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Etravirine

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https://www.readbyqxmd.com/read/29201980/experimental-data-of-co-crystals-of-etravirine-and-l-tartaric-acid
#1
Mikal Rekdal, Aravind Pai, Muddukrishna Bs
Etravirine is a drug used alongside other medication in the treatment of HIV and is a non-nucleoside reverse transcriptase inhibitor. It is a BCS class IV drug, having low solubility and high permeability (Drugbank, https://www.drugbank.ca/drugs/DB06414) [1]. As a result, large doses of the drug are required for treatment. Two pills have to be taken twice a day, making it a "pill burden" (Intelence, http://www.intelence.com/hcp/dosing/administration-options) [2]. Therefore, attempts of co-crystallizing Etravirine are attractive as the solubility of the drug tends to increase in this solid form (Schultheiss and Newman, 2009) [3]...
February 2018: Data in Brief
https://www.readbyqxmd.com/read/29192124/drugs-and-scaffold-that-inhibit-cytochrome-p450-27a1-cyp27a1-in-vitro-and-in-vivo
#2
Morrie Lam, Natalia Mast, Irina Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency due to genetic mutations is detrimental to human health, whereas 50% of activity retention is not and does not affect the whole body cholesterol levels. CYP27A1 is considered as a potential therapeutic target in breast cancer and age-related neurodegenerative diseases; however CYP27A1 inhibition should be 50%. Herein, 131 pharmaceuticals were tested for their effect on CYP27A1-mediated cholesterol 27-hydroxylation by in vitro enzyme assay...
November 30, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29156381/structure-based-methods-to-predict-mutational-resistance-to-diarylpyrimidine-non-nucleoside-reverse-transcriptase-inhibitors
#3
Syeda Maryam Azeem, Alecia N Muwonge, Nehaben Thakkar, Kristina W Lam, Kathleen M Frey
Resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) is a leading cause of HIV treatment failure. Often included in antiviral therapy, NNRTIs are chemically diverse compounds that bind an allosteric pocket of enzyme target reverse transcriptase (RT). Several new NNRTIs incorporate flexibility in order to compensate for lost interactions with amino acid conferring mutations in RT. Unfortunately, even successful inhibitors such as diarylpyrimidine (DAPY) inhibitor rilpivirine are affected by mutations in RT that confer resistance...
November 9, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29140932/characteristics-of-treatment-experienced-hiv-infected-african-children-and-adolescents-initiating-darunavir-and-or-etravirine-based-antiretroviral-treatment
#4
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/28987601/design-synthesis-and-anti-hiv-evaluation-of-novel-diarylpyridine-derivatives-as-potent-hiv-1-nnrtis
#5
Zhaoqiang Liu, Ye Tian, Jinghan Liu, Boshi Huang, Dongwei Kang, Erik De Clercq, Dirk Daelemans, Christophe Pannecouque, Peng Zhan, Xinyong Liu
As a continuation of our efforts to discover and develop "me-better" drugs of DAPYs, novel diarylpyridine derivatives were designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. The majority of these compounds showed high activity against wild-type HIV-1 strain (IIIB) with EC50 values in the range of 0.04-4.41 μM. Among them, compound 5b2 (EC50 = 0.04 μM, SI = 3963) was the most potent. This compound showed anti-HIV-1IIIB activity superior than of Nevirapine but still inferior than of Etravirine...
July 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28959444/efficacy-of-raltegravir-etravirine-and-darunavir-ritonavir-for-treatment-experienced-hiv-patients-from-a-non-urban-clinic-population-in-the-united-states
#6
Andrew M Ebers, Yusra Alkabab, Brian Wispelwey, Rebecca Dillingham, Xin-Qun Wang, Julie Schexnayder, Scott K Heysell
BACKGROUND: The regimen of raltegravir (RAL), ritonavir-boosted darunavir (DAR/r), and etravirine (ETR) for HIV treatment-experienced patients in a non-clinical trial setting in the rural/semi-urban United States had not been evaluated. OBJECTIVE: A retrospective cohort analysis was performed of adult patients prescribed the regimen from 2008 to 2013 at a HIV clinic serving such a population. RESULTS: In all, 51 patients met inclusion criteria including 15 with suppressed viral loads at regimen initiation...
September 2017: Therapeutic Advances in Infectious Disease
https://www.readbyqxmd.com/read/28931682/susceptibility-of-human-endogenous-retrovirus-type-k-to-reverse-transcriptase-inhibitors
#7
Rafael Contreras-Galindo, Derek Dube, Koh Fujinaga, Mark H Kaplan, David M Markovitz
Human endogenous retroviruses (HERVs) make up 8% of the human genome. The HERV type K (HERV-K) HML-2 (HK2) family contains proviruses that are the most recent entrants into the human germ line and are transcriptionally active. In HIV-1 infection and cancer, HK2 genes produce retroviral particles that appear to be infectious, yet the replication capacity of these viruses and potential pathogenicity has been difficult to ascertain. In this report, we screened the efficacy of commercially available reverse transcriptase inhibitors (RTIs) at inhibiting the enzymatic activity of HK2 RT and HK2 genomic replication...
December 1, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28872867/multidrug-anti-hiv-amorphous-solid-dispersions-nature-and-mechanisms-of-impacts-of-drugs-on-each-other-s-solution-concentrations
#8
Hale Çiğdem Arca, Laura I Mosquera-Giraldo, Durga Dahal, Lynne S Taylor, Kevin J Edgar
Drug therapy has been instrumental in prolonging the lives of patients infected by human immunodeficiency virus (HIV). In order to combat development of resistance, therapies involving three or more drugs in combination are recommended by the World Health Organization (WHO) to suppress HIV and prevent development of acquired immune deficiency syndrome (AIDS). It is desirable for multidrug combinations to be coformulated into single dosage forms where possible, to promote patient convenience and adherence to dosage regimens, for which amorphous solid dispersion (ASD) is particularly well-suited...
November 6, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28802690/nanoparticle-releasing-nanofiber-composites-for-enhanced-in%C3%A2-vivo-vaginal-retention
#9
Emily A Krogstad, Renuka Ramanathan, Christina Nhan, John C Kraft, Anna K Blakney, Shijie Cao, Rodney J Y Ho, Kim A Woodrow
Current approaches for topical vaginal administration of nanoparticles result in poor retention and extensive leakage. To overcome these challenges, we developed a nanoparticle-releasing nanofiber delivery platform and evaluated its ability to improve nanoparticle retention in a murine model. We individually tailored two components of this drug delivery system for optimal interaction with mucus, designing (1) mucoadhesive fibers for better retention in the vaginal tract, and (2) PEGylated nanoparticles that diffuse quickly through mucus...
November 2017: Biomaterials
https://www.readbyqxmd.com/read/28770176/inhibition-of-plasmodium-hepatic-infection-by-antiretroviral-compounds
#10
Marta Machado, Margarida Sanches-Vaz, João P Cruz, António M Mendes, Miguel Prudêncio
Recent WHO guidelines on control of human immunodeficiency virus (HIV) call for the widespread use of antiretroviral (AR) therapy (ART) for people living with HIV. Given the considerable overlap between infections by HIV and Plasmodium, the causative agent of malaria, it is important to understand the impact of AR compounds and ART regimens on infections by malaria parasites. We undertook a systematic approach to identify AR drugs and ART drug combinations with inhibitory activity against the obligatory hepatic stage of Plasmodium infection...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28753637/collaborative-update-of-a-rule-based-expert-system-for-hiv-1-genotypic-resistance-test-interpretation
#11
Roger Paredes, Philip L Tzou, Gert van Zyl, Geoff Barrow, Ricardo Camacho, Sergio Carmona, Philip M Grant, Ravindra K Gupta, Raph L Hamers, P Richard Harrigan, Michael R Jordan, Rami Kantor, David A Katzenstein, Daniel R Kuritzkes, Frank Maldarelli, Dan Otelea, Carole L Wallis, Jonathan M Schapiro, Robert W Shafer
INTRODUCTION: HIV-1 genotypic resistance test (GRT) interpretation systems (IS) require updates as new studies on HIV-1 drug resistance are published and as treatment guidelines evolve. METHODS: An expert panel was created to provide recommendations for the update of the Stanford HIV Drug Resistance Database (HIVDB) GRT-IS. The panel was polled on the ARVs to be included in a GRT report, and the drug-resistance interpretations associated with 160 drug-resistance mutation (DRM) pattern-ARV combinations...
2017: PloS One
https://www.readbyqxmd.com/read/28750647/high-level-of-hiv-1-drug-resistance-mutations-in-patients-with-unsuppressed-viral-loads-in-rural-northern-south-africa
#12
Elizabeth M Etta, Lufuno Mavhandu, Cecile Manhaeve, Keanan McGonigle, Patrick Jackson, David Rekosh, Marie-Louise Hammarskjold, Pascal O Bessong, Denis M Tebit
BACKGROUND: Combination antiretroviral therapy (cART) has significantly reduced HIV morbidity and mortality in both developed and developing countries. However, the sustainability of cART may be compromised by the emergence of viral drug resistance mutations (DRM) and the cellular persistence of proviruses carrying these DRM. This is potentially a more serious problem in resource limited settings. METHODS: DRM were evaluated in individuals with unsuppressed viral loads after first or multiple lines of cART at two sites in rural Limpopo, South Africa...
July 27, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28653971/addition-of-etravirine-does-not-enhance-the-initial-decline-of-hiv-1-rna-in-treatment-experienced-patients-receiving-raltegravir
#13
Philippe Flandre, Anne-Geneviève Marcelin, Vincent Calvez
OBJECTIVE: The importance of an early reduction of HIV-1 RNA as a marker for positive longer term outcome is still under debate. We investigate whether antiretroviral-experienced patients receiving raltegravir plus etravirine have a higher early reduction of HIV-1 RNA compared with patients receiving raltegravir. DESIGN: An observational study of treatment-experienced patients. METHODS: The objective is to investigate 349 patients included in a raltegravir resistance study...
August 1, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
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
#14
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/28520611/treatment-outcomes-of-third-line-antiretroviral-regimens-in-hiv-infected-thai-adolescents
#15
Wasana Prasitsuebsai, Jiratchaya Sophonphan, Kulkanya Chokephaibulkit, Jurai Wongsawat, Suparat Kanjanavanit, Pope Kosalaraksa, Chaiwat Ngampiyakul, Pakarat Sangkla, Rawiwan Hansudewechakul, Stephen J Kerr, Thanyawee Puthanakit, Jintanat Ananworanich
BACKGROUND: Efficacy and safety data of third-line antiretroviral (ARV) regimens in adolescents are limited. METHODOLOGY: This study enrolled HIV-infected Thais who were treated with third-line regimens consisting of darunavir/ritonavir (DRV/r), etravirine (ETR), tipranavir/ritonavir or raltegravir. RESULTS: Fifty-four adolescents 2-17 years of age were enrolled from 8 sites and followed for 48 weeks. Reasons for switch were second-line failure (n = 44) and toxicity to second-line regimens (n = 10)...
October 2017: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/28481112/structure-based-optimization-of-thiophene-3-2-d-pyrimidine-derivatives-as-potent-hiv-1-non-nucleoside-reverse-transcriptase-inhibitors-with-improved-potency-against-resistance-associated-variants
#16
Dongwei Kang, Zengjun Fang, Boshi Huang, Xueyi Lu, Heng Zhang, Haoran Xu, Zhipeng Huo, Zhongxia Zhou, Zhao Yu, Qing Meng, Gaochan Wu, Xiao Ding, Ye Tian, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu
This work follows on from our initial discovery of a series of piperidine-substituted thiophene[3,2-d]pyrimidine HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTI) ( J. Med. Chem. 2016 , 59 , 7991 - 8007 ). In the present study, we designed, synthesized, and biologically tested several series of new derivatives in order to investigate previously unexplored chemical space. Some of the synthesized compounds displayed single-digit nanomolar anti-HIV potencies against wild-type (WT) virus and a panel of NNRTI-resistant mutant viruses in MT-4 cells...
May 25, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28403052/second-and-third-line-antiretroviral-therapy-for-children-and-adolescents-a-scoping-review
#17
REVIEW
Erica Lazarus, Simone Nicol, Lisa Frigati, Martina Penazzato, Mark F Cotton, Elizabeth Centeno-Tablante, Avy Violari, Liesl Nicol
BACKGROUND: The World Health Organization 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-line and subsequent ART regimens in children younger than 18 years. METHODS: We comprehensively searched, without language or date limitations, the Cochrane Central Register of Controlled Trials, MEDLINE, EMBASE, the World Health Organization's International Clinical Trials Registry Platform and ClinicalTrials...
May 2017: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/28390117/different-cell-cycle-modulation-in-skov-3-ovarian-cancer-cell-line-by-anti-hiv-drugs
#18
Angelica Perna, Angela Lucariello, Carmine Sellitto, Iolanda Agliata, Maria Carleo, Vincenzo Sangiovanni, Vincenzo Esposito, Germano Guerra, Luigi Cobellis, Antonio De Luca
Anti-retroviral drugs used for the treatment of Human Immunodeficiency Virus (HIV) have proven to be effective even against cancer. Drawing from this background the aim of our research project was to evaluate the effects of anti-HIV drugs that belong to the Nucleoside and Nucleotide Reverse Transcriptase Inhibitors (NRTI, abacavir and tenofovir), Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI, efavirenz and etravirine) and Protease Inhibitors (PI, darunavir) on ovarian adenocarcinoma cell line (Skov-3)...
March 26, 2017: Oncology Research
https://www.readbyqxmd.com/read/28382208/etravirine-combined-with-antiretrovirals-other-than-darunavir-ritonavir-for-hiv-1-infected-treatment-experienced-adults-week-48-results-of-a-phase-iv-trial
#19
Eduardo Arathoon, Asad Bhorat, Rodica Silaghi, Herta Crauwels, Ludo Lavreys, Lotke Tambuyzer, Ben Van Baelen, Simon Vanveggel, Magda Opsomer
OBJECTIVE: VIOLIN (TMC125IFD3002; NCT01422330) evaluated the safety, tolerability, and pharmacokinetics of etravirine with antiretrovirals other than darunavir/ritonavir in HIV-1-infected patients. METHODS: In a 48-week, phase IV, single-arm, multicenter study, patients on prior antiretroviral therapy (⩾8 weeks) who needed to change regimen for virologic failure (viral load ⩾ 500 copies/mL) or simplification/adverse events (viral load < 50 copies/mL) received etravirine 200 mg bid with ⩾1 other active antiretroviral, excluding darunavir/ritonavir or only nucleoside/tide reverse transcriptase inhibitors...
2017: SAGE Open Medicine
https://www.readbyqxmd.com/read/28375119/physical-characterization-and-dissolution-performance-assessment-of-etravirine-solid-dispersions-prepared-by-spray-drying-process
#20
Pavan Kommavarapu, Arthanareeswari Maruthapillai, Kamaraj Palanisamy, Ravi Teja Koya
The aim of the current exertion was to prepare Solid Dispersion of Etravirine by Spray drying technique to enhance aqueous solubility and dissolution rate. Solid dispersions (SD) of Etravirine were prepared using Copovidone and Povidone-Copovidone in dichloromethane and physical properties were characterized by Scanning electron microscopy (SEM), X-Ray diffractometry (PXRD), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC). SD's were evaluated for equilibrium solubility and in vitro drug release profile by dissolution testing...
November 2016: Pakistan Journal of Pharmaceutical Sciences
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