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Darunavir

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https://www.readbyqxmd.com/read/29683855/a-week-48-randomized-phase-3-trial-of-darunavir-cobicistat-emtricitabine-tenofovir-alafenamide-in-treatment-na%C3%A3-ve-hiv-1-patients
#1
Joseph J Eron, Chloe Orkin, Joel Gallant, Jean-Michel Molina, Eugenia Negredo, Andrea Antinori, Anthony Mills, Jacques Reynes, Erika Van Landuyt, Erkki Lathouwers, Veerle Hufkens, John Jezorwski, Simon Vanveggel, Magda Opsomer
OBJECTIVES: To investigate efficacy and safety of a single-tablet regimen of darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) 800/150/200/10 mg vs. darunavir/cobicistat plus emtricitabine/tenofovir disoproxyl fumarate (TDF) (control) in antiretroviral-treatment-naïve, HIV-1-infected adults. DESIGN: Phase-3, randomized, active-controlled, double-blind, international, multicenter, noninferiority study (NCT02431247). METHODS: Seven hundred and twenty-five participants were randomized (1 : 1) to D/C/F/TAF (362) or control (363)...
April 19, 2018: AIDS
https://www.readbyqxmd.com/read/29662875/positive-virological-outcomes-of-hiv-infected-patients-on-protease-inhibitor-based-second-line-regimen-in-cambodia-the-anrs-12276-2picam-study
#2
Olivier Ségéral, Eric Nerrienet, Sansothy Neth, Bruno Spire, Vohith Khol, Laurent Ferradini, Saramony Sarun, Chandara Mom, Sopheak Ngin, Charlotte Charpentier, Pagnaroat Men, Marion Mora, Vun Mean Chhi, Penhsun Ly, Vonthanak Saphonn
Background: Assessment of virological outcomes among HIV-infected patients receiving protease (PR) inhibitor-based second-line regimen are uncommon in Cambodia. The objective of this study is to assess the virological effectiveness of this regimen as well as impact of adherence boosting for patients experiencing virological failure. Methods: The 2PICAM study (Clinicaltrial: NCT01801618) is a cross-sectional study of HIV-infected adults on PR inhibitor-based second-line regimen since at least 6 months, conducted in 13 representative sites, comprising more than 90% of the target population...
2018: Frontiers in Public Health
https://www.readbyqxmd.com/read/29656080/an-nmr-strategy-to-detect-conformational-differences-in-a-protein-complexed-with-highly-analogous-inhibitors-in-solution
#3
John D Persons, Shahid N Khan, Rieko Ishima
This manuscript presents an NMR strategy to investigate conformational differences in protein-inhibitor complexes, when the inhibitors tightly bind to a protein at sub-nanomolar dissociation constants and are highly analogous to each other. Using HIV-1 protease (PR), we previously evaluated amide chemical shift differences, ΔCSPs, of PR bound to darunavir (DRV) compared to PR bound to several DRV analogue inhibitors, to investigate subtle but significant long-distance conformation changes caused by the inhibitor's chemical moiety variation [Khan, S...
April 12, 2018: Methods: a Companion to Methods in Enzymology
https://www.readbyqxmd.com/read/29649076/pharmacokinetics-of-tenofovir-alafenamide-when-co-administered-with-other-hiv-antiretrovirals
#4
Rebecca Begley, Moupali Das, Lijie Zhong, John Ling, Brian P Kearney, Joseph M Custodio
BACKGROUND: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen (elvitegravir/cobicistat/emtricitabine (F)/tenofovir alafenamide (TAF), rilpivirine/F/TAF, bictegravir/F/TAF), or for use with other ARVs (F/TAF), for treatment of HIV. TAF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. Disposition of TAF may be altered by co-medications that can inhibit or induce P-gp or BCRP transporters...
April 10, 2018: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/29625416/molecular-dynamics-and-ligand-docking-of-a-hinge-region-variant-of-south-african-hiv-1-subtype-c-protease
#5
Jake Zondagh, Vijayakumar Balakrishnan, Ikechukwu Achilonu, Heini W Dirr, Yasien Sayed
HIV-1 protease is an important antiretroviral drug target due to its key role in viral maturation. Computational models have been successfully used in the past to understand the dynamics of HIV-1 protease variants. We performed molecular dynamics simulations and induced fit docking on a wild-type South African HIV-1 subtype C protease and an N37T↑V hinge region variant. The simulations were initiated in a cubic cell universe and run in explicit solvent, with the wild-type and variant proteases in the fully closed conformation and under periodic boundary conditions...
March 27, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29623779/long-term-use-of-darunavir-ritonavir-containing-regimens-in-daily-practice-in-belgium-retrospective-observational-cohort-data-of-1701-hiv-patients
#6
Stéphane De Wit, Eric Florence, Linos Vandekerckhove, Bernard Vandercam, Jean-Christophe Goffard, Eric Van Wijngaerden, Michel Moutschen, Remy Demeester, Pushpike Thilakarathne, Hilde Piryns
Background Once daily (QD) ritonavir or cobicistat-boosted darunavir (DRV/b), in combination with other antiretrovirals (ARVs), is recommended as a first-line option for human immunodeficiency virus-infected patients in European and USA guidelines. The objective of this study was to analyse the outcomes of DRV/r QD-based antiretroviral therapy (ART) regimens in real-life settings. Methods This is an observational, non-interventional, non-comparative, retrospective, multicentre cohort study. Data were collected from the databases of eight Belgian AIDS Reference Centres...
April 6, 2018: Acta Clinica Belgica
https://www.readbyqxmd.com/read/29608687/darunavir-ritonavir-600-100-mg-once-daily-it-s-time-for-larger-non-inferiority-randomized-trials
#7
S Nicolè, M Lanzafame, G Cucchetto, F Rigo, E Lattuada, E Concia
No abstract text is available yet for this article.
March 28, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29592840/doravirine-versus-ritonavir-boosted-darunavir-in-antiretroviral-naive-adults-with-hiv-1-drive-forward-48-week-results-of-a-randomised-double-blind-phase-3-non-inferiority-trial
#8
Jean-Michel Molina, Kathleen Squires, Paul E Sax, Pedro Cahn, Johan Lombaard, Edwin DeJesus, Ming-Tain Lai, Xia Xu, Anthony Rodgers, Lisa Lupinacci, Sushma Kumar, Peter Sklar, Bach-Yen Nguyen, George J Hanna, Carey Hwang
BACKGROUND: Doravirine is a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) with a pharmacokinetic profile supporting once-daily dosing, and potent in-vitro activity against the most common NNRTI-resistant HIV-1 variants. We compared doravirine with ritonavir-boosted darunavir, when both were given with two nucleoside reverse transcriptase inhibitors (NRTIs), in adults with previously untreated HIV-1 infection. METHODS: In this randomised, controlled, double-blind, multicentre, non-inferiority trial, adults with HIV-1 infection were screened and enrolled at 125 clinical centres in 15 countries...
March 23, 2018: Lancet HIV
https://www.readbyqxmd.com/read/29588457/efficacy-and-safety-of-boosted-darunavir-based-antiretroviral-therapy-in-hiv-1-positive-patients-results-from-a-meta-analysis-of-clinical-trials
#9
A Antinori, A Lazzarin, A Uglietti, M Palma, D Mancusi, R Termini
Darunavir/ritonavir (DRV/r) is a second-generation protease inhibitor used in treatment-naïve and -experienced HIV-positive adult patients. To evaluate efficacy and safety in these patient settings, we performed a meta-analysis of randomized controlled trials. We considered eight studies involving 4240 antiretroviral treatment (ART)-naïve patients and 14 studies involving 2684 ART-experienced patients. Regarding efficacy in the ART-naive patients, the virological response rate was not significantly different between DRV/r and the comparator...
March 27, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29575909/nucleoside-reverse-transcriptase-inhibitors-with-reduced-predicted-activity-does-not-impair-second-line-therapy-with-lopinavir-ritonavir-or-darunavir-ritonavir
#10
Christian-Julian Villabona-Arenas, Sabrina Eymard-Duvernay, Avelin Fobang Aghokeng, Emilande Guichet, Coumba Toure-Kane, Guillaume Bado, Sinata Koulla-Shiro, Eric Delaporte, Laura Ciaffi, Martine Peeters
Second-line therapy randomized trials with Lopinavir/Ritonavir question the value of resistance testing to guide Nucleoside Reverse Transcriptase Inhibitors selection. Here, we investigated the association between baseline drug resistance and treatment outcome after 104 weeks of second-line therapy with NRTIs and either Darunavir/Ritonavir or Lopinavir/Ritonavir in West-central Africa. We did an observational analysis of data from 387 individuals in the randomized, open-label 2LADY trial in Burkina Faso, Cameroon and Senegal...
March 25, 2018: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/29570286/hydration-structure-and-dynamics-of-inhibitor-bound-hiv-1-protease
#11
Florian Leidner, Nese Kurt Yilmaz, Janet Paulsen, Yves A Muller, Celia A Schiffer
Water is an essential in many biological processes, and the hydration structure plays a critical role in facilitating protein folding, dynamics and ligand binding. A variety of biophysical spectroscopic techniques have been used to probe the water solvating proteins, often complemented with molecular dynamics (MD) simulations to resolve the spatial and dynamic features of the hydration shell, but comparing relative water structure is challenging. In this study 1 microsecond MD simulations were performed to identify and characterize hydration sites around HIV-1 protease bound to an inhibitor, darunavir (DRV)...
March 23, 2018: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/29550449/hiv-care-in-central-and-eastern-europe-how-close-are-we-to-the-target
#12
Deniz Gokengin, Cristiana Oprea, Josip Begovac, Andrzej Horban, Arzu Nazlı Zeka, Dalibor Sedlacek, Bayjanov Allabergan, Esmira A Almamedova, Tatevik Balayan, Denes Banhegyi, Pavlina Bukovinova, Nikoloz Chkhartishvili, Alymbaeva Damira, Edona Deva, Ivaylo Elenkov, Luljeta Gashi, Dafina Gexha-Bunjaku, Vesna Hadciosmanovic, Arjan Harxhi, Tiberiu Holban, Djorje Jevtovic, David Jilich, Justyna Kowalska, Djhamal Kuvatova, Natalya Ladnaia, Adkhamjon Mamatkulov, Aleksandra Marjanovic, Maria Nikolova, Mario Poljak, Kristi Rüütel, Azzaden Shunnar, Milena Stevanovic, Zhanna Trumova, Oleg Yurin
OBJECTIVES: The aim of this survey was to describe the current status of HIV care in Central and Eastern European countries and to look at how close the region is to achieve the UNAIDS 2020 target of 90-90-90. METHODS: In 2014 data were collected from 24 Central and Eastern European countries by a 38-item questionnaire. RESULTS: All countries reported mandatory screening of blood and organ donors for HIV. Other groups who were subjected to targeted screening were people who inject drugs (PWID) (15/24; 62...
March 14, 2018: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/29533303/changes-in-plasma-rankl-osteoprotegerin-in-a-prospective-randomized-clinical-trial-of-initial-antiviral-therapy-a5260s
#13
Theodoros Kelesidis, Carlee B Moser, Elizabeth Johnston, James H Stein, Michael P Dube, Otto O Yang, Grace A McComsey, Judith S Currier, Todd T Brown
BACKGROUND: The contributions of the Receptor activator of nuclear factor kappa-B ligand (RANKL)/osteoprotegerin (OPG) axis to cardiovascular and bone disease in treated HIV-1 infection is not well-defined. SETTING: Prospective, observational, longitudinal study. METHODS: In a subset analysis of a prospective randomized clinical trial, 234 HIV-1-infected antiretroviral therapy (ART)-naïve participants received tenofovir-emtricitabine plus either atazanavir/ritonavir, darunavir/ritonavir, or raltegravir and achieved plasma HIV-1 RNA <50 copies/ml by week 24 and thereafter...
March 12, 2018: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/29528852/fixed-dose-darunavir-boosted-with-cobicistat-combined-with-emtricitabine-and-tenofovir-alafenamide-fumarate
#14
Muge Cevik, Chloe Orkin
PURPOSE OF REVIEW: In an era when virological efficacy approaches 100%, novel antiretroviral (ARV) therapies must deliver better tolerability, safety, and convenient coformulated regimens. We review the phase II and III clinical data on the fixed dose combination (FDC) darunavir (DRV) 800mg / cobicistat (COBI/C) 150 mg / emtricitabine (F/FTC) 200 mg / tenofovir alafenamide fumarate (TAF) 10mg (D/C/F/TAF) for the treatment of HIV-1 infection. RECENT FINDINGS: In an exploratory phase II study, D/C/F/TAF FDC demonstrated similar virological efficacy to darunavir/cobicistat FDC + F /tenofovir disoproxil fumarate (TDF) FDC in treatment-naive HIV-1-infected individuals with favorable bone and renal outcomes...
March 9, 2018: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/29523599/mrp2-inhibition-by-hiv-protease-inhibitors-in-rat-and-human-hepatocytes-a-quantitative-confocal-microscopy-study
#15
Nico Holmstock, Marlies Oorts, Jan Snoeys, Pieter Annaert
Hepatic drug transporters play a pivotal role in the excretion of drugs from the body, in drug-drug interactions as well as in drug-induced liver toxicity. Hepatocytes cultured in sandwich configuration are an advantageous model to investigate the interactions of drug candidates with apical efflux transporters in a bio-relevant manner. However, the commonly used 'offline' assays (i.e. that rely on measuring intracellular accumulated amounts after cell lysis) are time and resource consuming while data output is often high and variable...
March 9, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29522076/drug-drug-interactions-studies-between-hcv-antivirals-sofosbuvir-velpatasvir-and-boosted-and-unboosted-hiv-antiretroviral-regimens-in-healthy-volunteers
#16
Erik Mogalian, Luisa M Stamm, Anu Osinusi, Diana M Brainard, Gong Shen, Kah Hiing John Ling, Anita Mathias
Background: Combining antiviral regimens in the HCV/HIV coinfected population can be complex as they share overlapping mechanisms for elimination that may result in potential drug interactions. The pharmacokinetics, safety, and tolerability of concomitantly administered sofosbuvir/velpatasvir (SOF/VEL) with multiple commonly prescribed antiretroviral (ARV) regimens were evaluated. Methods: Healthy volunteers were enrolled into two phase 1, open-label, randomized, multiple-dose, cross-over studies...
March 7, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29513131/dolutegravir-with-boosted-darunavir-treatment-simplification-for-the-transmitted-hiv-thymidine-analog-resistance-in-manitoba-canada
#17
J Wheeler, S Chan, P R Harrigan, M Becker, K Kasper, Y Keynan
No abstract text is available yet for this article.
April 2018: International Journal of STD & AIDS
https://www.readbyqxmd.com/read/29511083/mechanism-of-darunavir-drv-s-high-genetic-barrier-to-hiv-1-resistance-a-key-v32i-substitution-in-protease-rarely-occurs-but-once-it-occurs-it-predisposes-hiv-1-to-develop-drv-resistance
#18
Manabu Aoki, Debananda Das, Hironori Hayashi, Hiromi Aoki-Ogata, Yuki Takamatsu, Arun K Ghosh, Hiroaki Mitsuya
Darunavir (DRV) has bimodal activity against HIV-1 protease, enzymatic inhibition and protease dimerization inhibition, and has an extremely high genetic barrier against development of drug resistance. We previously generated a highly DRV-resistant HIV-1 variant (HIVDRV R P51 ). We also reported that four amino acid substitutions (V32I, L33F, I54M, and I84V) identified in the protease of HIVDRV R P51 are largely responsible for its high-level resistance to DRV. Here, we attempted to elucidate the role of each of the four amino acid substitutions in the development of DRV resistance...
March 6, 2018: MBio
https://www.readbyqxmd.com/read/29493419/durability-and-tolerability-of-first-line-regimens-including-two-nucleoside-reverse-transcriptase-inhibitors-and-raltegravir-or-ritonavir-boosted-atazanavir-or-darunavir-data-from-the-icona-cohort
#19
Antonella d'Arminio Monforte, Patrizia Lorenzini, Alessandro Cozzi-Lepri, Cristina Mussini, Antonella Castagna, Franco Baldelli, Massimo Puoti, Francesca Vichi, Adelaide Maddaloni, Sergio Lo Caputo, Nicola Gianotti, Andrea Antinori
Background We aimed to mimic the ACTG 5257 trial, comparing raltegravir (RAL), ritonavir-boosted atazavavir (ATV/r) and ritonavir-boosted darunavir (DRV/r) in the observational setting. Methods All the ICONA patients starting a first cART with 2NRTI + ATV/r, DRV/r or RAL were included. Primary end-point was treatment failure, i.e. virological failure (confirmed HIV-RNA > 200copies/mL > 6 months therapy) or discontinuation for any reason of the third drug. Secondary end-points: virological failure50 (50 copies/mL threshold), and discontinuation of the third drug due to intolerance/toxicity...
March 1, 2018: HIV Clinical Trials
https://www.readbyqxmd.com/read/29478329/single-tablet-hiv-regimens-facilitate-virologic-suppression-and-retention-in-care-among-treatment-na%C3%A3-ve-patients
#20
Vagish Hemmige, Charlene A Flash, Josephinel Carter, Thomas P Giordano, Teddy Zerai
Newer HIV regimens are typically taken once daily but vary in the number of pills required. Whether the number of pills in a once-daily HIV regimen affects clinical outcomes is unknown. We retrospectively compared adherence, retention in care, and virologic outcomes between patients starting a once daily single-tablet regimen (STR) to patients starting a once-daily multi-tablet regimen (MTR) in a publicly funded clinic in the United States. Outcomes were measured in the year after starting ART and included retention in care, virologic suppression, and medication possession ratio of at least 80%...
February 25, 2018: AIDS Care
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