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https://www.readbyqxmd.com/read/28507107/in-vitro-cross-resistance-profiles-of-rilpivirine-dapivirine-and-miv-150-nnrti-microbicides-in-clinical-development-for-the-prevention-of-hiv-1-infection
#1
Nicholas S Giacobbi, Nicolas Sluis-Cremer
Rilpivirine, dapivirine (DPV) and MIV-150 are in development as microbicides. It is not known whether they will block infection of circulating NNRTI-resistant HIV-1 variants. Here, we demonstrate that the activity of DPV and MIV-150 are compromised by many resistant viruses containing single or double substitutions. High DPV genital tract concentrations from DPV-ring use may block replication of resistant viruses. However, MIV-150 genital tract concentrations may be insufficient to inhibit many resistant viruses, including those harboring K103N or Y181C...
May 15, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28484509/factors-associated-with-pre-treatment-hiv-rna-application-for-the-use-of-abacavir-and-rilpivirine-as-the-first-line-regimen-for-hiv-infected-patients-in-resource-limited-settings
#2
Sasisopin Kiertiburanakul, David Boettiger, Oon Tek Ng, Nguyen Van Kinh, Tuti Parwati Merati, Anchalee Avihingsanon, Wing-Wai Wong, Man Po Lee, Romanee Chaiwarith, Adeeba Kamarulzaman, Pacharee Kantipong, Fujie Zhang, Jun Yong Choi, Nagalingeswaran Kumarasamy, Rossana Ditangco, Do Duy Cuong, Shinichi Oka, Benedict Lim Heng Sim, Winai Ratanasuwan, Penh Sun Ly, Evy Yunihastuti, Sanjay Pujari, Jeremy L Ross, Matthew Law, Somnuek Sungkanuparph
BACKGROUND: Abacavir and rilpivirine are alternative antiretroviral drugs for treatment-naïve HIV-infected patients. However, both drugs are only recommended for the patients who have pre-treatment HIV RNA <100,000 copies/mL. In resource-limited settings, pre-treatment HIV RNA is not routinely performed and not widely available. The aims of this study are to determine factors associated with pre-treatment HIV RNA <100,000 copies/mL and to construct a model to predict this outcome...
2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28476131/factors-associated-with-pre-treatment-hiv-rna-application-for-the-use-of-abacavir-and-rilpivirine-as-the-first-line-regimen-for-hiv-infected-patients-in-resource-limited-settings
#3
Sasisopin Kiertiburanakul, David Boettiger, Oon Tek Ng, Nguyen Van Kinh, Tuti Parwati Merati, Anchalee Avihingsanon, Wing-Wai Wong, Man Po Lee, Romanee Chaiwarith, Adeeba Kamarulzaman, Pacharee Kantipong, Fujie Zhang, Jun Yong Choi, Nagalingeswaran Kumarasamy, Rossana Ditangco, Do Duy Cuong, Shinichi Oka, Benedict Lim Heng Sim, Winai Ratanasuwan, Penh Sun Ly, Evy Yunihastuti, Sanjay Pujari, Jeremy L Ross, Matthew Law, Somnuek Sungkanuparph
BACKGROUND: Abacavir and rilpivirine are alternative antiretroviral drugs for treatment-naïve HIV-infected patients. However, both drugs are only recommended for the patients who have pre-treatment HIV RNA <100,000 copies/mL. In resource-limited settings, pre-treatment HIV RNA is not routinely performed and not widely available. The aims of this study are to determine factors associated with pre-treatment HIV RNA <100,000 copies/mL and to construct a model to predict this outcome...
May 5, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28472812/agreement-between-estimated-and-measured-renal-function-in-an-everyday-clinical-outpatient-setting-of-human-immunodeficiency-virus-infected-individuals
#4
Magnus Glindvad Ahlström, Andreas Kjær, Jan Gerstoft, Niels Obel
INTRODUCTION: Estimated renal function (eRF) has been widely implemented as a screening tool in handling human immunodeficiency virus (HIV)-infected individuals. Our primary objective was to investigate the agreement between measured renal function (mRF) and eRF in HIV-infected individuals in an everyday clinical setting. METHODS: A single-center study at the HIV-outpatient clinic at Copenhagen University Hospital, Rigshospitalet. Study period from January 1, 2004-June 1, 2015...
May 5, 2017: Nephron
https://www.readbyqxmd.com/read/28465101/drug-like-property-driven-optimization-of-4-substituted-1-5-diarylanilines-as-potent-hiv-1-non-nucleoside-reverse-transcriptase-inhibitors-against-rilpivirine-resistant-mutant-virus
#5
Lei Wei, Hui-Ling Wang, Li Huang, Chin-Ho Chen, Susan L Morris-Natschke, Kuo-Hsiung Lee, Lan Xie
On the basis of our prior structure-activity relationship (SAR) results, our current lead optimization of 1,5-diarylanilines (DAANs) focused on the 4-substituent (R(1)) on the central phenyl ring as a modifiable position related simultaneously to improved drug resistance profiles and drug-like properties. Newly synthesized p-cyanovinyl-DAANs (8a-8g) with different R(1) side chains plus prior active p-cyanoethyl-DAANs (4a-4c) were evaluated not only for anti-HIV potency against both wild-type HIV virus and rilpivirine-resistant (E138K, E138K+M184I) viral replication, but also for multiple drug-like properties, including aqueous solubility, lipophilicity, and metabolic stability in human liver microsomes and human plasma...
April 22, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28449051/viral-kinetics-in-semen-with-different-antiretroviral-families-in-treatment-na%C3%A3-ve-hiv-infected-patients-a-randomized-trial
#6
Alicia Gutierrez-Valencia, Omar J Benmarzouk-Hidalgo, Inmaculada Rivas-Jeremías, Nuria Espinosa, María Trujillo-Rodríguez, Tamara Fernandez-Magdaleno, Pompeyo Viciana, Luis F López-Cortés
Background: There are several regimens for starting antiretroviral treatment, but it remains unknown whether either of them is more advantageous regarding the time course and magnitude of HIV-RNA decay in semen. Objective: To evaluate the differential effect of different antiretroviral drug families on viral kinetics in seminal plasma of treatment-naïve HIV-infected patients. Methods: Phase II, randomized, open-label study in which participants were randomized 1:1:1 to receive tenofovir-DF plus emtricitabine, and either cobicistat-boosted elvitegravir (EVGcobi), rilpivirine (RPV), or ritonavir-boosted darunavir (DRVrtv)...
April 25, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28408657/negative-regulation-of-human-pregnane-x-receptor-by-microrna-18a-5p-evidence-for-suppression-of-microrna-18a-5p-expression-by-rifampin-and-rilpivirine
#7
Devinder Sharma, Abdullah A Turkistani, Wenjun Chang, Catherine Hu, Zhaoming Xu, Thomas K H Chang
Small non-coding microRNAs act as post-transcriptional regulators of gene expression involved in diverse biological functions. Pregnane X receptor (PXR, NR1I2), which is a member of the superfamily of nuclear receptors, is a transcription factor governing the transport and biotransformation of various endobiotics and xenobiotics. In the present study, we identified a specific microRNA involved in regulating the expression and functionality of human PXR (hPXR). According to bioinformatics analysis employing three commonly used algorithms (TargetScan, miRanda, and DIANA-microT-CDS), miR-18a-5p was predicted to be the top candidate microRNA regulator of hPXR...
April 13, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28402970/the-genotyping-resistance-profile-of-the-pol-gene-detected-in-blood-of-newly-diagnosed-hiv-positive-men-is-durably-archived-in-the-gut-whatever-the-time-of-initiation-of-cart
#8
Anne Emmanuelle Depincé, Elodie Dussert, Delphine Vergnon-Miszczycha, Abdelaye Keita, Sylvie Pillet, Elisabeth Botelho-Nevers, Anne Frésard, Amandine Gagneux-Brunon, Frédéric R Lucht, Xavier Roblin, Bruno Pozzetto, Stéphane Paul, Thomas Bourlet
OBJECTIVE: To evaluate the mutational patterns on the pol gene of the main HIV-1 strain archived in cell genome of 10 chronically infected men according to their clinical and therapeutic history. The genotyping resistance profiles were compared between the first blood plasma available at the time of HIV diagnosis and rectal biopsies and PBMC sampled 1-5 years after the initiation of combined antiretroviral therapy (cART). METHODS: HIV-1 RNA and cell-associated HIV-1 DNA were quantified by Abbott Real-Time HIV-1 and Generic HIV® DNA cell (Biocentric) assays...
April 13, 2017: Intervirology
https://www.readbyqxmd.com/read/28369542/variable-endothelial-cell-function-restoration-after-initiation-of-two-antiretroviral-regimens-in-hiv-infected-individuals
#9
P Echeverría, E Gómez-Mora, S Roura, A Bonjoch, J Puig, N Pérez-Alvarez, A Bayés-Genís, B Clotet, J Blanco, E Negredo
Background: The effect of ART on endothelial cell function is incompletely characterized. Methods: We performed a 24 week prospective, case-control and comparative pilot study of ART-naive HIV-infected patients who started a darunavir- or rilpivirine-based regimen, matched with non-HIV-infected volunteers, to compare changes at week 24 from baseline in levels of circulating endothelial cells (CECs), endothelial progenitor cells (EPCs) and circulating angiogenic cells, as well as changes in immune-activation markers...
March 22, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28368868/universal-antiretroviral-regimens-thinking-beyond-one-pill-once-a-day
#10
Jeffrey M Jacobson, Charles Flexner
PURPOSE OF REVIEW: Poor adherence to oral antiretroviral treatment in a subpopulation of persons with HIV-1 infection interferes with the potential success of the drug regimens in treating the infection. Here, we review long-acting antiretroviral strategies currently in clinical development that could prove useful for the treatment of HIV-1 infection in individuals not succeeding with short-acting oral regimens. RECENT FINDINGS: Pharmaceutical nanotechnology has succeeded in creating two novel long-acting injectable antiretroviral compounds, carbotegravir and rilpivirine, which have completed early clinical trials demonstrating the safety, tolerability and prolonged antiretroviral activity...
March 31, 2017: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/28368071/long-acting-agents-for-hiv-infection-biological-aspects-role-in-treatment-and-prevention-and-patient-s-perspective
#11
Stefano Rusconi, Simone Marcotullio, Antonella Cingolani
Current cART regimens are highly potent and well tolerated, but long-term toxicities, drug-drug interactions, lifetime costs and scarce option for multiclass failed patients could limit the efficacy of treatment itself. Long-acting formulations of antiretrovirals, which could potentially replace daily tablets, have been developed and are under investigation for prevention and treatment of HIV infection. Cabotegravir and rilpivirine represent the first drugs studied in this context. The aim of this review is to summarize the biological bases, the available information on completed and ongoing clinical trials and the potential development of long-acting regimens for the treatment and prevention of HIV infection...
April 3, 2017: New Microbiologica
https://www.readbyqxmd.com/read/28303548/long-acting-antiretrovirals-where-are-we-now
#12
REVIEW
Amesika N Nyaku, Sean G Kelly, Babafemi O Taiwo
PURPOSE OF REVIEW: Current HIV treatment options require daily use of combination antiretroviral drugs. Many persons living with HIV experience treatment fatigue and suboptimal adherence as a result. Long-acting antiretroviral drugs are being developed to expand options for HIV treatment. Here, we review the agents in development, and evaluate data from recent clinical trials. In addition, we anticipate challenges to successful widespread use of long-acting antiretrovirals. RECENT FINDINGS: Parenteral nanosuspensions of cabotegravir and rilpivirine, and dapivirine vaginal ring are the farthest in clinical development...
April 2017: Current HIV/AIDS Reports
https://www.readbyqxmd.com/read/28279181/a-mature-macrophage-is-a-principal-hiv-1-cellular-reservoir-in-humanized-mice-after-treatment-with-long-acting-antiretroviral-therapy
#13
Mariluz Araínga, Benson Edagwa, R Lee Mosley, Larisa Y Poluektova, Santhi Gorantla, Howard E Gendelman
BACKGROUND: Despite improved clinical outcomes seen following antiretroviral therapy (ART), resting CD4+ T cells continue to harbor latent human immunodeficiency virus type one (HIV-1). However, such cells are not likely the solitary viral reservoir and as such defining where and how others harbor virus is imperative for eradication measures. To such ends, we used HIV-1ADA-infected NOD.Cg-Prkdc (scid) Il2rg (tm1Wjl) /SzJ mice reconstituted with a human immune system to explore two long-acting ART regimens investigating their abilities to affect viral cell infection and latency...
March 9, 2017: Retrovirology
https://www.readbyqxmd.com/read/28276283/novel-fused-pyrimidine-and-isoquinoline-derivatives-as-potent-hiv-1-nnrtis-a-patent-evaluation-of-wo2016105532a1-wo2016105534a1-and-wo2016105564a1
#14
REVIEW
Dongwei Kang, Zhipeng Huo, Gaochan Wu, Jiabao Xu, Peng Zhan, Xinyong Liu
In the three patent applications, the impact of changing the pyrimidine core of the rilpivirine (RPV) to a variety of alternative fused cores was explored, culminating in the identification of a series of conformationally restricted compounds with comparable potencies against WT and mutant HIV-1 strains with those of efavirenz (EFV) and RPV, and higher security in the Human Ether-a-go-go-Related Gene (hERG) assay. Areas covered: The present review provides a fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs, and highlights the conformational restriction strategies in the development of NNRTIs...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28259777/switching-from-tenofovir-disoproxil-fumarate-to-tenofovir-alafenamide-coformulated-with-rilpivirine-and-emtricitabine-in-virally-suppressed-adults-with-hiv-1-infection-a-randomised-double-blind-multicentre-phase-3b-non-inferiority-study
#15
Chloe Orkin, Edwin DeJesus, Moti Ramgopal, Gordon Crofoot, Peter Ruane, Anthony LaMarca, Anthony Mills, Bernard Vandercam, Joseph de Wet, Jürgen Rockstroh, Adriano Lazzarin, Bart Rijnders, Daniel Podzamczer, Anders Thalme, Marcel Stoeckle, Danielle Porter, Hui C Liu, Andrew Cheng, Erin Quirk, Devi SenGupta, Huyen Cao
BACKGROUND: Tenofovir alafenamide, a tenofovir prodrug, results in 90% lower tenofovir plasma concentrations than does tenofovir disproxil fumarate, thereby minimising bone and renal risks. We investigated the efficacy, safety, and tolerability of switching to a single-tablet regimen containing rilpivirine, emtricitabine, and tenofovir alafenamide compared with remaining on rilpivirine, emtricitabine, and tenofovir disoproxil fumarate. METHODS: In this randomised, double-blind, multicentre, placebo-controlled, non-inferiority trial, HIV-1-infected adults were screened and enrolled at 119 hospitals in 11 countries in North America and Europe...
March 1, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28259776/switching-from-efavirenz-emtricitabine-and-tenofovir-disoproxil-fumarate-to-tenofovir-alafenamide-coformulated-with-rilpivirine-and-emtricitabine-in-virally-suppressed-adults-with-hiv-1-infection-a-randomised-double-blind-multicentre-phase-3b-non-inferiority
#16
Edwin DeJesus, Moti Ramgopal, Gordon Crofoot, Peter Ruane, Anthony LaMarca, Anthony Mills, Claudia T Martorell, Joseph de Wet, Hans-Jürgen Stellbrink, Jean-Michel Molina, Frank A Post, Ignacio Pérez Valero, Danielle Porter, YaPei Liu, Andrew Cheng, Erin Quirk, Devi SenGupta, Huyen Cao
BACKGROUND: Tenofovir alafenamide is a prodrug that reduces tenofovir plasma concentrations by 90% compared with tenofovir disoproxil fumarate, thereby decreasing bone and renal risks. The coformulation of rilpivirine, emtricitabine, and tenofovir alafenamide has recently been approved, and we aimed to investigate the efficacy, safety, and tolerability of switching to this regimen compared with remaining on coformulated efavirenz, emtricitabine, and tenofovir disoproxil fumarate. METHODS: In this randomised, double-blind, placebo-controlled, non-inferiority trial, HIV-1-infected adults were enrolled at 120 hospitals and outpatient clinics in eight countries in North America and Europe...
March 1, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28222098/multicenter-study-of-skin-rashes-and-hepatotoxicity-in-antiretroviral-na%C3%A3-ve-hiv-positive-patients-receiving-non-nucleoside-reverse-transcriptase-inhibitor-plus-nucleoside-reverse-transcriptase-inhibitors-in-taiwan
#17
Pei-Ying Wu, Chien-Yu Cheng, Chun-Eng Liu, Yi-Chien Lee, Chia-Jui Yang, Mao-Song Tsai, Shu-Hsing Cheng, Shih-Ping Lin, De-Yu Lin, Ning-Chi Wang, Yi-Chieh Lee, Hsin-Yun Sun, Hung-Jen Tang, Chien-Ching Hung
OBJECTIVES: Two nucleos(t)ide reverse-transcriptase inhibitors (NRTIs) plus 1 non-NRTI (nNRTI) remain the preferred or alternative combination antiretroviral therapy (cART) for antiretroviral-naive HIV-positive patients in Taiwan. The three most commonly used nNRTIs are nevirapine (NVP), efavirenz (EFV) and rilpivirine (RPV). This study aimed to determine the incidences of hepatotoxicity and skin rashes within 4 weeks of initiation of cART containing 1 nNRTI plus 2 NRTIs. METHODS: Between June, 2012 and November, 2015, all antiretroviral-naive HIV-positive adult patients initiating nNRTI-containing cART at 8 designated hospitals for HIV care were included in this retrospective observational study...
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
#18
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/28207816/hiv-drug-therapy-duration-a-swedish-real-world-nationwide-cohort-study-on-infcarehiv-2009-2014
#19
Amanda Häggblom, Stefan Lindbäck, Magnus Gisslén, Leo Flamholc, Bo Hejdeman, Andreas Palmborg, Amy Leval, Eva Herweijer, Sverrir Valgardsson, Veronica Svedhem
BACKGROUND: As HIV infection needs a lifelong treatment, studying drug therapy duration and factors influencing treatment durability is crucial. The Swedish database InfCareHIV includes high quality data from more than 99% of all patients diagnosed with HIV infection in Sweden and provides a unique opportunity to examine outcomes in a nationwide real world cohort. METHODS: Adult patients who started a new therapy defined as a new 3rd agent (all antiretrovirals that are not N[t]RTIs) 2009-2014 with more than 100 observations in treatment-naive or treatment-experienced patients were included...
2017: PloS One
https://www.readbyqxmd.com/read/28198203/enteral-administration-of-twice-daily-dolutegravir-and-rilpivirine-as-a-part-of-a-triple-therapy-regimen-in-a-critically-ill-patient-with-hiv
#20
Sarah Lynn Turley, Patricia Pecora Fulco
The administration of antiretroviral therapy (ART) in intubated critically ill patients may be challenging. Limited pharmacokinetic data exist characterizing the effects of crushed ART with subsequent enteral administration on antiretroviral drug concentrations or the clinical impact on HIV virologic suppression. We report a case of a 27-year-old HIV-positive male with presumed multidrug-resistant HIV and a diagnosis of lymphoma who required enteral ART administration after intensive care unit admission. Crushed twice-daily dolutegravir (separated from enteral nutrition by 2 hours) and rilpivirine (concurrently with a bolus feed) were administered via an orogastric tube...
January 1, 2017: Journal of the International Association of Providers of AIDS Care
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