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NNRTI HIV

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https://www.readbyqxmd.com/read/28738474/-hiv-1-drug-resistance-transmission-threshold-survey-in-dehong-prefecture-of-yunnan-province-2015
#1
M Chen, J B Wang, H Xing, Y L Ma, J Yang, H C Chen, S T Yao, H B Luo, X Duan, Y K Wang, S Duan, M H Jia
Objective: To study the HIV-1 drug resistance transmission level in HIV infected persons receiving no antiviral therapy in Dehong prefecture of Yunnan province in 2015. Methods: A total of 72 plasma samples were collected from recently reported HIV-infected persons aged 16-25 years in Dehong from January to July 2015 for drug resistance gene detection. Results: Forty eight samples were successfully sequenced and analyzed. Among them, 31.2% (15/48) were from Chinese, and 68.8% (33/48) were from Burmese. Based on pol sequences, HIV genotypes included URF (52...
July 10, 2017: Zhonghua Liu Xing Bing Xue za Zhi, Zhonghua Liuxingbingxue Zazhi
https://www.readbyqxmd.com/read/28732792/drug-resistance-in-b-and-non-b-subtypes-amongst-subjects-recently-diagnosed-as-primary-recent-or-chronic-hiv-infected-over-the-period-2013-2016-impact-on-susceptibility-to-first-line-strategies-including-integrase-strand-transfer-inhibitors
#2
Samantha Andreis, Monica Basso, Renzo Scaggiante, Mario Cruciani, Roberto Ferretto, Vinicio Manfrin, Sandro Panese, Maria Cristina Rossi, Ermenegildo Francavilla, Caterina Boldrin, Mario Alvarez, Federico Dal Bello, Carlo Mengoli, Ombretta Turriziani, Loredana Sarmati, Guido Antonelli, Massimo Andreoni, Giorgio Palu, Saverio Giuseppe Parisi
OBJECTIVES: to characterize the prevalence of transmitted drug resistance mutations (TDRMs) by plasma analysis of 750 patients at the time of HIV diagnosis from January 1, 2013 to November, 16, 2016 in the Veneto region (Italy), where all drugs included in the recommended first line therapies were prescribed, included integrase strand transfer inhibitors (InNSTI). METHODS: TDRMs were defined according to the Stanford HIV database algorithm. RESULTS: Subtype B was the most prevalent HIV clade (67...
July 18, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28722475/ann-qsar-workflow-for-predicting-the-inhibition-of-hiv-1-reverse-transcriptase-by-pyridinone-non-nucleoside-derivatives
#3
Abolfazl Barzegar, Elham Zamani-Gharehchamani, Ali Kadkhodaie-Ilkhchi
AIM: Pyridinone derivatives have high potency against non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant human immunodeficiency virus type-1 strains. Quantitative structure-activity relationship (QSAR) studies on a series of pyridinone derivatives acting as NNRTIs are very important in designing the next generation of NNRTIs. Methodology & results: The QSAR models were developed using linear (single and forward stepwise) and combined nonlinear artificial neural network (ANN) approaches...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28715160/meeting-the-who-90-target-antiretroviral-treatment-efficacy-in-poland-is-associated-with-baseline-clinical-patient-characteristics
#4
Milosz Parczewski, Ewa Siwak, Magdalena Leszczyszyn-Pynka, Iwona Cielniak, Ewa Burkacka, Piotr Pulik, Adam Witor, Karolina Muller, Ewelina Zasik, Anna Grzeszczuk, Maria Jankowska, Małgorzata Lemańska, Anita Olczak, Edyta Grąbczewska, Aleksandra Szymczak, Jacek Gąsiorowski, Bartosz Szetela, Monika Bociąga-Jasik, Paweł Skwara, Magdalena Witak-Jędra, Elżbieta Jabłonowska, Kamila Wójcik-Cichy, Juliusz Kamerys, Małgorzata Janczarek, Dagny Krankowska, Tomasz Mikuła, Katarzyna Kozieł, Dariusz Bielec, Justyna Stempkowska, Aleksandra Kocbach, Wiesława Błudzin, Andrzej Horban
INTRODUCTION: Modern combined antiretroviral therapies (cART) allow to effectively suppress HIV-1 viral load, with the 90% virologic success rate, meeting the WHO target in most clinical settings. The aim of this study was to analyse antiretroviral treatment efficacy in Poland and to identify variables associated with virologic suppression. M: ethods Cross-sectional data on 5152 (56.92% of the countrywide treated at the time-point of analysis) patients on cART for more than six months with at least one HIV-RNA measurement in 2016 were collected from 14 Polish centres...
July 17, 2017: Journal of the International AIDS Society
https://www.readbyqxmd.com/read/28696229/mdr1-and-bcrp-transporter-mediated-drug-drug-interaction-between-rilpivirine-and-abacavir-effect-on-intestinal-absorption
#5
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/28692532/cardiovascular-outcomes-among-hiv-infected-veterans-receiving-atazanavir-a-us-national-historical-cohort-study
#6
Joanne Lafleur, Adam P Bress, Lisa Rosenblatt, Jacob Crook, Paul E Sax, Joel Myers, Corey Ritchings
OBJECTIVE: Patients with HIV infection have an increased risk of cardiovascular disease compared with uninfected individuals. Antiretroviral therapy with atazanavir delays progression of atherosclerosis markers; whether this reduces cardiovascular disease event risk compared with other antiretroviral regimens is currently unknown. DESIGN: Population-based, non-interventional, historical cohort study conducted from July 1, 2003, through December 31, 2015. SETTING: Veterans Health Administration (VHA) hospitals and clinics throughout the United States...
July 7, 2017: AIDS
https://www.readbyqxmd.com/read/28690229/-hiv-resistance-in-men-who-have-sex-with-men-a-meta-analysis
#7
Lin Yang, Ruiwei Xu, Guanglu Zhao, Tiejian Feng, Pingcheng Hu
To assess the prevalence of HIV primary drug resistance and drug resistance gene mutations among men who have sex with men (MSM).
 Methods: We searched eight electronic databases (CNKI, VIP, CBM, Wanfang Database, PubMed, Web of Knowledge, Springer, Medline) for the studies of HIV drug resistance relevant to MSM. Drug resistance and drug resistance mutations data were pooled and analyzed according to statistical test of homogeneity. Subgroups were further divided according to sample size, location, race, quality rating score, sampling time...
June 28, 2017: Zhong Nan da Xue Xue Bao. Yi Xue Ban, Journal of Central South University. Medical Sciences
https://www.readbyqxmd.com/read/28690189/efavirenz-what-is-known-about-the-cellular-mechanisms-responsible-for-its-adverse-effects
#8
REVIEW
Nadezda Apostolova, Ana Blas-Garcia, Maria J Galindo, Juan V Esplugues
The HIV infection remains an important health problem worldwide. However, due to the efficacy of combined antiretroviral therapy (cART), it has ceased to be a mortal condition, becoming a chronic disease instead. Efavirenz, the most prescribed non-nucleoside analogue reverse transcriptase inhibitor (NNRTI), has been a key component of cART since its commercialization in 1998. Though still a drug of choice in many countries, its primacy has been challenged by the arrival of newer antiretroviral agents with better toxicity profiles and treatment adherence...
July 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28689453/switching-to-the-single-tablet-regimen-of-elvitegravir-cobicistat-emtricitabine-and-tenofovir-df-from-non-nucleoside-reverse-transcriptase-inhibitor-plus-coformulated-emtricitabine-and-tenofovir-df-regimens-week-96-results-of-strategy-nnrti
#9
Anton Pozniak, Jason Flamm, Andrea Antinori, Mark Bloch, Douglas Ward, Juan Berenguer, Pierre Cote, Kristen Andreatta, William Garner, Javier Szwarcberg, Thai Nguyen-Cleary, Damian J McColl, David Piontkowsky
BACKGROUND: HIV-1-infected, virologically suppressed adults wanting to simplify or change their non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens may benefit from switching to the single-tablet regimen of elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate (E/C/F/TDF). OBJECTIVE: We examined differences in the proportion of participants with HIV-1 RNA < 50 copies/mL (Snapshot analysis), change in CD4 cell count, safety, and patient-reported outcomes in participants switching to E/C/F/TDF from an NNRTI + FTC/TDF (TVD) regimen...
July 9, 2017: HIV Clinical Trials
https://www.readbyqxmd.com/read/28688977/prevalence-of-drug-resistance-among-hiv-1-treatment-naive-patients-in-greece-during-2003-2015-transmitted-drug-resistance-is-due-to-onward-transmissions
#10
D Paraskevis, E Kostaki, G Magiorkinis, P Gargalianos, G Xylomenos, E Magiorkinis, M Lazanas, M Chini, G Nikolopoulos, A Skoutelis, V Papastamopoulos, A Antoniadou, A Papadopoulos, M Psichogiou, G L Daikos, M Oikonomopoulou, A Zavitsanou, G Chrysos, V Paparizos, S Kourkounti, H Sambatakou, N V Sipsas, M Lada, P Panagopoulos, E Maltezos, S Drimis, A Hatzakis
BACKGROUND: The prevalence of HIV-1 drug resistance among treatment-naïve patients ranges between 8.3% and 15% in Europe and North America. Previous studies showed that subtypes A and B were the most prevalent in the Greek HIV-1 epidemic. Our aim was to estimate the prevalence of resistance among drug naïve patients in Greece and to investigate the levels of transmission networking among those carrying resistant strains. METHODS: HIV-1 sequences were determined from 3428 drug naïve HIV-1 patients, in Greece sampled during 01/01/2003-30/6/2015...
July 5, 2017: Infection, Genetics and Evolution
https://www.readbyqxmd.com/read/28685686/hiv-1-non-nucleoside-reverse-transcriptase-inhibitors-sar-and-lead-optimization-using-comfa-and-comsia-studies-1995-2016
#11
Murugesan Vanangamudi, Vasanthanathan Poongavanam, Vigneshwaran Namasivayam
BACKGROUND: Design of inhibitors for HIV-1 reverse transcriptase inhibition (HIV-1 RT) is one of the successful chemotherapy for the treatment of HIV infection. Among the inhibitors available for HIV-1 RT, non-nucleoside reverse transcriptase inhibitors (NNRTIs) have shown to be very promising and clinically approved drug. However, the efficiency of many of these drugs has been reduced by the drug-resistant variants of HIV-1 RT. The aim of the current review is to provide a summary of lead optimization strategies from the 3D-QSARs studies on NNRTI class from the past 21 years (1995 to 2016) Methods: The conformation dependent-alignment based (CoMFA and CoMSIA) methods have been proven very successful ligand based strategy in the drug design...
July 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28673027/pretreatment-hiv-drug-resistance-results-in-virological-failure-and-accumulation-of-additional-resistance-mutations-in-ugandan-children
#12
Cissy Kityo, Ragna S Boerma, Kim C E Sigaloff, Elizabeth Kaudha, Job C J Calis, Victor Musiime, Sheila Balinda, Rita Nakanjako, T Sonia Boender, Peter N Mugyenyi, Tobias F Rinke de Wit
Background: Pretreatment HIV drug resistance (PDR) can impair virological response to ART, jeopardizing effective treatment for children. Methods: Children aged ≤12 years initiated first-line ART in Uganda during 2010-11. Baseline and 6 monthly viral load (VL) and genotypic resistance testing if VL >1000 copies/mL was done. The 2015 IAS-USA mutation list and Stanford algorithm were used to score drug resistance mutations (DRMs) and susceptibility. Virological failure (VF) was defined as two consecutive VLs >1000 copies/mL or death after 6 months of ART...
June 30, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28652115/longitudinal-trends-of-hiv-drug-resistance-in-a-large-canadian-cohort-1996-2016
#13
Genevieve Rocheleau, Chanson J Brumme, Jeannie Shoveller, Viviane Lima, Richard Harrigan
OBJECTIVES: We aim to identify long-term trends in HIV drug resistance before and after combined antiretroviral therapy (cART) initiation. METHODS: IAS-USA (2015) mutations were identified in 23,271 HIV protease-reverse transcriptase sequences from 6543 treatment naïve British Columbia adults. Participants that started cART between 1996-2014 were followed until April 2016. Equality of proportions test compared the percentage of participants with acquired drug resistance (ADR) or transmitted drug resistance (TDR) in 1996, to those in 2014...
June 23, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/28650382/hiv-drug-resistance-in-infants-increases-with-changing-pmtct-regimens
#14
Lisa K Poppe, Catherine Chunda-Liyoka, Eun Hee Kwon, Clement Gondwe, John T West, Chipepo Kankasa, Clement B Ndongmo, Charles Wood
OBJECTIVES: The objectives of this study were to determine HIV drug resistance prevalence in Zambian infants upon diagnosis, and to determine how changing prevention of mother-to-child transmission (PMTCT) regimens affect drug resistance. DESIGN: Dried blood spot (DBS) samples from infants in the Lusaka District of Zambia, obtained during routine diagnostic screening, were collected during four different years representing three different PMTCT treatment regimens...
June 23, 2017: AIDS
https://www.readbyqxmd.com/read/28649306/decreasing-prevalence-of-transmitted-drug-resistance-among-art-naive-hiv-1-infected-patients-in-iceland-1996-2012
#15
Malik Sallam, Gülşen Özkaya Şahin, Hlynur Indriðason, Joakim Esbjörnsson, Arthur Löve, Anders Widell, Magnus Gottfreðsson, Patrik Medstrand
Introduction: Resistance to antiretroviral drugs can complicate the management of HIV-1 infection and impair control of its spread. The aim of the current study was to investigate the prevalence and transmission of HIV-1 drug resistance among 106 antiretroviral therapy (ART)-naïve patients diagnosed in Iceland (1996-2012). Methods: HIV-1 polymerase sequences were analysed using the Calibrated Population Resistance tool. Domestic spread of transmitted drug resistance (TDR) was investigated through maximum likelihood and Bayesian approaches...
2017: Infection Ecology & Epidemiology
https://www.readbyqxmd.com/read/28628528/increased-persistence-of-initial-treatment-for-hiv-infection-with-modern-antiretroviral-therapy
#16
Thibaut Davy-Mendez, Joseph J Eron, Oksana Zakharova, David A Wohl, Sonia Napravnik
BACKGROUND: Initiating antiretroviral therapy (ART) early improves clinical outcomes and prevents transmission. Guidelines for first-line therapy have changed with the availability of newer ART agents. In this study, we compared persistence and virologic response to initial ART according to the class of anchor agent used. SETTING: An observational clinical cohort study in the Southeastern United States. METHODS: All HIV-infected patients participating in the UNC Center for AIDS Research Clinical Cohort (UCHCC) and initiating ART between 1996 and 2014 were included...
June 15, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28627486/the-association-between-detected-drug-resistance-mutations-and-cd4-t-cell-decline-in-hiv-positive-individuals-maintained-on-a-failing-treatment-regimen
#17
Anna Schultze, Roger Paredes, Caroline Sabin, Andrew N Phillips, Deenan Pillay, Nicola Mackie, Antonella Castagna, David Chadwick, Karolin Falconer, Anna Maria Geretti, Frank A Post, Teresa Hill, Ole Kirk, Anton Pozniak, Mark Nelson, Anna Tostevin, David Dunn, Jens Lundgren, Alessandro Cozzi-Lepri
BACKGROUND: To analyse the effect of drug resistance mutations (DRM) on CD4 cell trends in HIV-positive people maintained on virologically failing antiretroviral therapy (ART). METHODS: Individuals from two large cohorts experiencing virological failure (VF) while maintained on ART with >1 CD4 count and >1 resistance test were included. CD4 cell slopes were estimated using linear mixed models. Principal component analysis (PCA) was used to assess the effect of clusters of mutations, defined using extracted component based scores from the PCA, on CD4 cell decline...
June 19, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28600625/an-intravaginal-ring-that-releases-three-antiviral-agents-and-a-contraceptive-blocks-shiv-rt-infection-reduces-hsv-2-shedding-and-suppresses-hormonal-cycling-in-rhesus-macaques
#18
Nina Derby, Meropi Aravantinou, Jessica Kenney, Shweta R Ugaonkar, Asa Wesenberg, Jolanta Wilk, Larisa Kizima, Aixa Rodriguez, Shimin Zhang, Olga Mizenina, Keith Levendosky, Michael L Cooney, Samantha Seidor, Agegnehu Gettie, Brooke Grasperge, James Blanchard, Michael Piatak, Jeffrey D Lifson, José Fernández-Romero, Thomas M Zydowsky, Melissa Robbiani
Women globally need access to multipurpose prevention technologies (MPTs) that prevent human immunodeficiency virus (HIV), sexually transmitted infections that increase HIV acquisition/transmission risk, and unintended pregnancy. Seeking an MPT with activity against HIV, herpes simplex virus-2 (HSV-2), and human papillomavirus (HPV), we developed a prototype intravaginal ring (IVR), the MZCL IVR, which released the antiviral agents MIV-150, zinc acetate, and carrageenan (MZC for short) and the contraceptive levonorgestrel (LNG)...
June 9, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28589720/development-of-a-sp-2-sp-3-stille-cross-coupling-for-rapid-synthesis-of-hiv-nnrti-doravirine-analogues
#19
Abdellatif ElMarrouni, Mark Campbell, James J Perkins, Antonella Converso
The development of a C(sp(2))-C(sp(3)) cross-coupling reaction for rapid, parallel synthesis of analogues of two HIV NNRTI clinical candidates is described. This method allowed easy access to the C-ring space using a practical alkylation with commercially available tributyl(iodomethyl)stannane followed by a palladium-catalyzed coupling with a variety of aryl halides (I, Br) in the presence of copper chloride. Optimization and scope of this method are reported.
June 7, 2017: Organic Letters
https://www.readbyqxmd.com/read/28589513/prevalence-of-hiv-1-transmitted-drug-resistance-in-recently-infected-treatment-na%C3%A3-ve-persons-in-the-southwest-of-iran-2014-2015
#20
Shokouh Ghafari, Arash Memarnejadian, Alireza Samarbaf-Zadeh, Ehsan Mostafavi, Manoochehr Makvandi, Shokrolah Salmanzadeh, Ata Ghadiri, Michael R Jordan, Elham Mousavi, Fatemeh Jahanbakhsh, Kayhan Azadmanesh
The emergence and transmission of drug resistant HIV mutants is a major concern, especially in resource-limited countries with expanding antiretroviral therapy. Studies have recently reported the prevalence of HIV-1 transmitted drug resistance (TDR) mutations in certain Iranian cities; however, no information is currently available about the level of TDR, as well as the nature of the circulating HIV-1 subtypes, in the Southwestern bordering province of Iran, Khuzestan. Herein, we used a WHO-recommended TDR survey method to classify the prevalence of TDR in indigenous people of Khuzestan province...
June 6, 2017: Archives of Virology
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