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Rilpivirine

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https://www.readbyqxmd.com/read/28696229/mdr1-and-bcrp-transporter-mediated-drug-drug-interaction-between-rilpivirine-and-abacavir-effect-on-intestinal-absorption
#1
Josef Reznicek, Martina Ceckova, Zuzana Ptackova, Ondrej Martinec, Lenka Tupova, Lukas Cerveny, Frantisek Staud
Rilpivirine (TMC278) is a highly potent second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) representing an effective component of combination antiretroviral therapy (cART) in the treatment of HIV-positive patients. Many antiretroviral drugs commonly used in cART are substrates of ATP-binding cassette (ABC) and/or solute carrier (SLC) drug transporters and, therefore, prone to pharmacokinetic drug-drug interactions (DDIs). The aim of our study was to evaluate rilpivirine interactions with abacavir and lamivudine on selected ABC and SLC transporters in vitro and assess its importance for pharmacokinetics in vivoUsing accumulation assays in MDCK cells overexpressing selected ABC or SLC drug transporters we revealed rilpivirine as a potent inhibitor of MDR1 and BCRP, but not MRP2, OCT1, OCT2 or MATE1...
July 10, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28683720/rilpivirine-use-in-the-swiss-hiv-cohort-study-a-prospective-cohort-study
#2
Delphine Sculier, Angèle Gayet-Ageron, Manuel Battegay, Matthias Cavassini, Jan Fehr, Cedric Hirzel, Patrick Schmid, Enos Bernasconi, Alexandra Calmy
BACKGROUND: Rilpivirine is safe and effective in HIV-naïve patients with low baseline HIV-RNA or in switch strategy. It offers the advantages of few drug-drug interactions and a favourable toxicity profile. We aimed to determine the reasons for prescribing the rilpivirine (RPV)/tenofovir disoproxil (TDF)/emtricitabine (FTC) co-formulation within the Swiss HIV Cohort Study and to assess its effectiveness and safety over a 24 months period. METHODS: All individuals enrolled in the Swiss HIV Cohort Study who initiated a RPV/TDF/FTC co-formulation between April 2013 and March 2014 were included...
July 6, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28664942/darunavir-stands-up-as-preferred-hiv-protease-inhibitor
#3
Josep Mallolas
Current antiretroviral therapy reaches and maintains viral suppression over the years in more than 90% of treated HIV-infected individuals. Although integrase inhibitors are the preferred third agent in antiretroviral therapy in the current guidelines, rilpivirine, a non-nucleoside reverse transcrip- tase inhibitor, and darunavir (DRV), a second-generation protease inhibitor, are the preferred third companion to be used along with a backbone of two nucleos(t)ide reverse transcriptase inhibitors as first-line triple HIV combination treatment...
April 2017: AIDS Reviews
https://www.readbyqxmd.com/read/28650381/potential-for-immune-driven-viral-polymorphisms-to-compromise-antiretroviral-based-pre-exposure-prophylaxis-for-prevention-of-hiv-1-infection
#4
Hiroyuki Gatanaga, Zabrina L Brumme, Emily Adland, Gustavo Reyes-Terán, Santiago Avila-Rios, Carlos R Mejía-Villatoro, Tsunefusa Hayashida, Takayuki Chikata, Giang Van Tran, Kinh Van Nguyen, Rita I Meza, Elsa Y Palou, Humberto Valenzuela-Ponce, Juan M Pascale, Guillermo Porras-Cortés, Marvin Manzanero, Guinevere Q Lee, Jeffrey N Martin, Mary N Carrington, Mina John, Simon Mallal, Art F Y Poon, Philip Goulder, Masafumi Takiguchi, Shinichi Oka
OBJECTIVE: Long-acting rilpivirine is a candidate for pre-exposure prophylaxis (PrEP) for prevention of HIV-1 infection. However, rilpivirine resistance mutations at reverse transcriptase codon 138 (RT-E138X) occur naturally in a minority of HIV-1-infected persons; in particular those expressing Human Leukocyte Antigen (HLA)-B*18 where RT-E138X arises as an immune escape mutation. We investigate the global prevalence, B*18-linkage and replicative cost of RT-E138X and its regional implications for rilpivirine PrEP...
June 23, 2017: AIDS
https://www.readbyqxmd.com/read/28621159/dual-antiretroviral-therapy-for-hiv-infection
#5
Vicente Soriano
For two decades' triple combinations of antiretrovirals have been the standard treatment for HIV infection. The challenges of such lifelong therapy include long-term side effects, high costs and reduced drug adherence. The recent advent of more potent and safer antiretrovirals has renewed the interest for simpler HIV regimens. Areas covered: We discuss the pros and cons of dual antiretroviral therapies in both drug-naïve and in treatment-experienced patients with viral suppression (switch strategy). Expert Opinion: Some dual antiretroviral regimens are safe and efficacious, particularly as maintenance therapy...
June 16, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28598790/croi-2017-advances-in-antiretroviral-therapy
#6
Joyce Jones, Barbara S Taylor, Hong-Van Tieu, Timothy J Wilkin
The 2017 Conference on Retroviruses and Opportunistic Infections (CROI) featured exciting preclinical data on investigational antiretroviral agents with good in vitro efficacy and long half-lives. Investigational medications, including bictegravir, demonstrated excellent efficacy and tolerability, as did dual-agent therapy with dolutegravir paired with rilpivirine or with lamivudine. Dolutegravir monotherapy proved inadvisable due to virologic failure and resistance. The gap between high- and low-income settings along the HIV care continuum is narrowing, with Zimbabwe, Malawi, and Zambia approaching the 90-90-90 targets established by the joint United Nations Programme on HIV/AIDS (UNAIDS), whereas communities in the Southern United States are falling behind...
May 2017: Topics in Antiviral Medicine
https://www.readbyqxmd.com/read/28595298/lowered-rilpivirine-exposure-during-third-trimester-of-pregnancy-in-hiv-1-positive-women
#7
Stein Schalkwijk, Angela Colbers, Deborah Konopnicki, Andrea Gingelmaier, John Lambert, Marchina van der Ende, José Moltó, David Burger
Background: The use of antiretroviral therapy during pregnancy is important for control of maternal HIV disease and the prevention of perinatal HIV transmission. Physiological changes during pregnancy can reduce antiretroviral exposure. We studied the pharmacokinetics of rilpivirine 25 mg once daily (QD) in HIV-1-positive women during late pregnancy. Methods: We conducted a non-randomized, open-label, multi-centre, phase-IV study. HIV-positive pregnant women receiving rilpivirine 25 mg QD were included...
June 8, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28582463/drug-resistance-testing-through-remote-genotyping-and-predicted-treatment-options-in-human-immunodeficiency-virus-type-1-infected-tanzanian-subjects-failing-first-or-second-line-antiretroviral-therapy
#8
Jenny Svärd, Sabina Mugusi, Doreen Mloka, Ujjwal Neogi, Genny Meini, Ferdinand Mugusi, Francesca Incardona, Maurizio Zazzi, Anders Sönnerborg
INTRODUCTION: Antiretroviral therapy (ART) has been successfully introduced in low-middle income countries. However an increasing rate of ART failure with resistant virus is reported. We therefore described the pattern of drug resistance mutations at antiretroviral treatment (ART) failure in a real-life Tanzanian setting using the remote genotyping procedure and thereafter predicted future treatment options using rule-based algorithm and the EuResist bioinformatics predictive engine. According to national guidelines, the default first-line regimen is tenofovir + lamivudine + efavirenz, but variations including nevirapine, stavudine or emtricitabine can be considered...
2017: PloS One
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
#9
(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/28569550/ultra-deep-sequencing-analysis-on-hiv-drug-resistance-associated-mutations-among-hiv-infected-individuals-first-report-from-the-philippines
#10
Ivo N SahBandar, Genesis Samonte, Elizabeth Telan, Nalyn Siripong, Mahdi Belcaid, David Schanzenbach, Susan Leano, Haorile Chagan-Yasutan, Toshio Hattori, Cecilia M Shikuma, Lishomwa C Ndhlovu
A sharp increase in the number of people living with HIV has been documented in the Philippines. In response, the government has instituted antiretroviral therapy (ART) nationwide through HIV treatment hubs. However, no data presently exist on the status of ART drug-resistance-associated mutations (DRMs). In this study, we aim at analyzing DRM profiles in the Philippines and at providing comprehensive data on DRMs to guide treatment decisions and prevent viral failures. We conducted a cross-sectional study in 119 volunteers who tested positive for HIV from more than 8,000 participants screened for HIV across the nation through the 2013 Integrated HIV Behavioral and Serologic Surveillance (IHBSS) program...
July 5, 2017: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/28540638/in-silico-dose-prediction-for-long-acting-rilpivirine-and-cabotegravir-administration-to-children-and-adolescents
#11
Rajith K R Rajoli, David J Back, Steve Rannard, Caren Freel Meyers, Charles Flexner, Andrew Owen, Marco Siccardi
BACKGROUND AND OBJECTIVES: Long-acting injectable antiretrovirals represent a pharmacological alternative to oral formulations and an innovative clinical option to address adherence and reduce drug costs. Clinical studies in children and adolescents are characterised by ethical and logistic barriers complicating the identification of dose optimisation. Physiologically-based pharmacokinetic modelling represents a valuable tool to inform dose finding prior to clinical trials. The objective of this study was to simulate potential dosing strategies for existing long-acting injectable depot formulations of cabotegravir and rilpivirine in children and adolescents (aged 3-18 years) using physiologically-based pharmacokinetic modelling...
May 24, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28507107/in-vitro-cross-resistance-profiles-of-rilpivirine-dapivirine-and-miv-150-nonnucleoside-reverse-transcriptase-inhibitor-microbicides-in-clinical-development-for-the-prevention-of-hiv-1-infection
#12
Nicholas S Giacobbi, Nicolas Sluis-Cremer
Rilpivirine (RPV), dapivirine (DPV), and MIV-150 are in development as microbicides. It is not known whether they will block infection of circulating nonnucleoside reverse transcriptase inhibitor (NNRTI)-resistant human immunodeficiency virus type 1 (HIV-1) variants. Here, we demonstrate that the activity of DPV and MIV-150 is 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...
July 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
#13
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
#14
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
#15
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
#16
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...
June 15, 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
#17
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
#18
Devinder Sharma, Abdullah A Turkistani, Wenjun Chang, Catherine Hu, Zhaoming Xu, Thomas K H Chang
Small noncoding microRNAs act as post-transcriptional regulators of gene expression involved in diverse biologic functions. Pregnane X receptor (PXR, NR1I2), a member of the superfamily of nuclear receptors, is a transcription factor governing the transport and biotransformation of various drugs and other chemicals. In the present study, we identified a specific microRNA (miR) 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...
July 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
#19
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
#20
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
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