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https://www.readbyqxmd.com/read/29232276/contemporary-protease-inhibitors-and-cardiovascular-risk
#1
Jens Lundgren, Amanda Mocroft, Lene Ryom
PURPOSE OF REVIEW: To review the evidence linking use of HIV protease inhibitors with excess risk of cardiovascular disease (CVD) in HIV+ populations. RECENT FINDINGS: For the two contemporary most frequently used protease inhibitors, darunavir and atazanavir [both pharmacologically boosted with ritonavir (/r)], darunavir/r has been shown to be associated with increased CVD risk. The effect is cumulative with longer exposure increasing risk and an effect size comparable to what has been observed for previously developed protease inhibitors...
December 9, 2017: Current Opinion in Infectious Diseases
https://www.readbyqxmd.com/read/29226149/role-of-p-glycoprotein-inhibitors-in-the-bioavailability-enhancement-of-solid-dispersion-of-darunavir
#2
Saleha Rehman, Bushra Nabi, Mohammad Fazil, Saba Khan, Naimat Kalim Bari, Romi Singh, Shavej Ahmad, Varinder Kumar, Sanjula Baboota, Javed Ali
Objective: The aim of the present study was to improve bioavailability of an important antiretroviral drug, Darunavir (DRV), which has low water solubility and poor intestinal absorption through solid dispersion (SD) approach incorporating polymer with P-glycoprotein inhibitory potential. Methods: A statistical approach where design of experiment (DoE) was used to prepare SD of DRV with incorporation of P-glycoprotein inhibitors. Using DoE, different methods of preparation, like melt, solvent evaporation, and spray drying method, utilizing carriers like Kolliphor TPGS and Soluplus were evaluated...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29216346/darunavir-ritonavir-monotherapy-at-a-low-dose-600-100%C3%A2-mg-day-in-hiv-1-infected-individuals-with-suppressed-hiv-viraemia
#3
S Seang, L Schneider, T Nguyen, M P Lê, C Soulie, R Calin, F Caby, M-A Valantin, R Tubiana, L Assoumou, A-G Marcelin, G Peytavin, C Katlama
Background: Darunavir/ritonavir is a potent PI with a high genetic barrier and pharmacological robustness favourably investigated as monotherapy. Whether darunavir could be dose reduced in the context of monotherapy deserves investigation. Methods: Patients with HIV suppressed viraemia (plasma viral load <50 copies/mL for 12 months) under ART who had switched to darunavir/ritonavir monotherapy at 600/100 mg/day between 2013 and 2015 were included in this observational 48 week single-centre study...
December 5, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29212044/multi-spectroscopic-and-molecular-docking-studies-on-the-interaction-of-darunavir-a-hiv-protease-inhibitor-with-calf-thymus-dna
#4
Jie-Hua Shi, Kai-Li Zhou, Yan-Yue Lou, Dong-Qi Pan
Molecular interaction of darunavir (DRV), a HIV protease inhibitor with calf thymus deoxyribonucleic acid (ct-DNA) was studied in physiological buffer (pH7.4) by multi-spectroscopic approaches hand in hand with viscosity measurements and molecular docking technique. The UV absorption and fluorescence results together revealed the formation of a DRV-ct-DNA complex having binding affinities of the order of 103M-1, which was more in keeping with the groove binding. The results that DRV bound to ct-DNA via groove binding mode was further evidenced by KI quenching studies, viscosity measurements, competitive binding investigations with EB and Rhodamine B and CD spectral analysis...
November 29, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29210626/short-term-cost-and-efficiency-analysis-of-raltegravir-versus-atazanavir-ritonavir-or-darunavir-ritonavir-for-treatment-naive-adults-with-hiv-1-infection-in-spain
#5
Ashley E Davis, Anita J Brogan, Bridgett Goodwin, Gonzalo Nocea, Virginia Lozano
INTRODUCTION: The AIDS Clinical Trial Group (ACTG) 5257 clinical trial showed that raltegravir (RAL) was superior to atazanavir/ritonavir (ATV/r) and darunavir/ritonavir (DRV/r), when used in combination with emtricitabine/tenofovir DF (FTC/TDF), in a 96-week composite endpoint combining virologic efficacy and tolerability for treatment-naive adults with HIV-1 infection. This study aimed to estimate the efficiency associated with these three regimens in Spain. METHODS: An economic model was developed to estimate costs for antiretroviral drugs, adverse event management, and HIV care for individuals initiating first-line therapy...
November 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/29210336/simplification-to-dual-therapy-containing-lamivudine-and-darunavir-ritonavir-or-atazanavir-ritonavir-in-hiv-infected-patients-on-virologically-suppressive-antiretroviral-therapy
#6
Leonardo Calza, Matteo Cafaggi, Vincenzo Colangeli, Marco Borderi, Enrico Barchi, Massimiliano Lanzafame, Stefano Nicole', Anna Maria Degli Antoni, Isabella Bon, Maria Carla Re, Pierluigi Viale
BACKGROUND: The ritonavir-boosted protease inhibitor (PI/r)-based dual regimens are warranted in order to optimize the combination antiretroviral therapy (cART), prevent the long-term toxicity and reduce the cost of treatments. METHODS: We performed an observational, retrospective study of HIV-infected patients on suppressive antiretroviral therapy who switched to a dual regimen containing lamivudine (3TC) plus darunavir/ritonavir (DRV/r) 800/100 mg qd or atazanavir/ritonavir (ATV/r) 300/100 mg qd...
December 6, 2017: Infectious Diseases
https://www.readbyqxmd.com/read/29210076/in-vitro-effect-of-antiretroviral-drugs-on-cultured-primary-astrocytes-analysis-of-neurotoxicity-and-matrix-metalloproteinase-inhibition
#7
Tiziana Latronico, Ilaria Pati, Rossana Ciavarella, Anna Fasano, Fabio Mengoni, Miriam Lichtner, Vincenzo Vullo, Claudio Maria Mastroianni, Grazia Maria Liuzzi
There is little information available on the possible toxic effects that antiretroviral (ARV) drugs used for the treatment of human immunodeficiency virus (HIV)-infected subjects, may have on the central nervous system (CNS) resident cells. Moreover, it is unclear whether the efficacy of the ARV drugs may also be due to their ability to exert extravirological effects on factors responsible for the development of HIV brain injury, e.g. matrix metalloproteinases (MMPs). This study investigates the toxicity of three different ARV drugs and on their ability to modulate levels and expression of gelatinases A (MMP-2) and B (MMP-9) in astrocytes...
December 6, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29189101/pharmacokinetics-and-pharmacodynamics-of-the-nucleoside-sparing-dual-regimen-containing-rilpivirine-plus-darunavir-ritonavir-in-treatment-na%C3%A3-ve-hiv-1-infected-individuals
#8
Akil Jackson, Laura Else, Christopher Higgs, Zeenat Karolia, Saye Khoo, David Back, Emma Devitt, Anton Pozniak, Marta Boffito
BACKGROUND: We aimed at investigating the antiviral activity and the pharmacokinetics of the dual antiretroviral (ARV) combination of rilpivirine plus darunavir/ritonavir 25/800/100 mg once-daily in naïve HIV-1-infected individuals (NHII) with different baseline viral loads. SETTINGS: Pharmacokinetic/pharmacodynamics study in ARV-naïve HIV-infected individuals. METHODS: The primary endpoint was the number of NHII with HIV-RNA < 40 copies/mL at week 48...
November 30, 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/29161288/switch-to-maraviroc-with-darunavir-r-both-qd-in-patients-with-suppressed-hiv-1-was-well-tolerated-but-virologically-inferior-to-standard-antiretroviral-therapy-48-week-results-of-a-randomized-trial
#9
Barbara Rossetti, Roberta Gagliardini, Genny Meini, Gaetana Sterrantino, Vincenzo Colangeli, Maria Carla Re, Alessandra Latini, Manuela Colafigli, Francesca Vignale, Stefano Rusconi, Valeria Micheli, Antonio Di Biagio, Giancarlo Orofino, Valeria Ghisetti, Alessandra Fantauzzi, Vincenzo Vullo, Pierfrancesco Grima, Daniela Francisci, Claudio Mastroianni, Andrea Antinori, Michele Trezzi, Lucia Lisi, Pierluigi Navarra, Benedetta Canovari, Antonella D'Arminio Monforte, Silvia Lamonica, Alessandro D'Avino, Maurizio Zazzi, Simona Di Giambenedetto, Andrea De Luca
OBJECTIVES: Primary study outcome was absence of treatment failure (virological failure, VF, or treatment interruption) per protocol at week 48. METHODS: Patients on 3-drug ART with stable HIV-1 RNA <50 copies/mL and CCR5-tropic virus were randomized 1:1 to maraviroc with darunavir/ritonavir qd (study arm) or continue current ART (continuation arm). RESULTS: In June 2015, 115 patients were evaluable for the primary outcome (56 study, 59 continuation arm)...
2017: PloS One
https://www.readbyqxmd.com/read/29159965/improvement-in-lipids-after-switch-to-boosted-atazanavir-or-darunavir-in-children-adolescents-with-perinatally-acquired-hiv-on-older-protease-inhibitors-results-from-the-pediatric-hiv-aids-cohort-study
#10
J Jao, W Yu, K Patel, T L Miller, B Karalius, M E Geffner, L A DiMeglio, A Mirza, J S Chen, M Silio, E J McFarland, R B Van Dyke, D Jacobson
OBJECTIVES: Dyslipidaemia is common in perinatally HIV-infected (PHIV) youth receiving protease inhibitors (PIs). Few studies have evaluated longitudinal lipid changes in PHIV youth after switch to newer PIs. METHODS: We compared longitudinal changes in fasting lipids [total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), and TC:HDL-C ratio] in PHIV youth enrolled in the Pediatric HIV/AIDS Cohort Study (PHACS) Adolescent Master Protocol (AMP) study who switched to atazanavir/ritonavir (ATV/r)- or darunavir/ritonavir (DRV/r)-based antiretroviral therapy (ART) from an older PI-based ART and those remaining on an older PI...
November 21, 2017: HIV Medicine
https://www.readbyqxmd.com/read/29143565/hiv-1-resistance-rarely-observed-in-subjects-using-darunavir-once-daily-regimens-across-clinical-studies
#11
Erkki Lathouwers, Eric Y Wong, Donghan Luo, Sareh Seyedkazemi, Sandra De Meyer, Kimberley Brown
BACKGROUND: Darunavir 800 mg once daily (QD) is indicated for HIV-1-infected treatment-naïve and treatment-experienced (without darunavir resistance-associated mutations [RAMs]) individuals, and has been evaluated in phase 2/3 studies with durations between 48 and 192 weeks. OBJECTIVE: To summarize the development (or identification) of post-baseline resistance (RAMs and antiretroviral phenotypic susceptibility) among subjects receiving darunavir QD dosing. METHODS: Seven phase 2/3 studies with available genotypes/phenotypes for subjects treated with ritonavir- or cobicistat-boosted darunavir 800 mg QD regimens were assessed: ARTEMIS (NCT00258557; n = 343), GS-US-299-0102 (NCT01565850; n = 153), GS-US-216-0130 (NCT01440569; n = 313), ODIN (NCT00524368; n = 294), INROADS (NCT01199939; n = 54), MONET (NCT00458302; n = 256), and PROTEA (NCT01448707; n = 273)...
November 16, 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/29140932/characteristics-of-treatment-experienced-hiv-infected-african-children-and-adolescents-initiating-darunavir-and-or-etravirine-based-antiretroviral-treatment
#12
Bethany Corrigan, Irene Mukui, Lloyd Mulenga, Nobuhle Mthethwa, Mosilinyane Letsie, Stephanie Bruno, Natella Rakhmanina
BACKGROUND: Data are limited on the selection and sequencing of second and third-line pediatric antiretroviral treatment (ART) in resource-limited settings. This study aimed to evaluate characteristics of African pediatric patients initiated on darunavir (DRV) and/or etravirine (ETR) through a specific drug donation program. METHODS: This was a cross-sectional study of baseline immunologic, virologic and demographic characteristics of children and adolescents initiating DRV- and/or ETR-based ART...
November 14, 2017: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/29135577/protease-inhibitors-and-preterm-delivery-another-piece-in-the-puzzle
#13
Graziella Favarato, Claire L Townsend, Heather Bailey, Helen Peters, Pat Tookey, Graham P Taylor, Claire Thorne
BACKGROUND: Questions remain regarding preterm delivery (PTD) risk in HIV-infected women on antiretroviral therapy (ART), including the role of ritonavir-boosted protease inhibitors (PI/r), timing of ART initiation and immune status. METHODS: We examined data from the UK/Ireland National Study of HIV in Pregnancy and Childhood on women with HIV delivering a singleton live infant in 2007-2015, including those pregnancies receiving PI/r-based (n=4184) or non-nucleoside reverse transcriptase inhibitors (NNRTI)-based regimens (n = 1889)...
November 10, 2017: AIDS
https://www.readbyqxmd.com/read/29110408/design-synthesis-biological-evaluation-and-x-ray-studies-of-hiv-1-protease-inhibitors-with-modified-p2-ligands-of-darunavir
#14
Arun K Ghosh, W Sean Fyvie, Margherita Brindisi, Melinda Steffey, Johnson Agniswamy, Yuan-Fang Wang, Manabu Aoki, Masayuki Amano, Irene T Weber, Hiroaki Mitsuya
The structure-based design, synthesis, and biological evaluation of a series of nonpeptidic HIV-1 protease inhibitors with rationally designed P2' ligands are described. The inhibitors are designed to enhance backbone binding interactions, particularly at the S2'-subsite. Synthesis of inhibitors was carried out efficiently. The stereochemistry of alcohol functionalities of the P2'-ligands was set by asymmetric reduction of the corresponding ketone using (R,R)- or (S,S)-Noyori's catalysts. A number of inhibitors displayed very potent enzyme inhibitory and antiviral activity...
November 6, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29106584/plasma-trough-concentrations-of-antiretrovirals-in-hiv-infected-persons-treated-with-direct-acting-antiviral-agents-for-hepatitis-c-in-the-real-world
#15
Massimo Tempestilli, Gabriele Fabbri, Ilaria Mastrorosa, Laura Timelli, Stefania Notari, Rita Bellagamba, Raffaella Libertone, Federico Lupi, Mauro Zaccarelli, Andrea Antinori, Chiara Agrati, Adriana Ammassari
Background: Possible drug-drug interactions (DDIs) between antiretrovirals (ARVs) and direct-acting antiviral agents (DAAs) are of some concern. Objectives: To investigate ARV plasma trough concentrations (Ctrough) before and during DAAs in patients treated in the real world. Methods: Single-centre, prospective, observational study including HIV/HCV coinfected persons undergoing DAA treatment. Self-reported adherence was assessed and ARVs Ctrough measured by HPLC-UV...
November 2, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29105160/strength-in-amalgamation-newer-combination-agents-for-hiv-and-implications-for-practice
#16
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/29097142/exploring-the-feasibility-of-the-use-of-biopolymers-as-a-carrier-in-the-formulation-of-amorphous-solid-dispersions-part-i-gelatin
#17
Timothy Pas, Bjorn Vergauwen, Guy Van den Mooter
Biopolymers have rarely been used so far as carriers in the formulation of amorphous solid dispersions (ASD) to overcome poor solubility of active pharmaceutical ingredients (APIs). In an attempt to enlarge our knowledge on this topic, gelatin, type 50PS was selected. A screening study was initiated in which twelve structurally different poorly soluble biopharmaceutical classification system (BCS) Class II drugs (carbamazepine, cinnarizine, diazepam, itraconazole, nifedipine, indomethacin, darunavir (ethanolate), ritonavir, fenofibrate, griseofulvin, ketoconazole and naproxen) were selected for evaluation...
October 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29096670/hiv-treatment-simplification-to-elvitegravir-cobicistat-emtricitabine-tenofovir-disproxil-fumarate-e-c-f-tdf-plus-darunavir-a-pharmacokinetic-study
#18
Marianne Harris, Bruce Ganase, Birgit Watson, P Richard Harrigan, Julio S G Montaner, Mark W Hull
BACKGROUND: As a simplification strategy for treatment-experienced HIV-infected patients who have achieved virologic suppression on a multi-drug, multi-class antiretroviral regimen, the aim of this study was to evaluate the safety, efficacy, and pharmacokinetics of once-daily elvitegravir/cobicistat/emtricitabine/tenofovir disproxil fumarate (E/C/F/TDF) with darunavir. METHODS: A single arm, open-label 48-week study was conducted of regimen simplification to E/C/F/TDF plus darunavir 800 mg daily from stable therapy including two nucleoside/nucleotide reverse transcriptase inhibitors, a ritonavir-boosted protease inhibitor, and an integrase inhibitor...
November 2, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/29082041/ritonavir-boosted-darunavir-plus-two-nucleoside-reverse-transcriptase-inhibitors-versus-other-regimens-for-initial-antiretroviral-therapy-for-people-with-hiv-infection-a-systematic-review
#19
REVIEW
Tatevik Balayan, Hacsi Horvath, George W Rutherford
BACKGROUND: Darunavir is a second-generation protease-inhibitor used with ritonavir (DRV/r) and two nucleoside reverse-transcriptase inhibitors as an option in first-line antiretroviral treatment (ART). METHODS: We systematically reviewed randomized controlled trials (RCTs) of DRV/r versus other regimens in patients initiating ART. We searched five bibliographic databases and other key resources. We had no language limitations. We assessed bias risk with the Cochrane tool and used GRADE to assess evidence quality...
2017: AIDS Research and Treatment
https://www.readbyqxmd.com/read/29077926/no-impact-of-hiv-1-protease-minority-resistant-variants-on-the-virological-response-to-a-first-line-pi-based-regimen-containing-darunavir-or-atazanavir
#20
Marine Perrier, Benoit Visseaux, Roland Landman, Véronique Joly, Eve Todesco, Yazdan Yazdanpanah, Vincent Calvez, Anne-Geneviève Marcelin, Diane Descamps, Charlotte Charpentier
Objectives: To evaluate, in a clinical cohort of HIV-1-infected patients, the prevalence of PI minority resistant variants (MRV) at ART baseline and their impact on the virological response to a first-line PI-based regimen. Patients and methods: In an observational single-centre cohort, we assessed all ART-naive patients initiating a first-line regimen including two NRTI and one boosted PI, darunavir/ritonavir or atazanavir/ritonavir, between January 2012 and March 2015...
October 25, 2017: Journal of Antimicrobial Chemotherapy
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