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https://www.readbyqxmd.com/read/28441177/right-hip-and-bilateral-shoulder-capsulitis-in-an-hiv-infected-individual-treated-with-elvitegravir-and-cobicistat
#1
Omar Al Tabaa, Victor Audren, Emma Hayton, Edouard Pertuiset, Laurent Blum
No abstract text is available yet for this article.
May 15, 2017: AIDS
https://www.readbyqxmd.com/read/28397245/interactions-between-integrase-inhibitors-and-human-arginase-1
#2
Lucia Lisi, Michela Pizzoferrato, Fabiola Teresa Miscioscia, Alessandra Topai, Pierluigi Navarra
The neuro-pathogenic mechanism(s) underlying HIV-associated neurocognitive disorders are mostly unknown. HIV-infected macrophages and microglial cells play a crucial role and the metabolic fate of L-arginine may be highly relevant for microglia activation. In this context Arginase (ARG), which uses L-arginine as substrate, can be on the same time a target and source of oxidative stress and inflammation. In the present study, we investigated whether Integrase Strand Transfer Inhibitors (INSTIs) share with the other antiretroviral drugs the ability to inhibit ARG activity...
April 11, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28375875/emergent-drug-resistance-with-integrase-strand-transfer-inhibitor-based-regimens-incidence-and-risk-factors
#3
Katherine J Lepik, P Richard Harrigan, Benita Yip, Lu Wang, Marjorie A Robbins, Wendy W Zhang, Junine Toy, Linda Akagi, Viviane Dias Lima, Silvia Guillemi, Julio S G Montaner, Rolando Barrios
OBJECTIVES: To estimate the incidence of and risk factors for emergent resistance to integrase inhibitors (INSTI) and nucleoside(-tide) reverse transcriptase inhibitors (NRTI) in HIV-1-infected adults receiving an INSTI plus two NRTIs. DESIGN: Retrospective cohort study. METHODS: Persons ≥19 years were included if they received their first prescription for raltegravir, elvitegravir or dolutegravir in British Columbia, Canada in 2012-2014, and were followed to 31-Dec-2015...
April 3, 2017: AIDS
https://www.readbyqxmd.com/read/28356041/recent-advances-in-antiretroviral-agents-potent-integrase-inhibitors
#4
Mina Psichogiou, Garyphalia Poulakou, Dimitrios Basoulis, Dimitrios Paraskevis, Antonios Markogiannakis, George L Daikos
Integrase strand transfer inhibitors (INSTIs) belong to a novel class of antiretroviral agents that have emerged as the new first-line treatments. Three such compounds are currently available, raltegravir, elvitegravir, dolutegravir and two more under development, bictegravir and cabotegravir. These compounds share the same mode of action but exhibit different pharmacokinetic/ pharmacodynamic properties, and drug-drug interactions. A series of studies in the past decade have established their efficacy compared to previous regimens, both in treatment-naïve and experienced patients...
March 29, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28351160/extensive-bruising-and-elevated-rivaroxaban-plasma-concentration-in-a-patient-receiving-cobicistat-boosted-elvitegravir
#5
Deborah Yoong, Mark Naccarato, Kevin Gough
No abstract text is available yet for this article.
March 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28348149/pharmacokinetics-and-placental-transfer-of-elvitegravir-and-dolutegravir-and-other-antiretrovirals-during-pregnancy
#6
Bassam H Rimawi, Erica Johnson, Augustine Rajakumar, Sijia Tao, Yong Jiang, Scott Gillespie, Raymond F Schinazi, Mark Mirochnick, Martina L Badell, Rana Chakraborty
The integrase inhibitors, elvitegravir (EVG) and dolutegravir (DTG), rapidly decrease plasma HIV-1 viral load, a key factor in the prevention of maternal-to-fetal transmission of HIV-1. No data have been reported on the concentration of these drugs in cord blood, maternal peripheral blood mononuclear cells (PBMC) concentrations or placental tissue in pregnant women. We present in vivo pharmacokinetic data on antiretrovirals (ARV) within maternal and cord blood, and within placentae from HIV-1-infected pregnant women...
March 27, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28333303/efficacy-of-elvitegravir-cobicistat-emtricitabine-tenofovir-disoproxil-fumarate-as-treatment-for-primary-or-recent-hiv-infection-authors-response
#7
Silvia Nozza, Andrea Poli, Marco Ripa, Laura Galli, Stefania Chiappetta, Vincenzo Spagnuolo, Cristina Rovelli, Adriano Lazzarin, Antonella Castagna, Giuseppe Tambussi
No abstract text is available yet for this article.
March 14, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28333231/tolerability-of-integrase-inhibitors-in-a-real-life-setting
#8
Judit Peñafiel, Elisa de Lazzari, Mireia Padilla, Jhon Rojas, Ana Gonzalez-Cordon, Jose L Blanco, Jordi Blanch, Maria A Marcos, Montserrat Lonca, Maria Martinez-Rebollar, Montserrat Laguno, Amparo Tricas, Ana Rodriguez, Josep Mallolas, Jose M Gatell, Esteban Martinez
Background: Integrase inhibitors have shown better tolerability than other drugs in clinical trials, but some post-marketing data have suggested potential differences among them. Aims: We compared rates and reasons for discontinuation of raltegravir-, elvitegravir- and dolutegravir-based regimens in a large cohort of HIV-infected patients. Methods: Retrospective analysis of a prospectively followed cohort including all antiretroviral-naive and all virologically suppressed antiretroviral-experienced patients prescribed a first regimen containing raltegravir, elvitegravir or dolutegravir with at least one follow-up visit...
February 28, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28282300/a-randomized-double-blind-comparison-of-tenofovir-alafenamide-taf-vs-tenofovir-disoproxil-fumarate-tdf-each-coformulated-with-elvitegravir-cobicistat-and-emtricitabine-e-c-f-for-initial-hiv-1-treatment-week-144-results
#9
José R Arribas, Melanie Thompson, Paul E Sax, Bernhard Haas, Cheryl McDonald, David A Wohl, Edwin DeJesus, Amanda E Clarke, Susan Guo, Hui Wang, Christian Callebaut, Andrew Plummer, Andrew Cheng, Moupali Das, Scott McCallister
In two double-blind Phase 3 trials, 1733 antiretroviral-naïve adults were randomized to tenofovir alafenamide (TAF) or tenofovir disoproxil fumarate (TDF), each coformulated with elvitegravir/cobicistat/emtricitabine (E/C/F). At 144 weeks, TAF was superior to TDF in virologic efficacy, with 84.2% vs. 80.0% having HIV-1 RNA <50 copies/mL (difference 4.2%; 95%CI 0.6% to 7.8%). TAF had less impact than TDF on bone mineral density and renal biomarkers. No participants on TAF had renal-related discontinuations vs 12 on TDF (P<0...
March 9, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28231276/alterations-in-cellular-pharmacokinetics-and-pharmacodynamics-of-elvitegravir-in-response-to-ethanol-exposure-in-hiv-1-infected-monocytic-u1-cells
#10
Narasimha M Midde, Namita Sinha, Pradeep B Lukka, Bernd Meibohm, Santosh Kumar
Ethanol consumption is negatively associated with antiretroviral therapy (ART) adherence and general health in HIV positive individuals. Previously, we demonstrated ethanol-mediated alterations to metabolism of elvitegravir (EVG) in human liver microsomes. In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells. U1 cells were treated with 5 μM EVG, 2 μM Cobicistat (COBI), a booster drug, and 20 mM ethanol for up to 24 hours...
2017: PloS One
https://www.readbyqxmd.com/read/28219799/uplc-ms-ms-method-for-the-simultaneous-quantification-of-three-new-antiretroviral-drugs-dolutegravir-elvitegravir-and-rilpivirine-and-other-thirteen-antiretroviral-agents-plus-cobicistat-and-ritonavir-boosters-in-human-plasma
#11
Marco Simiele, Alessandra Ariaudo, Amedeo De Nicolò, Fabio Favata, Martina Ferrante, Chiara Carcieri, Stefano Bonora, Giovanni Di Perri, Antonio De Avolio
Rilpivirine (RPV), dolutegravir (DTG) and elvitegravir (EVG) are the latest antiretroviral drugs approved for treatment of HIV infection. Currently, poor information is currently available concerning their pharmacokinetic and pharmacodynamic properties, thus making the use of therapeutic drug monitoring for these drugs not useful. This lack of information is partially due to the absence of an high-throughput method for their simultaneous quantification together with other antiretroviral drugs. In this work, we describe the development and validation of a new UPLC-MS/MS method to quantify these drugs, together with other fourteen antiretroviral agents, in human plasma...
May 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28212411/lack-of-impact-of-pre-existing-t97a-hiv-1-integrase-mutation-on-integrase-strand-transfer-inhibitor-resistance-and-treatment-outcome
#12
Michael E Abram, Renee R Ram, Nicolas A Margot, Tiffany L Barnes, Kirsten L White, Christian Callebaut, Michael D Miller
T97A is an HIV-1 integrase polymorphism associated with integrase strand transfer inhibitor (INSTI) resistance. Using pooled data from 16 clinical studies, we investigated the prevalence of T97A (pre-existing and emergent) and its impact on INSTI susceptibility and treatment response in INSTI-naive patients who enrolled on elvitegravir (EVG)- or raltegravir (RAL)-based regimens. Prior to INSTI-based therapy, primary INSTI resistance-associated mutations (RAMs) were absent and T97A pre-existed infrequently (1...
2017: PloS One
https://www.readbyqxmd.com/read/28186251/switch-as-maintenance-to-elvitegravir-cobicistat-emtricitabine-tenofovir-disoproxil-fumarate-week-48-results-in-a-clinical-cohort
#13
Marine Perrier, Charlotte Charpentier, Gilles Peytavin, Minh Lê, Louis Blondel, Benoit Visseaux, Véronique Joly, Adriana Pinto, Sophie Matheron, Yazdan Yazdanpanah, Diane Descamps, Roland Landman
No abstract text is available yet for this article.
February 10, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28182625/viability-of-primary-osteoblasts-after-treatment-with-tenofovir-alafenamide-lack-of-cytotoxicity-at-clinically-relevant-drug-concentrations
#14
Christian Callebaut, Yang Liu, Darius Babusis, Adrian Ray, Michael Miller, Kathryn Kitrinos
Tenofovir alafenamide (TAF) is a phosphonoamidate prodrug of the nucleotide HIV reverse transcriptase inhibitor tenofovir (TFV). TAF is approved for the treatment of HIV-1 infection as part of the single-tablet regimen containing elvitegravir, cobicistat, emtricitabine, and TAF. When dosed once-daily, TAF results in approximately 90% lower levels of plasma TFV and a 4-fold increase in intracellular TFV-diphosphate (TFV-DP) in PBMCs compared with the TFV prodrug tenofovir disoproxil fumarate (TDF). Several antiretrovirals, including TDF, have been associated with bone mineral density decreases in patients; the effect of clinically relevant TAF concentrations on primary osteoblast viability was therefore assessed in vitro...
2017: PloS One
https://www.readbyqxmd.com/read/28166190/pharmacokinetics-of-crushed-elvitegravir-combination-tablet-given-with-or-without-enteral-nutrition
#15
Mieke Jongbloed-de Hoon, Angela Colbers, Kirsten Velthoven-Graafland, Marjolijn Duisenberg-van Essenberg, Martine Kruijssen, Evertine Abbink, Reinout van Crevel, David Burger
We investigated whether a fixed-dose combination tablet of elvitegravir, cobicistat, emtricitabine, and tenofovirDF (Stribild®), can be crushed and combined with enteral nutrition without influencing pharmacokinetics. This was an open-label, 3-period, single dose, randomized, cross-over, trial in 24 healthy volunteers. Subjects received Stribild whole tablet with breakfast (reference), crushed/suspended Stribild+breakfast, crushed/suspended Stribild+enteral nutrition. Crushed/suspended Stribild plus enteral nutrition was bio-equivalent (90% CI between 80-125%) with a whole Stribild tablet...
January 3, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28160503/comment-on-efficacy-of-elvitegravir-cobicistat-emtricitabine-tenofovir-disoproxil-fumarate-as-treatment-for-primary-or-recent-hiv-infection
#16
Juan Ambrosioni, María M Mosquera, José M Miró
No abstract text is available yet for this article.
February 4, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28151023/emtricitabine-tenofovir-alafenamide-for-the-treatment-of-hiv
#17
REVIEW
Katya C Corado, Eric S Daar
Tenofovir alafenamide is a new oral prodrug of tenofovir resulting in relatively low plasma levels and rapid uptake into peripheral blood mononuclear cells in its active form. The United States Food and Drug Administration has now approved this drug coformulated with elvitegravir/cobicistat/emtricitabine, rilpivirine/emtricitabine and emtricitabine. United States guidelines now list this formulation as one of the preferred components of a variety of antiretroviral regimens, and is included as an alternative in other international guidelines, with the notable exception of the World Health Organization, mostly due to limited availability...
March 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28121666/tenofovir-alafenamide-and-elvitegravir-loaded-nanoparticles-for-long-acting-prevention-of-hiv-1-vaginal-transmission
#18
Subhra Mandal, Pavan K Prathipati, Guobin Kang, You Zhou, Zhe Yuan, Wenjin Fan, Qingsheng Li, Christopher J Destache
OBJECTIVE: This report presents tenofovir (TFV) alafenamide (TAF) and elvitegravir (EVG) fabricated into nanoparticles for subcutaneous delivery as prevention strategy. DESIGN: Prospective prevention study in humanized bone marrow-liver-thymus (hu-BLT) mice. METHODS: Using an oil-in-water emulsion solvent evaporation technique, TAF + EVG drugs were entrapped together into nanoparticles containing poly(lactic-co-glycolic acid). In-vitro prophylaxis studies (90% inhibition concentration) compared nanoparticles with drugs in solution...
February 20, 2017: AIDS
https://www.readbyqxmd.com/read/28117606/tenofovir-alafenamide-emtricitabine-elvitegravir-and-cobicistat-combination-therapy-for-the-treatment-of-hiv
#19
Arkaitz Imaz, Daniel Podzamczer
Tenofovir alafenamide (TAF) is a novel prodrug of the nucleotide analogue reverse-transcriptase inhibitor, tenofovir. TAF has been co-formulated with emtricitabine (FTC), elvitegravir (EVG) and the EVG metabolic enhancer, cobicistat (COBI) as a single-tablet regimen being the first TAF-containing antiretroviral combination available. Areas covered: This article summarizes the available information on the pharmacology of the novel compound TAF and overviews TAF/FTC/EVG/COBI use for HIV-1 infected patients, with specific focus on clinical efficacy and safety data...
January 24, 2017: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/28112280/tenofovir-alafenamide-fumarate-for-the-treatment-of-hiv-infection
#20
REVIEW
R Sampath, J Zeuli, S Rizza, Z Temesgen
Tenofovir alafenamide fumarate is a recently developed prodrug of tenofovir, a nucleotide analogue reverse transcriptase inhibitor with potent inhibitory activity against HIV. The utility of a previously developed tenofovir prodrug, tenofovir disoproxil fumarate, had been hampered by renal and bone mineral adverse events. Tenofovir alafenamide fumarate overcomes the shortcomings of tenofovir disoproxil fumarate by delivering high intracellular concentrations of the parent drug, tenofovir, while substantially reducing systemic exposure...
November 2016: Drugs of Today
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