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https://www.readbyqxmd.com/read/29156381/structure-based-methods-to-predict-mutational-resistance-to-diarylpyrimidine-non-nucleoside-reverse-transcriptase-inhibitors
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
https://www.readbyqxmd.com/read/28994660/pharmacokinetics-of-rilpivirine-and-24-week-outcomes-after-switching-from-efavirenz-in-virologically-suppressed-hiv-1-infected-adolescents
#8
Watsamon Jantarabenjakul, Suvaporn Anugulruengkitt, Naruporn Kasipong, Narukjaporn Thammajaruk, Jiratchaya Sophonphan, Torsak Bunupuradah, Tim R Cressey, Angela Colbers, David M Burger, Wanatpreeya Phongsamart, Thanyawee Puthanakit, Chitsanu Pancharoen
BACKGROUND: Rilpivirine (RPV), a non-nucleoside reverse transcriptase inhibitor drug, could be a favorable drug for maintenance therapy in HIV-infected adolescents because it has few long-term side effects. However, data among adolescents switching from efavirenz (EFV) to RPV are limited. This study investigated the pharmacokinetics (PK), safety and efficacy of RPV in virologically-suppressed HIV-1-infected adolescents after switching from EFV. METHODS: Adolescents aged 12-18 years on EFV-based antiretroviral therapy (ART) were switched from EFV to RPV (25 mg, once daily)...
October 10, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28971607/lack-of-clinically-important-pk-interaction-between-coformulated-ledipasvir-sofosbuvir-and-rilpivirine-emtricitabine-tenofovir-alafenamide
#9
Joseph M Custodio, Susan K Chuck, Hoa Chu, Huyen Cao, Grace Ma, John Flaherty, John Ling, Brian P Kearney
The drug-drug interaction (DDI) potential between the fixed-dose combinations of ledipasvir/sofosbuvir 90/400 mg for hepatitis C virus and emtricitabine/rilpivirine/tenofovir alafenamide (TAF) 200/25/25 mg for HIV was evaluated in a randomized, open-label, single-center, multiple-dose, 3-way, 6-sequence, crossover Phase 1 study in 42 healthy subjects. Emtricitabine/rilpivirine/TAF had no relevant effect on the pharmacokinetic parameters of maximum concentration [Cmax ] and area under the concentration versus time curve over the dosing interval [AUCtau ] for ledipasvir, sofosbuvir, and the metabolites GS-566500 and GS-331007...
October 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28968669/human-immunodeficiency-virus-type-1-drug-resistance-mutations-update
#10
Robert W Shafer
As treatment options coalesce around a smaller number of antiretroviral drugs (ARVs), data are emerging on the drug resistance mutations (DRMs) selected by the most widely used ARVs and on the impact of these DRMs on ARV susceptibility and virological response to first- and later-line treatment regimens. Recent studies have described the DRMs that emerge in patients receiving tenofovir prodrugs, the nonnucleoside reverse transcriptase inhibitors efavirenz and rilpivirine, ritonavir-boosted lopinavir, and the integrase inhibitors raltegravir and elvitegravir...
September 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28961979/penetration-and-antiviral-efficacy-of-total-and-unbound-maraviroc-raltegravir-and-rilpivirine-in-both-female-and-male-genital-fluids-from-hiv-positive-patients-receiving-regimens-containing-these-antiretrovirals
#11
Minh P Lê, Linda Belarbi, Marie-Laure Chaix, Emmanuel Dulioust, Nadia Mahjoub, Dominique Salmon, Jean-Paul Viard, Claudine Duvivier, Gilles Peytavin, Odile Launay, Jade Ghosn
Background: Sub-optimal penetration of antiretroviral drugs in genital compartments might promote local HIV persistence and increase the risk of HIV transmission. Objectives: To describe the penetration of maraviroc, raltegravir, raltegravir glucuronide and rilpivirine in seminal plasma and cervico-vaginal secretions (CVS) and to assess local antiretroviral efficacy in HIV-1-positive patients. Methods: This was a prospective, multicentre study...
November 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28961903/m184i-v-substitutions-and-e138k-m184i-v-double-substitutions-in-hiv-reverse-transcriptase-do-not-significantly-affect-the-antiviral-activity-of-efda
#12
Maureen Oliveira, Bluma G Brenner, Hongtao Xu, Ruxandra-Ilinca Ibanescu, Thibault Mesplède, Mark A Wainberg
Background: 4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) is a potent nucleoside analogue inhibitor of HIV that has an unusually long half-life. Cell culture selections with either EFdA or lamivudine using both subtype B and non-B clinical isolates selected the M184I/V substitutions in reverse transcriptase (RT). Unlike lamivudine, however, EFdA retained significant activity against viruses containing the M184I/V substitutions. In other clinical trials that evaluated rilpivirine together with emtricitabine in first-line therapy, the emergence of both the M184I/V and E138K mutations in RT was demonstrated...
November 1, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28944075/efficacy-of-switching-to-dolutegravir-plus-rilpivirine-the-small-tablet-regimen-in-patients-with-dysphagia-two-case-reports
#13
Takefumi Suzuki, Nobuko Hara, Morichika Osa, Kazuhisa Misawa, Kazuo Imai, Yuji Fujikura, Takuya Maeda, Wataru Sonehara, Akihiko Kawana
BACKGROUND: The advent of well-tolerated and effective anti-retroviral drugs against human immunodeficiency virus-1 (HIV-1) infection has been a major step forward that has achieved long-term survival in recent years. The number of HIV-1 infected patients who experience difficulty in swallowing tablets is expected to increase as the HIV-infected population advances in age or develops comorbidities or treatment sequelae affecting the central nervous system. CASE PRESENTATION: Here, we describe two HIV-1-infected patients who experienced progressive dysphagia leading to inability to swallow the antiretroviral tablets included in the standard regimen...
2017: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/28854832/pharmacokinetic-drug-evaluation-of-dolutegravir-plus-rilpivirine-for-the-treatment-of-hiv
#14
REVIEW
Amedeo F Capetti, Noemi Astuti, Dario Cattaneo, Giuliano Rizzardini
The search for simple, potent, metabolic-friendly and nucleoside/nucleotide sparing antiretroviral regimens has led clinical investigators to move steps towards dual therapies. Among these the association of rilpivirine and dolutegravir is emerging as a twin randomized clinical trial (SWORD1&2) and at least three observational cohort describe it as a safe and highly effective regimen for switch from other therapies Areas covered: We review the evidence supporting the use of dolutegravir plus rilpivirine for the treatment of HIV in virologically suppressed patients taking other antiretroviral regimens...
November 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28845699/enhancement-of-oral-bioavailability-of-anti-hiv-drug-rilpivirine-hcl-through-nanosponge-formulation
#15
Rana Zainuddin, Zahid Zaheer, Jaiprakash N Sangshetti, Mufassir Momin
OBJECTIVE: To synthesize β cyclodextrin nanosponges using a novel and efficient microwave mediated method for enhancing bioavailability of Rilpivirine HCl (RLP). SIGNIFICANCE: Belonging to BCS class II RLP has pH dependent solubility and poor oral bioavailability. However, a fatty meal enhances its absorption hence the therapy indicates that the dosage form be consumed with a meal. But then it becomes tedious and inconvenient to continue the therapy for years with having to face the associated gastric side effects such as nausea...
December 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28836468/effectiveness-safety-and-costs-of-a-treatment-switch-to-dolutegravir-plus-rilpivirine-dual-therapy-in-treatment-experienced-hiv-patients
#16
José Luis Revuelta-Herrero, Esther Chamorro-de-Vega, Carmen Guadalupe Rodríguez-González, Roberto Alonso, Ana Herranz-Alonso, María Sanjurjo-Sáez
BACKGROUND: Evidence about the use of dolutegravir (DTG) and rilpivirine (RPV) as an antiretroviral therapy (ART) in treatment-experienced patients is scarce. OBJECTIVE: To explore the effectiveness, safety, and costs of switching to a DTG plus RPV regimen in this population. METHODS: This observational, prospective study included all treatment-experienced patients who switched to DTG plus RPV between November 2014 and July 2016. Patients were excluded if resistance mutations to integrase inhibitors or RPV were found...
August 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28827354/covalent-inhibitors-for-eradication-of-drug-resistant-hiv-1-reverse-transcriptase-from-design-to-protein-crystallography
#17
Albert H Chan, Won-Gil Lee, Krasimir A Spasov, José A Cisneros, Shalley N Kudalkar, Zaritza O Petrova, Amanda B Buckingham, Karen S Anderson, William L Jorgensen
Development of resistance remains a major challenge for drugs to treat HIV-1 infections, including those targeting the essential viral polymerase, HIV-1 reverse transcriptase (RT). Resistance associated with the Tyr181Cys mutation in HIV-1 RT has been a key roadblock in the discovery of nonnucleoside RT inhibitors (NNRTIs). It is the principal point mutation that arises from treatment of HIV-infected patients with nevirapine, the first-in-class drug still widely used, especially in developing countries. We report covalent inhibitors of Tyr181Cys RT (CRTIs) that can completely knock out activity of the resistant mutant and of the particularly challenging Lys103Asn/Tyr181Cys variant...
September 5, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28799920/3-year-efficacy-and-durability-of-simplification-to-single-tablet-regimens-a-comparison-between-co-formulated-efavirenz-emtricitabine-tenofovir-and-rilpivirine-emtricitabine-tenofovir
#18
Roberta Gagliardini, Alessandra Bandera, Mauro Zaccarelli, Gaetana Sterrantino, Alessandra Latini, Alessandro D'Avino, Giuseppe Lapadula, Andrea Antinori, Roberto Cauda, Andrea De Luca, Andrea Gori, Simona Di Giambenedetto, Massimiliano Fabbiani
BACKGROUND: Few data are available about efficacy and durability of simplification from multi-tablet antiretroviral regimens to co-formulated efavirenz(EFV)/emtricitabine(FTC)/tenofovir(TDF) versus rilpivirine(RPV)/emtricitabine/tenofovir in virologically-suppressed HIV-1-infected patients. METHODS: We retrospectively analyzed HIV-infected patients with HIV-RNA<50copies/mL switching to co-formulated EFV/FTC/TDF or RPV/FTC/TDF at 5 Italian centers. Patients were followed from time of switch until regimen discontinuation or a maximum of 3-years follow-up...
August 11, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28753637/collaborative-update-of-a-rule-based-expert-system-for-hiv-1-genotypic-resistance-test-interpretation
#19
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/28750935/long-acting-intramuscular-cabotegravir-and-rilpivirine-in-adults-with-hiv-1-infection-latte-2-96-week-results-of-a-randomised-open-label-phase-2b-non-inferiority-trial
#20
David A Margolis, Juan Gonzalez-Garcia, Hans-Jürgen Stellbrink, Joseph J Eron, Yazdan Yazdanpanah, Daniel Podzamczer, Thomas Lutz, Jonathan B Angel, Gary J Richmond, Bonaventura Clotet, Felix Gutierrez, Louis Sloan, Marty St Clair, Miranda Murray, Susan L Ford, Joseph Mrus, Parul Patel, Herta Crauwels, Sandy K Griffith, Kenneth C Sutton, David Dorey, Kimberly Y Smith, Peter E Williams, William R Spreen
BACKGROUND: Cabotegravir and rilpivirine are antiretroviral drugs in development as long-acting injectable formulations. The LATTE-2 study evaluated long-acting cabotegravir plus rilpivirine for maintenance of HIV-1 viral suppression through 96 weeks. METHODS: In this randomised, phase 2b, open-label study, treatment-naive adults infected with HIV-1 initially received oral cabotegravir 30 mg plus abacavir-lamivudine 600-300 mg once daily. The objective of this study was to select an intramuscular dosing regimen based on a comparison of the antiviral activity, tolerability, and safety of the two intramuscular dosing regimens relative to oral cabotegravir plus abacavir-lamivudine...
July 21, 2017: Lancet
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