFV) or other agents. SETTING: This population-based historical cohort study used national Veterans Health Administration (VHA) clinical and administrative datasets to identify treatment-naïve HIV-infected veterans initiating antiretroviral therapy (ART) with TDF/emtricitabine (FTC)+EFV, rilpivirine (RPV), elvitegravir/cobicistat (EVG/c), or ritonavir (RTV)-boosted protease inhibitors (PIs) from 2003-2015...
November 27, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/29189101/pharmacokinetics-and-pharmacodynamics-of-the-nucleoside-sparing-dual-regimen-containing-rilpivirine-plus-darunavir-ritonavir-in-treatment-na%C3%A3-ve-hiv-1-infected-individuals
#13
Akil Jackson, Laura Else, Christopher Higgs, Zeenat Karolia, Saye Khoo, David Back, Emma Devitt, Anton Pozniak, Marta Boffito
BACKGROUND: We aimed at investigating the antiviral activity and the pharmacokinetics of the dual antiretroviral (ARV) combination of rilpivirine plus darunavir/ritonavir 25/800/100 mg once-daily in naïve HIV-1-infected individuals (NHII) with different baseline viral loads. SETTINGS: Pharmacokinetic/pharmacodynamics study in ARV-naïve HIV-infected individuals. METHODS: The primary endpoint was the number of NHII with HIV-RNA < 40 copies/mL at week 48...
November 30, 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/29156381/structure-based-methods-to-predict-mutational-resistance-to-diarylpyrimidine-non-nucleoside-reverse-transcriptase-inhibitors
#14
Syeda Maryam Azeem, Alecia N Muwonge, Nehaben Thakkar, Kristina W Lam, Kathleen M Frey
Resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) is a leading cause of HIV treatment failure. Often included in antiviral therapy, NNRTIs are chemically diverse compounds that bind an allosteric pocket of enzyme target reverse transcriptase (RT). Several new NNRTIs incorporate flexibility in order to compensate for lost interactions with amino acid conferring mutations in RT. Unfortunately, even successful inhibitors such as diarylpyrimidine (DAPY) inhibitor rilpivirine are affected by mutations in RT that confer resistance...
November 9, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29147636/drug-induced-lupus-erythematosus-associated-with-antiretroviral-therapy-in-a-patient-with-human-immunodeficiency-virus-a-case-report
#15
Jazila Mantis, Ravi Bhavsar, Adriana Abrudescu
Antiretroviral medications are the mainstay of human immunodeficiency virus (HIV) therapy and some have been in use for over 20 years. To date, there have been no reported cases of antiretroviral therapy (ART) induced drug-induced lupus erythematosus (DILE). We present a case of a 35-year-old woman who received a combination of emtricitabine, rilpivirine, and tenofovir disoproxil fumarate for HIV treatment. Three years later, she developed an extensive rash and polyarthralgia in her extremities with laboratory findings significant for positive antinuclear antibody (ANA), anti-double stranded deoxyribonucleic acid (DNA) antibody (anti-dsDNA), and anti-histone antibody titers...
September 7, 2017: Curēus
https://www.readbyqxmd.com/read/29145807/durability-of-switch-regimens-based-on-rilpivirine-or-on-integrase-inhibitors-both-in-association-with-tenofovir-and-emtricitabine-in-hiv-infected-virologically-suppressed-patients
#16
Nicola Gianotti, Andrea Poli, Silvia Nozza, Laura Galli, Nadia Galizzi, Marco Ripa, Marco Merli, Alessia Carbone, Vincenzo Spagnuolo, Adriano Lazzarin, Antonella Castagna
BACKGROUND: Switch strategies based on rilpivirine/tenofovir/emtricitabine or on an integrase inhibitor (InSTI) plus tenofovir/emtricitabine have never been compared in randomized clinical trials. The main aim of the study was to investigate the durability of these two switch regimens in virologically suppressed, HIV-infected patients. METHODS: Retrospective analysis of patients who started rilpivirine or an InSTI (both with tenofovir and emtricitabine) with <50 HIV-RNA copies/mL and had at least one HIV-RNA assessed while receiving the study regimen...
November 16, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/29105160/strength-in-amalgamation-newer-combination-agents-for-hiv-and-implications-for-practice
#17
Christopher McCoy, Melissa Badowski, Elizabeth Sherman, Rustin Crutchley, Ethan Smith, Daniel B Chastain
Antiretroviral (ART) therapy for treatment of human immunodeficiency virus (HIV) infection has undergone significant changes over the past 30 years. Many single tablet regimens (STR), including newer fixed dose combination (FDC) tablets, are available, offering patients several options for choosing a treatment regimen that works best for them. Given these changes, patients are more likely to adhere to treatment, achieve better clinical outcomes, and experience both fewer side effects and drug-drug interactions...
November 3, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/29098886/diaryl-ethers-with-carboxymethoxyphenacyl-motif-as-potent-hiv-1-reverse-transcriptase-inhibitors-with-improved-solubility
#18
Tomasz Frączek, Rafał Kamiński, Agnieszka Krakowiak, Evelien Naessens, Bruno Verhasselt, Piotr Paneth
In search of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) with improved solubility, two series of novel diaryl ethers with phenacyl moiety were designed and evaluated for their HIV-1 reverse transcriptase inhibition potentials. All compounds exhibited good to excellent results with IC50 at low micromolar to submicromolar concentrations. Two most active compounds (7e and 7 g) exhibit inhibitory potency comparable or even better than that of nevirapine and rilpivirine. Furthermore, SupT1 and CD4(+) cell infectivity assays for the most promising (7e) have confirmed its strong antiviral potential while docking studies indicate a novel binding interactions responsible for high activity...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29066858/rilpivirine-the-key-for-long-term-success
#19
Pompeyo Viciana
During the past 30 years of antiretroviral therapy, continuous improvements in drug discovery have provided increasingly potent and safer antivirals that have transformed HIV infection in a chronic illness, rarely fatal. Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are frequently used as part of any antiretroviral combination therapy. Side effects and low resistance barrier of fi rst-generation NNRTIs (e.g., nevirapine and efavirenz) have been overcome with rilpivirine (RPV), and the last NNRTI approved for the treatment of HIV infection...
October 2017: AIDS Reviews
https://www.readbyqxmd.com/read/29019353/hot-news-ready-for-hiv-dual-therapy-new-data-from-international-hiv-aids-society-2017
#20
George A Yendewa, Robert A Salata
The introduction of combination antiretroviral therapy (ART) in the 1990s has fundamentally transformed the landscape of HIV medicine, greatly improved disease morbidity and mortality, and reduced transmission rates across all demographic groups. Central to this success was the idea that to achieve best disease outcomes and minimize the development of drug resistance, at least three antiretroviral agents should be used for HIV treatment. This therapeutic strategy is a core tenet of HIV medicine, backed by incontrovertible scientific evidence, and made easy to deploy by the high compliance levels with once-daily coformulations, which have generally been well tolerated...
October 2017: AIDS Reviews
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