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https://www.readbyqxmd.com/read/28790862/hyperbilirubinemia-in-atazanavir-treated-hiv-infected-patients-the-impact-of-the-ugt1a1-28-allele
#1
REVIEW
Periklis Panagopoulos, Efstathios Maltezos, Angelos Hatzakis, Dimitrios Paraskevis
Combination antiretroviral treatment (cART) has significantly improved the life expectancy of people living with HIV. The life-long nature of cART increases the risk of side effects, which in some cases may have been caused by specific genetic characteristics. Patients treated with atazanavir (ATV) boosted with ritonavir (rit), which is a protease inhibitor used for the treatment of HIV, present with elevated bilirubin levels, at high proportions. ATV/rit-related hyperbilirubinemia has been previously associated with genetic characteristics in uridine diphosphate glucuronosyltransferase (UGT) enzyme...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/28762239/high-performance-liquid-chromatography-tandem-mass-spectrometry-for-simultaneous-determination-of-raltegravir-dolutegravir-and-elvitegravir-concentrations-in-human-plasma-and-cerebrospinal-fluid-samples
#2
Kiyoto Tsuchiya, Mayu Ohuchi, Naoe Yamane, Hiroaki Aikawa, Hiroyuki Gatanaga, Shinichi Oka, Akinobu Hamada
A simple sample treatment procedure and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method were developed for the simultaneous quantification of the concentrations of human immunodeficiency virus-1 (HIV-1) integrase strand transfer inhibitors (INSTIs); raltegravir (RAL), dolutegravir (DTG), and elvitegravir (EVG); in human plasma and cerebrospinal fluid (CSF). Plasma and CSF samples (20 μL each) were deproteinized with acetonitrile. Raltegravir-d3 was used as the internal standard (IS)...
July 31, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28753637/collaborative-update-of-a-rule-based-expert-system-for-hiv-1-genotypic-resistance-test-interpretation
#3
Roger Paredes, Philip L Tzou, Gert van Zyl, Geoff Barrow, Ricardo Camacho, Sergio Carmona, Philip M Grant, Ravindra K Gupta, Raph L Hamers, P Richard Harrigan, Michael R Jordan, Rami Kantor, David A Katzenstein, Daniel R Kuritzkes, Frank Maldarelli, Dan Otelea, Carole L Wallis, Jonathan M Schapiro, Robert W Shafer
INTRODUCTION: HIV-1 genotypic resistance test (GRT) interpretation systems (IS) require updates as new studies on HIV-1 drug resistance are published and as treatment guidelines evolve. METHODS: An expert panel was created to provide recommendations for the update of the Stanford HIV Drug Resistance Database (HIVDB) GRT-IS. The panel was polled on the ARVs to be included in a GRT report, and the drug-resistance interpretations associated with 160 drug-resistance mutation (DRM) pattern-ARV combinations...
2017: PloS One
https://www.readbyqxmd.com/read/28741965/cost-effectiveness-of-dolutegravir-abacavir-lamivudine-in-hiv-1-treatment-naive-tn-patients-in-france
#4
Gilles Pialoux, Anne-Geneviève Marcelin, Hélène Cawston, Caroline Guilmet, Laurent Finkielsztejn, Audrey Laurisse, Céline Aubin
BACKGROUND: To evaluate the cost-effectiveness of an integrase inhibitor (INI), dolutegravir (DTG), in combination with abacavir (ABC)/lamivudine (3TC) in France, in treatment-naive (TN) HIV adult patients. METHODS: The ARAMIS microsimulation Markov model, evaluates costs and effects of DTG vs. first-line ARVs options including INIs (raltegravir, elvitegravir/c), protease inhibitors (PIs) (darunavir/r, atazanavir/r, lopinavir/r), non-nucleoside reverse transcriptase inhibitors (efavirenz and rilpivirine)...
July 31, 2017: Expert Review of Pharmacoeconomics & Outcomes Research
https://www.readbyqxmd.com/read/28741582/prevalence-of-drug-drug-interactions-in-the-era-of-hiv-integrase-inhibitors-a-retrospective-clinical-study
#5
C Baecke, I C Gyssens, L Decoutere, J C H van der Hilst, P Messiaen
BACKGROUND: Antiretroviral agents pose a high risk for drug-drug interactions (DDIs), mainly but not limited to being a substrate, inducer or inhibitor of P450 cytochrome enzymes. In part metabolised by other pathways, integrase inhibitors might show a more favourable profile. The aim of this study was to investigate the prevalence of DDIs in daily clinical practice for patients starting different antiretroviral treatment (ART) regimens. METHODS: All patients starting ART in our centre from January 2009 to April 2016 were included...
July 2017: Netherlands Journal of Medicine
https://www.readbyqxmd.com/read/28737946/structure-guided-optimization-of-hiv-integrase-strand-transfer-inhibitors
#6
Xue Zhi Zhao, Steven J Smith, Daniel P Maskell, Mathieu Métifiot, Valerie E Pye, Katherine Fesen, Christophe Marchand, Yves Pommier, Peter Cherepanov, Stephen H Hughes, Terrence R Burke
Integrase mutations can reduce effectiveness of the first-generation FDA-approved integrase strand transfer inhibitors (INSTIs), raltegravir (RAL) and elvitegravir (EVG). The second-generation agent, dolutegravir (DTG) has enjoyed considerable clinical success; however, resistance-causing mutations that diminish the efficacy of DTG have appeared. Our current findings support and extend the substrate envelope concept that broadly effective INSTIs can be designed by filling the envelope defined by the DNA substrates...
July 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28696345/optimal-hiv-postexposure-prophylaxis-regimen-completion-with-single-tablet-daily-elvitegravir-cobicistat-tenofovir-disoproxil-fumarate-emtricitabine-compared-with-more-frequent-dosing-regimens
#7
COMPARATIVE STUDY
Kenneth H Mayer, Daniel Jones, Catherine Oldenburg, Sachin Jain, Marcy Gelman, Shayne Zaslow, Chris Grasso, Matthew J Mimiaga
STRUCTURE: The study evaluated elvitegravir/cobicistat/tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) ("Quad pill") for postexposure prophylaxis (PEP). BACKGROUND: HIV-exposed individuals may benefit from PEP, but completion rates have been suboptimal because of regimen complexity and side effects. Newer antiretroviral combinations coformulated as single daily pills may optimize PEP adherence. SETTING: One hundred HIV-uninfected individuals who presented to a Boston community health center after an acute HIV sexual exposure were enrolled and initiated PEP with the daily, single-pill combination Quad pill for a 28-day course...
August 15, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28689453/switching-to-the-single-tablet-regimen-of-elvitegravir-cobicistat-emtricitabine-and-tenofovir-df-from-non-nucleoside-reverse-transcriptase-inhibitor-plus-coformulated-emtricitabine-and-tenofovir-df-regimens-week-96-results-of-strategy-nnrti
#8
Anton Pozniak, Jason Flamm, Andrea Antinori, Mark Bloch, Douglas Ward, Juan Berenguer, Pierre Cote, Kristen Andreatta, William Garner, Javier Szwarcberg, Thai Nguyen-Cleary, Damian J McColl, David Piontkowsky
BACKGROUND: HIV-1-infected, virologically suppressed adults wanting to simplify or change their non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens may benefit from switching to the single-tablet regimen of elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate (E/C/F/TDF). OBJECTIVE: We examined differences in the proportion of participants with HIV-1 RNA < 50 copies/mL (Snapshot analysis), change in CD4 cell count, safety, and patient-reported outcomes in participants switching to E/C/F/TDF from an NNRTI + FTC/TDF (TVD) regimen...
July 9, 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/28664752/comment-extensive-bruising-and-elevated-rivaroxaban-plasma-concentration-in-a-patient-receiving-cobicistat-boosted-elvitegravir
#9
Jamielynn C Sebaaly, Denise Kelley
No abstract text is available yet for this article.
June 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28650901/application-of-quality-by-design-approach-to-bioanalysis-development-of-a-method-for-elvitegravir-quantification-in-human-plasma
#10
Sara Baldelli, Giorgio Marrubini, Dario Cattaneo, Emilio Clementi, Matteo Cerea
BACKGROUND: The application of Quality by Design (QbD) principles in clinical laboratories can help to develop an analytical method through a systematic approach, providing a significant advance over the traditional heuristic and empirical methodology. In the present work, we applied for the first time the QbD concept in the development of a method for drug quantification in human plasma using elvitegravir as the test molecule. METHODS: The goal of the study was to develop a fast and inexpensive quantification method, with precision and accuracy as requested by the EMA guidelines on bioanalytical method validation...
June 22, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28632758/safety-and-tolerability-of-elvitegravir-cobicistat-emtricitabine-tenofovir-disoproxil-fumarate-in-a-real-life-setting-data-from-surveillance-cohort-long-term-toxicity-antiretrovirals-antivirals-scolta-project
#11
Nicola Squillace, Elena Ricci, Tiziana Quirino, Andrea Gori, Alessandra Bandera, Laura Carenzi, Giuseppe Vittorio De Socio, Giancarlo Orofino, Canio Martinelli, Giordano Madeddu, Stefano Rusconi, Paolo Maggi, Benedetto Maurizio Celesia, Laura Cordier, Francesca Vichi, Leonardo Calza, Katia Falasca, Antonio Di Biagio, Giovanni Francesco Pellicanò, Paolo Bonfanti
OBJECTIVES: The study aim was to evaluate the impact on Liver and Kidney toxicity of the single tablet regimen Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Disoproxil Fumarate (EVG/COBI/FTC/TDF) on Antiretroviral Therapy (ART) experienced or naïve patients. METHODS: Patients initiating EVG/COBI/FTC/TDF were enrolled in the SCOLTA project, a multicenter observational study reporting grade 3-4 Adverse Events in subjects beginning new antiretroviral drug regimens...
2017: PloS One
https://www.readbyqxmd.com/read/28627771/clinical-experience-with-the-integrase-inhibitors-dolutegravir-and-elvitegravir-in-hiv-infected-patients-efficacy-safety-and-tolerance
#12
Purificación Cid-Silva, Josep M Llibre, Noelia Fernández-Bargiela, Luis Margusino-Framiñán, Vanesa Balboa-Barreiro, Berta Pernas-Souto, Isabel Martín-Herranz, Ángeles Castro-Iglesias, Eva Poveda
Two integrase inhibitors (INSTIs), dolutegravir (DTG) and elvitegravir/cobicistat (EVG/COBI), have joined recently the pharmacotherapy arsenal against HIV. This study evaluated the efficacy and tolerability of these INSTIs in the last two years. A retrospective observational study in patients who started DTG or EVG/COBI from January 2015 to January 2017 at a reference hospital in north-western Spain was done. Epidemiological, clinical and immunovirological data were recorded. A statistical analysis was performed with SPSS software...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627229/cobicistat-versus-ritonavir-similar-pharmacokinetic-enhancers-but-some-important-differences
#13
Alice Tseng, Christine A Hughes, Janet Wu, Jason Seet, Elizabeth J Phillips
OBJECTIVE: To describe properties of cobicistat and ritonavir; compare boosting data with atazanavir, darunavir, and elvitegravir; and summarize antiretroviral and comedication interaction studies, with a focus on similarities and differences between ritonavir and cobicistat. Considerations when switching from one booster to another are discussed. DATA SOURCES: A literature search of MEDLINE was performed (1985 to April 2017) using the following search terms: cobicistat, ritonavir, pharmacokinetic, drug interactions, booster, pharmacokinetic enhancer, HIV, antiretrovirals...
June 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28627222/reply-extensive-bruising-and-elevated-rivaroxaban-plasma-concentration-in-a-patient-receiving-cobicistat-boosted-elvitegravir
#14
Deborah Yoong, Mark Naccarato, Kevin Gough
No abstract text is available yet for this article.
June 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28583191/hiv-drug-resistance-against-strand-transfer-integrase-inhibitors
#15
REVIEW
Kaitlin Anstett, Bluma Brenner, Thibault Mesplede, Mark A Wainberg
Integrase strand transfer inhibitors (INSTIs) are the newest class of antiretroviral drugs to be approved for treatment and act by inhibiting the essential HIV protein integrase from inserting the viral DNA genome into the host cell's chromatin. Three drugs of this class are currently approved for use in HIV-positive individuals: raltegravir (RAL), elvitegravir (EVG), and dolutegravir (DTG), while cabotegravir (CAB) and bictegravir (BIC) are currently in clinical trials. RAL and EVG have been successful in clinical settings but have relatively low genetic barriers to resistance...
June 5, 2017: Retrovirology
https://www.readbyqxmd.com/read/28582509/high-decay-of-blood-hiv-reservoir-when-tenofovir-emtricitabine-elvitegravir-cobicistat-is-initiated-during-the-acute-primary-hiv-infection
#16
Elisabeth Carolle Ngo Bell, Marie-Anne Vandenhende, Sabrina Caldato, Aurélie Saunier, Pantxika Bellecave, Camille Tumiotto, Véronique Avettand-Fenoel, Mojgan Hessamfar, Philippe Morlat, Fabrice Bonnet
No abstract text is available yet for this article.
June 5, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28581645/effects-of-a-nutritional-protein-rich-drink-on-the-pharmacokinetics-of-elvitegravir-cobicistat-emtricitabine-tenofovir-alafenamide-and-tenofovir-compared-with-a-standard-meal-in-healthy-japanese-male-subjects
#17
REVIEW
Hiroyuki Yamada, Ippei Ikushima, Takanori Nemoto, Tomohiro Ishikawa, Noriko Ninomiya, Shin Irie
This study investigated the effects of ingested meal types on the pharmacokinetics of elvitegravir (EVG), cobicistat (COBI), emtricitabine (FTC), tenofovir alafenamide (TAF), and tenofovir (TFV) following a single administration of the single-tablet regimen (STR) of EVG/COBI/FTC/TAF (150/150/200/10 mg) in Japanese HIV-negative healthy subjects (n = 12). In this open-label, randomized, 3-way crossover study, the bioequivalence of the EVG/COBI/FTC/TAF STR following ingestion of a nutritional protein-rich drink with a reference treatment of taking a standard breakfast was evaluated...
June 5, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28579016/executive-summary-of-the-gesida-national-aids-plan-consensus-document-on-antiretroviral-therapy-in-adults-infected-by-the-human-immunodeficiency-virus-updated-january-2017
#18
(no author information available yet)
Antiretroviral therapy (ART) is recommended for all patients infected by HIV-1. The objective of ART is to achieve an undetectable plasma viral load (PVL). Initial ART should be based on a combination of 3 drugs, including 2 nucleoside reverse transcriptase inhibitors (tenofovir in either of its two formulations plus emtricitabine or abacavir plus lamivudine) and another drug from a different family. Four of the recommended regimens, all of which have an integrase inhibitor as the third drug (dolutegravir, elvitegravir boosted with cobicistat or raltegravir), are considered preferential, whereas a further 3 regimens (based on elvitegravir/cobicistat, rilpivirine, or darunavir boosted with cobicistat or ritonavir) are considered alternatives...
May 31, 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28569776/hiv-integrase-inhibitor-elvitegravir-impairs-rag-functions-and-inhibits-v-d-j-recombination
#19
Mayilaadumveettil Nishana, Namrata M Nilavar, Rupa Kumari, Monica Pandey, Sathees C Raghavan
Integrase inhibitors are a class of antiretroviral drugs used for the treatment of AIDS that target HIV integrase, an enzyme responsible for integration of viral cDNA into host genome. RAG1, a critical enzyme involved in V(D)J recombination exhibits structural similarity to HIV integrase. We find that two integrase inhibitors, Raltegravir and Elvitegravir, interfered with the physiological functions of RAGs such as binding, cleavage and hairpin formation at the recombination signal sequence (RSS), though the effect of Raltegravir was limited...
June 1, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28558493/a-review-of-the-efficacy-and-safety-of-genvoya-%C3%A2-elvitegravir-cobicistat-emtricitabine-and-tenofovir-alafenamide-in-the-management-of-hiv-1-infection
#20
Sara A Angione, Sibyl M Cherian, Ayşe Elif Özdener
INTRODUCTION: This review evaluates the efficacy and safety of Genvoya® (elvitegravir, cobicistat, emtricitabine, and tenofovir alafenamide [EVG/c/TAF/FTC]), a single-tablet regimen used for the management of HIV-1 infection. Phase II and III randomized clinical trials evaluate the efficacy and safety of EVG/c/TAF/FTC and tenofovir disoproxil fumerate (TDF)-containing arms; renal impairment, bone mineral density, metabolic effects, and other adverse events are topics explored within this review...
January 1, 2017: Journal of Pharmacy Practice
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