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https://www.readbyqxmd.com/read/28097091/evaluation-of-novel-protease-inhibitors-against-darunavir-resistant-variants-of-hiv-type-1
#1
Mari Inoue, Daiki Oyama, Koushi Hidaka, Masanori Kameoka
HIV disease became a manageable chronic disease since combination antiretroviral therapy (cART) was introduced as the standard treatment regimen. However, the emergence of drug-resistant viruses is a major problem associated with cART. A phenotypic drug susceptibility test using a lentiviral vector was established and applied to evaluate new protease inhibitors (PIs). Lentiviral vectors representing a wild-type (WT-lentivector) and darunavir (DRV)-resistant HIV type 1 (HIV-1) (DRV (r)-lentivector) were generated...
January 2017: FEBS Open Bio
https://www.readbyqxmd.com/read/28096973/a-fission-yeast-cell-based-system-for-multidrug-resistant-hiv-1-proteases
#2
Zsigmond Benko, Dong Liang, Ge Li, Robert T Elder, Anindya Sarkar, Jun Takayama, Arun K Ghosh, Richard Y Zhao
BACKGROUND: HIV-1 protease (PR) is an essential enzyme for viral production. Thus, PR inhibitors (PIs) are the most effective class of anti-HIV drugs. However, the main challenge to the successful use of PI drugs in patient treatment is the emergence of multidrug resistant PRs (mdrPRs). This study aimed to develop a fission yeast cell-based system for rapid testing of new PIs that combat mdrPRs. RESULTS: Three mdrPRs were isolated from HIV-infected patients that carried seven (M7PR), ten (M10PR) and eleven (M11PR) PR gene mutations, respectively...
2017: Cell & Bioscience
https://www.readbyqxmd.com/read/28094565/the-decline-in-hiv-1-drug-resistance-in-heavily-antiretroviral-experienced-patients-is-associated-with-optimized-prescriptions-in-a-treatment-roll-out-program-in-mexico
#3
Juan J Calva, Silvana Larrea, Marco A Tapia-Maltos, Mauricio Ostrosky-Frid, Carolina Lara, Pedro Aguilar-Salinas, Héctor Rivera, Juan P Ramírez
A decrease in the rate of acquired antiretroviral (ARV) drug-resistance (ADR) over time has been documented in high-income settings, but data on the determinants of this phenomenon are lacking. We tested the hypothesis that in heavily ARV-experienced patients in the Mexican ARV therapy (ART) roll-out program, the drop in ADR would be associated with changes in ARV drug usage. Genotypic resistance tests obtained from 974 HIV-infected patients with virologic failure and at least 2 previously failed ARV regimens from throughout the country were analyzed for the presence of nRTI, NNRTI and PI resistance-associated mutations (RAMs)...
January 17, 2017: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/28065890/impact-of-obesity-on-antiretroviral-pharmacokinetics-and-immuno-virological-response-in-hiv-infected-patients-a-case-control-study
#4
Vincent Madelain, Minh P Le, Karen Champenois, Charlotte Charpentier, Roland Landman, Veronique Joly, Patrick Yeni, Diane Descamps, Yazdan Yazdanpanah, Gilles Peytavin
BACKGROUND: Obesity has high prevalence among HIV-infected patients. Increased adipose tissue mass affects the pharmacokinetics of numerous drugs, but few data are available for antiretroviral drugs. OBJECTIVES: In this study we aimed to explore the pharmacokinetics of antiretroviral drugs and the immuno-virological response in obese patients with HIV infection. PATIENTS AND METHODS: We examined data from 2009 to 2012 in our hospital's database for HIV-1-infected patients who received an antiretroviral drug (abacavir, emtricitabine, lamivudine, tenofovir, efavirenz, etravirine, nevirapine, atazanavir/ritonavir, darunavir/ritonavir, lopinavir/ritonavir or raltegravir)...
January 8, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28061820/associations-of-statins-and-antiretroviral-drugs-with-the-onset-of-type-2-diabetes-among-hiv-1-infected-patients
#5
Vincenzo Spagnuolo, Laura Galli, Andrea Poli, Stefania Salpietro, Nicola Gianotti, Piermarco Piatti, Francesca Cossarini, Concetta Vinci, Elisabetta Carini, Adriano Lazzarin, Antonella Castagna
BACKGROUND: Statin use is associated with a modest increase in the incidence of type 2 diabetes mellitus (DM) among the general population. However, HIV-infected patients have a higher risk of developing DM, and it is unclear whether statins have a diabetogenic effect in these patients. Therefore, we investigated the associations of statin use and exposure to antiretroviral drugs with type 2 DM onset in a cohort of HIV-infected patients. METHODS: This retrospective, controlled, cohort study identified HIV-1-infected patients who did not have DM and were not receiving statins at their antiretroviral treatment (ART) initiation...
January 7, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28034359/hiv-1-drug-susceptibility-to-potential-second-and-third-line-antiretroviral-regimens-among-cameroonian-patients-evidence-from-a-cross-sectional-design
#6
Aubin J Nanfack, Desire Takou, Joseph Fokam, Romina Salpini, Maria M Santoro, Giulia Cappelli, Martin Baane, Suzie M Tetang, Josef Eberle, Lutz Gürtler, Francesca Ceccherini-Silberstein, Judith N Torimiro, Vittorio Colizzi, Carlo-Federico Perno, Alexis Ndjolo
BACKGROUND: Scale-up of antiretroviral therapy (ART) and the growing number of long-term treated patients may favor multi-HIV drug resistance (HIVDR) in resource-limited settings. Understanding the burden of HIVDR with ART-exposure may provide new insights for an effective long-term management of infected patients. METHODS: Sixty-six HIV-infected individuals (18 ART-naïve, 24 failing first-line, 24 failing second-line ART) living in Yaoundé-Cameroon were evaluated by sequencing protease-reverse transcriptase (PR-RT, n=62), envelope-V3 loop (V3, n=58) and integrase (IN, n=30) regions...
December 29, 2016: Current HIV Research
https://www.readbyqxmd.com/read/28010730/from-antiretroviral-therapy-access-to-provision-of-third-line-regimens-evidence-of-hiv-drug-resistance-mutations-to-first-and-second-line-regimens-among-ugandan-adults
#7
Ivan Namakoola, Ivan Kasamba, Billy N Mayanja, Patrick Kazooba, Joseph Lutaakome, Fred Lyagoba, Anne A Kapaata, Pontiano Kaleebu, Paula Munderi
BACKGROUND: HIV care programs in resource-limited settings have hitherto concentrated on antiretroviral therapy (ART) access, but HIV drug resistance is emerging. In a cross-sectional study of HIV-positive adults on ART for ≥6 months enrolled into a prospective cohort in Uganda, plasma HIV RNA was measured and genotyped if ≥1000 copies/ml. Identified Drug resistance mutations (DRMs) were interpreted using the Stanford database, 2009 WHO list of DRMs and the IAS 2014 update on DRMs, and examined and tabulated by ART drug classes...
December 23, 2016: BMC Research Notes
https://www.readbyqxmd.com/read/28008867/dolutegravir-plasma-concentrations-according-to-companion-antiretroviral-drug-unwanted-drug-interaction-or-desirable-boosting-effect
#8
Dario Cattaneo, Davide Minisci, Valeria Cozzi, Agostino Riva, Paola Meraviglia, Emilio Clementi, Massimo Galli, Cristina Gervasoni
BACKGROUND: Studies in healthy volunteers have shown that the recently approved HIV integrase inhibitor dolutegravir has limited drug-to-drug interaction profile. Here we carried out a pharmacokinetic survey in HIV-infected patients given dolutegravir as part of their antiretroviral therapy. METHODS: Dolutegravir plasma trough concentrations were measured in 78 HIV infected patients given the drug in combination with a protease inhibitor, a non nucleoside reverse transcriptase inhibitor or abacavir/lamivudine...
December 23, 2016: Antiviral Therapy
https://www.readbyqxmd.com/read/27999051/pharmacokinetic-interactions-between-cobicistat-boosted-elvitegravir-and-darunavir-in-hiv-infected-patients
#9
Alicia Gutierrez-Valencia, Omar J Benmarzouk-Hidalgo, Silvia Llaves, Tamara Fernandez-Magdaleno, Nuria Espinosa, Pompeyo Viciana, Luis F Lopez-Cortes
OBJECTIVES: To evaluate if there are significant drug-drug interactions between cobicistat-boosted elvitegravir and 800 mg darunavir once daily taken simultaneously, as has been suggested previously. METHODS: The study population consisted of three groups of unselected volunteers taking a regimen of elvitegravir, cobicistat, emtricitabine and tenofovir disoproxil fumarate (150, 150, 200 and 300 mg, respectively) co-formulated in a single tablet plus 800 mg darunavir (group A); only co-formulated elvitegravir, cobicistat, emtricitabine and tenofovir disoproxil fumarate (group B); and cobicistat-boosted darunavir (800 mg darunavir + 150 mg cobicistat) plus two nucleos(t)ide analogues (group C)...
December 20, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27999009/use-of-a-physiologically-based-pharmacokinetic-model-to-simulate-drug-drug-interactions-between-antineoplastic-and-antiretroviral-drugs
#10
José Moltó, Rajith Rajoli, David Back, Marta Valle, Cristina Miranda, Andrew Owen, Bonaventura Clotet, Marco Siccardi
BACKGROUND: Co-administration of antineoplastics with ART is challenging due to potential drug-drug interactions (DDIs). However, trials specifically assessing such DDIs are lacking. Our objective was to simulate DDIs between the antineoplastics erlotinib and gefitinib with key antiretroviral drugs and to predict dose adjustments using a physiologically based pharmacokinetic (PBPK) model. METHODS: In vitro data describing chemical properties and pharmacokinetic processes of each drug and their effect on cytochrome P450 isoforms were obtained from the literature...
December 20, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27997522/second-and-third-line-antiretroviral-therapy-for-children-and-adolescents-a-scoping-review
#11
Erica Lazarus, Simone Nicol, Lisa Frigati, Martina Penazzato, Mark F Cotton, Elizabeth Centeno-Tablante, Avy Violari, Liesl Nicol
BACKGROUND: The World Health Organization (WHO) identified a need for evidence to inform revision of second and third-line antiretroviral therapy (ART) options in children failing ART. We performed an in-depth scoping review of all available literature on second and subsequent line ART regimens in children younger than 18 years. METHODS: We comprehensively searched, without language or date limitations, the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, EMBASE, the WHO International Clinical Trials Registry Platform and ClinicalTrials...
December 15, 2016: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/27997193/asymmetric-one-pot-synthesis-of-3r-3as-6ar-hexahydrofuro-2-3-b-furan-3-ol-a-key-component-of-current-hiv-protease-inhibitors
#12
Adrian Sevenich, Gong-Qing Liu, Anthony J Arduengo, B Frank Gupton, Till Opatz
A concise and efficient synthesis of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol, a key building block for several clinical and experimental HIV protease inhibitors including the highly important drug darunavir, was achieved via a one-pot procedure using furan and Cbz-protected glycol aldehyde as starting materials. A [2+2]-photocycloaddition between both reactants which can be prepared from wood-based starting materials according to the principles of xylochemistry, followed by hydrogenation and lipase-catalyzed kinetic resolution afforded the target compound in high yield and up to 99% ee...
January 4, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27993734/encapsulating-darunavir-nanocrystals-within-eudragit-l100-using-coaxial-electrospraying
#13
Duong Nhat Nguyen, Christian Clasen, Guy Van den Mooter
Electrospraying is renowned for its simplicity and versatility, and which can effectively produce particles with well-controlled size, size distribution, particle shape, morphology and microstructure at the nano/microscale. In this study, coaxial electrospraying was used to investigate its feasibility for preparing nanoparticles made up of nanocrystals encapsulated within a polymer shell. Firstly, aqueous nanosuspensions of darunavir were prepared by wet media milling. Then the nanosuspension and solutions of an enteric polymer, Eudragit L100, were used as the inner/core liquid and outer/shell liquid in a coaxial electorspraying setup, respectively...
December 16, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27992544/structural-studies-of-a-rationally-selected-multi-drug-resistant-hiv-1-protease-reveal-synergistic-effect-of-distal-mutations-on-flap-dynamics
#14
Johnson Agniswamy, John M Louis, Julien Roche, Robert W Harrison, Irene T Weber
We report structural analysis of HIV protease variant PRS17 which was rationally selected by machine learning to represent wide classes of highly drug-resistant variants. Crystal structures were solved of PRS17 in the inhibitor-free form and in complex with antiviral inhibitor, darunavir. Despite its 17 mutations, PRS17 has only one mutation (V82S) in the inhibitor/substrate binding cavity, yet exhibits high resistance to all clinical inhibitors. PRS17 has none of the major mutations (I47V, I50V, I54ML, L76V and I84V) associated with darunavir resistance, but has 10,000-fold weaker binding affinity relative to the wild type PR...
2016: PloS One
https://www.readbyqxmd.com/read/27984559/psychiatric-symptoms-in-patients-receiving-dolutegravir
#15
Anna Fettiplace, Chris Stainsby, Alan Winston, Naomi Givens, Sarah Puccini, Vani Vannappagari, Ricky Hsu, Jennifer Fusco, Romina Quercia, Michael Aboud, Lloyd Curtis
INTRODUCTION: Psychiatric symptoms are reported to occur frequently in people living with HIV and may be associated with specific antiretrovirals. We analysed psychiatric symptoms observed with dolutegravir and other frequently prescribed anchor drugs. METHODS: Selected psychiatric symptoms (insomnia, anxiety, depression, and suicidality) occurring in HIV-positive patients during dolutegravir treatment across 5 randomized clinical trials (3 double-blind), in the Observational Pharmaco-Epidemiology Research & Analysis (OPERA®) cohort, and among cases spontaneously reported to ViiV Healthcare were analysed...
December 7, 2016: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/27970765/cost-analysis-of-raltegravir-versus-atazanavir-r-or-darunavir-r-for-treatment-naive-adults-with-hiv-1-infection-in-spain
#16
A E Davis, A J Brogan, B B Goodwin, G Nocea, V Lozano
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27970763/budget-impact-analysis-of-the-introduction-of-darunavir-800-mg-qd-for-the-2nd-line-treatment-of-hiv-infected-treatment-experienced-adults-on-the-brazilian-national-hiv-program
#17
K A Ferreira, J A Neves, E Asano, L A Magno, R G Loureiro
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27923946/prevalence-of-antiretroviral-drug-resistance-in-patients-who-are-not-responding-to-protease-inhibitor-based-treatment-results-from-the-first-national-survey-in-south-africa
#18
K Steegen, M Bronze, M A Papathanasopoulos, G van Zyl, D Goedhals, C Van Vuuren, W Macleod, I Sanne, W S Stevens, S C Carmona
Limited data exist on human immunodeficiency virus type 1 (HIV-1) resistance in patients who are not responding to protease inhibitor (PI)-based regimens in resource-limited settings. This study assessed resistance profiles in adults across South Africa who were not responding to PI-based regimens. pol sequencing was undertaken and submitted to the Stanford HIV Drug Resistance Database. At least 1 major PI mutation was detected in 16.4% of 350 participants. A total of 53.4% showed intermediate resistance to darunavir/ritonavir, whereas high-level resistance was not observed...
December 15, 2016: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/27921997/comparative-molecular-dynamics-study-of-dimeric-and-monomeric-forms-of-hiv-1-protease-in-ligand-bound-and-unbound-state
#19
Monikaben Padariya, Umesh Kalathiya
Human immunodeficiency virus type 1 protease is a viral-encoded enzyme and it is essential for replication and assembly of the virus. Inactivation of HIV-1 protease causes production of immature, noninfectious viral particles and thus HIV-1 protease is an attractive target in anti-AIDS drug design. In our current work, we performed molecular dynamics (MD) calculations (500 ns) for two different ligands (COM5 - designed in our previous study, and Darunavir) and made effort to understand dynamics behaviour of our designed compound COM5...
December 6, 2016: General Physiology and Biophysics
https://www.readbyqxmd.com/read/27919899/pharmacokinetic-evaluation-of-darunavir-administered-once-or-twice-daily-in-combination-with-ritonavir-or-the-three-direct-acting-antiviral-regimen-of-ombitasvir-paritaprevir-ritonavir-and-dasabuvir-in-adults-co-infected-with-hepatitis-c-and-human-immunodeficiency
#20
Jennifer R King, Amit Khatri, Roger Trinh, Rolando M Viani, Bifeng Ding, Jiuhong Zha, Rajeev Menon
BACKGROUND: The three-direct acting antiviral (3D) regimen containing ombitasvir, paritaprevir, ritonavir and dasabuvir ± ribavirin (RBV) is approved for treatment of HCV GT1/HIV-1 co-infection. Results of a pharmacokinetic substudy of 3D and darunavir are presented. METHODS: HCV/HIV-1 infected subjects were randomized to maintain a darunavir 800 mg once daily (QD) or switch to a darunavir 600 mg twice daily (BID) based antiretroviral regimen. On Study Day 1, subjects received 3D and RBV plus darunavir for 12 weeks...
December 5, 2016: Antimicrobial Agents and Chemotherapy
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