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https://www.readbyqxmd.com/read/28923862/antiviral-activity-of-bictegravir-and-cabotegravir-against-integrase-inhibitor-resistant-sivmac239-and-hiv-1
#1
Said A Hassounah, Ahmad Alikhani, Maureen Oliveira, Simrat Bharaj, Ruxandra-Ilinca Ibanescu, Nathan Osman, Hong-Tao Xu, Bluma G Brenner, Thibault Mesplède, Mark A Wainberg
Animal models are essential to study novel antiretroviral drugs, resistance-associated mutations (RAMs), and treatment strategies. Bictegravir (BIC) is a novel potent integrase (IN) strand transfer inhibitor (INSTI) that has shown promising results against HIV-1 infection in vitro and in vivo and against clinical isolates with resistance against INSTIs. BIC has a higher genetic barrier to the development of resistance than two clinically approved INSTIs termed raltegravir and elvitegravir. Another clinically approved INSTI, dolutegravir (DTG) also possesses a high genetic barrier to resistance while a fourth compound termed cabotegravir (CAB) is currently in late phases of clinical development...
September 18, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28918878/raltegravir-becomes-a-once-daily-antiretroviral
#2
François Raffi, Clotilde Allavena
No abstract text is available yet for this article.
September 11, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28918877/raltegravir-1200-mg-once-daily-versus-raltegravir-400-mg-twice-daily-with-tenofovir-disoproxil-fumarate-and-emtricitabine-for-previously-untreated-hiv-1-infection-a-randomised-double-blind-parallel-group-phase-3-non-inferiority-trial
#3
Pedro Cahn, Richard Kaplan, Paul E Sax, Kathleen Squires, Jean-Michel Molina, Anchalee Avihingsanon, Winai Ratanasuwan, Evelyn Rojas, Mohammed Rassool, Mark Bloch, Linos Vandekerckhove, Peter Ruane, Yazdan Yazdanpanah, Christine Katlama, Xia Xu, Anthony Rodgers, Lilly East, Larissa Wenning, Sandy Rawlins, Brenda Homony, Peter Sklar, Bach-Yen Nguyen, Randi Leavitt, Hedy Teppler
BACKGROUND: Once daily regimens are preferred for HIV-1 treatment, to facilitate adherence and improve quality of life. We compared a new once daily formulation of raltegravir to the currently marketed twice daily formulation. METHODS: In this randomised, double-blind, parallel-group, phase 3, non-inferiority study, we enrolled participants aged 18 years or older with HIV-1 RNA of 1000 or more copies per mL and no previous antiretroviral treatment at 139 sites worldwide...
September 11, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28903510/changes-in-liver-steatosis-after-switching-from-efavirenz-to-raltegravir-among-human-immunodeficiency-virus-infected-patients-with-nonalcoholic-fatty-liver-disease
#4
Juan Macías, María Mancebo, Dolores Merino, Francisco Téllez, M Luisa Montes-Ramírez, Federico Pulido, Antonio Rivero-Juárez, Miguel Raffo, Montserrat Pérez-Pérez, Nicolás Merchante, Manuel Cotarelo, Juan A Pineda
Background: Antiretroviral drugs with a lower potential to induce hepatic steatosis in human immunodeficiency virus (HIV) infection need to be identified. We compared the effect of switching efavirenz (EFV) to raltegravir (RAL) on hepatic steatosis among HIV-infected patients with nonalcoholic fatty liver disease (NAFLD) receiving EFV plus 2 nucleoside analogues. Methods: HIV-infected patients on EFV plus tenofovir/emtricitabine or abacavir/lamivudine with NAFLD were randomized 1:1 to switch from EFV to RAL (400 mg twice daily), maintaining nucleoside analogues unchanged, or to continue with EFV plus 2 nucleoside analogues...
September 15, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28895059/central-nervous-system-penetrating-antiretrovirals-impair-energetic-reserve-in-striatal-nerve-terminals
#5
Kelly L Stauch, Katy Emanuel, Benjamin G Lamberty, Brenda Morsey, Howard S Fox
The use of antiretroviral (ARV) drugs with central nervous system (CNS) penetration effectiveness (CPE) may be useful in the treatment of HIV-associated neurocognitive disorder (HAND) as well as targeting a CNS reservoir in strategies to achieve a functional cure for HIV. However, increased cognitive deficits are linked to at least one of these drugs (efavirenz). As mitochondrial dysfunction has been found with a number of ARVs, and as such can affect neuronal function, the objective of this study was to assess the effects of ARV with high CPE for toxicological profiles on presynaptic nerve terminal energy metabolism...
September 11, 2017: Journal of Neurovirology
https://www.readbyqxmd.com/read/28893602/raltegravir-blocks-the-infectivity-of-red-fluorescent-protein-mcherry-labeled-hiv-1jr-fl-in-the-setting-of-post-exposure-prophylaxis-in-nod-scid-jak3-mice-transplanted-with-human-pbmcs
#6
Hiromi Ogata-Aoki, Nobuyo Higashi-Kuwata, Shin-Ichiro Hattori, Hironori Hayashi, Matthew Danish, Manabu Aoki, Chiemi Shiotsu, Yumi Hashiguchi, Akinobu Hamada, Hisataka Kobayashi, Hironobu Ihn, Seiji Okada, Hiroaki Mitsuya
Employing NOD/SCID/Jak3(-/-) mice transplanted with human PBMCs (hNOJ mice) and replication-competent, red-fluorescent-protein (mCherry; mC)-labeled HIV-1JR-FL (HIVmC), we examined whether early antiretroviral treatment blocked the establishment of HIV-1 infection. The use of hNOJ mice and HIVmC enabled us to visually locate infection foci and to examine the early dynamics of HIVmC infection without using a large amount of antiretroviral unlike in non-human primate models. Although when raltegravir (RAL) administration was begun 1 day after intraperitoneal (ip) inoculation of HIVmC, no plasma p24 or plasma HIV-1-RNA (pRNA) were detected in 10 of 12 hNOJ (hNOJmC(RAL+)) mice over 14-day observation, all 10 untreated hNOJmC (hNOJmC(RAL-)) mice became positive for p24 and pRNA and had significantly swollen lymph nodes in peritoneal cavity and abundant p24(+)/mC(+)/CD3(+)/CD4(+) T cells and p24(+)/mC(+)/CD68(+) monocytes/macrophages were identified in their omenta and mesenteric lymphoid tissues/lymph nodes...
September 8, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28891371/an-observational-retrospective-analysis-evaluating-switching-to-raltegravir-plus-abacavir-lamivudine-in-hiv-1-infected-patients-the-oraswiral-study
#7
Laura Galli, Andrea Poli, Camilla Muccini, Nadia Galizzi, Anna Danise, Vincenzo Spagnuolo, Nicola Gianotti, Elisabetta Carini, Adriano Lazzarin, Antonella Castagna
No abstract text is available yet for this article.
September 11, 2017: Infectious Diseases
https://www.readbyqxmd.com/read/28875397/boceprevir-and-antiretroviral-pharmacokinetic-interactions-in-hiv-hcv-co-infected-persons-aids-clinical-trials-group-study-a5309s
#8
Jennifer J Kiser, Darlene Lu, Susan L Rosenkranz, Gene D Morse, Robin DiFrancesco, Kenneth E Sherman, Adeel A Butt
OBJECTIVE: The objective of this study was to determine the magnitude of drug interactions between the hepatitis C virus (HCV) protease inhibitor boceprevir (BOC) and antiretroviral (ARV) agents in persons with HIV/HCV co-infection. METHODS: Participants taking two nucleos(t)ide analogs with either efavirenz, raltegravir, or ritonavir-boosted atazanavir, darunavir, or lopinavir underwent intensive pharmacokinetic (PK) sampling for ARV 2 weeks before (week 2) and 2 weeks after initiating BOC (week 6) and for BOC at week 6...
September 5, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28861811/differential-effects-of-antiretroviral-drugs-on-neurons-in-vitro-roles-for-oxidative-stress-and-integrated-stress-response
#9
Anna L Stern, Rebecca N Lee, Nina Panvelker, Jiean Li, Jenna Harowitz, Kelly L Jordan-Sciutto, Cagla Akay-Espinoza
Mounting evidence suggests that antiretroviral drugs may contribute to the persistence of HIV-associated neurocognitive disorders (HAND), which impact 30%-50% of HIV-infected patients in the post-antiretroviral era. We previously reported that two first generation HIV protease inhibitors, ritonavir and saquinavir, induced oxidative stress, with subsequent neuronal death in vitro, which was reversed by augmentation of the endogenous antioxidant response by monomethyl fumarate. We herein determined whether two newer-generation PIs, darunavir and lopinavir, were deleterious to neurons in vitro...
August 31, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28859447/hiv-1-non-group-m-phenotypic-susceptibility-to-integrase-strand-transfer-inhibitors
#10
E Alessandri-Gradt, G Collin, A Tourneroche, M Bertine, M Leoz, C Charpentier, G Unal, D Descamps, J C Plantier
Objectives: To determine natural phenotypic susceptibility of non-group M HIV-1 to integrase strand transfer inhibitors (INSTIs) in a large panel of 39 clinical strains from groups O, N and P and to identify genotypic polymorphisms according to susceptibility levels. Methods: Susceptibility to raltegravir, elvitegravir and dolutegravir was evaluated in 36 HIV-1/O, 2 HIV-1/N and 1 HIV-1/P strains plus an HIV-1/M reference strain. IC50 values were determined after 3 days, and fold changes (FCs) were calculated relative to the HIV-1/M strain...
September 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28832412/the-hiv-1-integrase-e157q-polymorphism-per-se-does-not-alter-susceptibility-to-raltegravir-and-dolutegravir-in-vitro
#11
Francesco Saladini, Alessia Giannini, Adele Boccuto, Diletta Tiezzi, Ilaria Vicenti, Maurizio Zazzi
: The HIV-1 integrase E157Q natural polymorphism has been reported to cause one case of raltegravir (RAL) and dolutegravir (DTG) failure. We constructed six recombinant viruses containing integrase from HIV-1 isolates found to harbour E157Q as the only integrase strand inhibitor (INSTI) resistance-related mutation. Phenotypic analysis showed that E157Q results in minimal changes in RAL and DTG susceptibility. Together with data retrieved from the Stanford HIV database, our results indicate that E157Q is not a relevant INSTI resistance mutation per se...
August 21, 2017: AIDS
https://www.readbyqxmd.com/read/28825943/weight-gain-in-persons-with-hiv-switched-from-efavirenz-based-to-integrase-strand-transfer-inhibitor-based-regimens
#12
Jamison Norwood, Megan Turner, Carmen Bofill, Peter Rebeiro, Bryan Shepherd, Sally Bebawy, Todd Hulgan, Stephen Raffanti, David W Haas, Timothy R Sterling, John R Koethe
BACKGROUND: With the introduction of integrase strand transfer inhibitor (INSTI)-based antiretroviral therapy (ART), persons living with HIV have a potent new treatment option. Recently, providers at our large treatment clinic noted weight gain in several patients switched from efavirenz/tenofovir disoproxil fumarate/emtricitabine (EFV/TDF/FTC) to dolutegravir/abacavir/lamivudine (DTG/ABC/3TC). In this study, we evaluated weight change in patients with sustained virologic suppression switched from EFV/TDF/FTC to an INSTI-containing regimen...
August 18, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28790862/hyperbilirubinemia-in-atazanavir-treated-hiv-infected-patients-the-impact-of-the-ugt1a1-28-allele
#13
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
#14
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 method were developed for the simultaneous quantification of the concentrations of human immunodeficiency virus-1 integrase strand transfer inhibitors - raltegravir, dolutegravir and elvitegravir - 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. Chromatographic separation was achieved on an XBridge C18 column (50 × 2...
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
#15
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
#16
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/28737946/structure-guided-optimization-of-hiv-integrase-strand-transfer-inhibitors
#17
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 the 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...
September 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28735382/combined-medication-of-antiretroviral-drugs-tenofovir-disoproxil-fumarate-emtricitabine-and-raltegravir-reduces-neural-progenitor-cell-proliferation-in-vivo-and-in-vitro
#18
Peipei Xu, Yingchun Wang, Zhao Qin, Lisha Qiu, Min Zhang, Yunlong Huang, Jialin C Zheng
The application of combination antiretroviral therapy has greatly reduced the death rate from AIDS. However, up to 50% of patients on combination antiretroviral therapy develop HIV-associated neurocognitive disorders (HAND), which is associated with residual neuroinflammation and oxidative injury in the brain. Neural stem cells (NSCs) and progenitors play a vital role in repairing neuronal injuries. Therefore, we hypothesize that combination antiretroviral therapy may adversely affect NSCs/progenitors, contributing to the increasing prevalence of HAND...
July 22, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28723333/enhanced-prophylaxis-plus-antiretroviral-therapy-for-advanced-hiv-infection-in-africa
#19
RANDOMIZED CONTROLLED TRIAL
James Hakim, Victor Musiime, Alex J Szubert, Jane Mallewa, Abraham Siika, Clara Agutu, Simon Walker, Sarah L Pett, Mutsa Bwakura-Dangarembizi, Abbas Lugemwa, Symon Kaunda, Mercy Karoney, Godfrey Musoro, Sheila Kabahenda, Kusum Nathoo, Kathryn Maitland, Anna Griffiths, Margaret J Thomason, Cissy Kityo, Peter Mugyenyi, Andrew J Prendergast, A Sarah Walker, Diana M Gibb
BACKGROUND: In sub-Saharan Africa, among patients with advanced human immunodeficiency virus (HIV) infection, the rate of death from infection (including tuberculosis and cryptococcus) shortly after the initiation of antiretroviral therapy (ART) is approximately 10%. METHODS: In this factorial open-label trial conducted in Uganda, Zimbabwe, Malawi, and Kenya, we enrolled HIV-infected adults and children 5 years of age or older who had not received previous ART and were starting ART with a CD4+ count of fewer than 100 cells per cubic millimeter...
July 20, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28721059/cost-effectiveness-analysis-of-dolutegravir-plus-backbone-compared-with-raltegravir-plus-backbone-darunavir-ritonavir-plus-backbone-and-efavirenz-tenofovir-emtricitabine-in-treatment-na%C3%A3-ve-and-experienced-hiv-positive-patients
#20
Umberto Restelli, Giuliano Rizzardini, Andrea Antinori, Adriano Lazzarin, Marzia Bonfanti, Paolo Bonfanti, Davide Croce
BACKGROUND: In January 2014, the European Medicines Agency issued a marketing authorization for dolutegravir (DTG), a second-generation integrase strand transfer inhibitor for HIV treatment. The study aimed at determining the incremental cost-effectiveness ratio (ICER) of the use of DTG+backbone compared with raltegravir (RAL)+backbone, darunavir (DRV)+ritonavir(r)+backbone and efavirenz/tenofovir/emtricitabine (EFV/TDF/FTC) in HIV-positive treatment-naïve patients and compared with RAL+backbone in treatment-experienced patients, from the Italian National Health Service's point of view...
2017: Therapeutics and Clinical Risk Management
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