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Efavirenz

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https://www.readbyqxmd.com/read/29438196/antiretroviral-drug-concentrations-in-hair-are-associated-with-virologic-outcomes-among-young-people-living-with-hiv-in-tanzania
#1
Zachary J Tabb, Blandina T Mmbaga, Monica Gandhi, Alexander Louie, Karen Kuncze, Hideaki Okochi, Aisa M Shayo, Elizabeth L Turner, Coleen K Cunningham, Dorothy E Dow
OBJECTIVE: We assessed the relationship of self-reported adherence versus antiretroviral therapy (ART) concentrations in hair with virologic outcomes among young people living with HIV. DESIGN: This was a cross-sectional study that enrolled young people living with HIV age 11-24 years, who attended a youth HIV clinic in Moshi, Tanzania. METHODS: ART adherence was assessed by self-report, drug concentration in hair samples, and plasma HIV-1 RNA measurements...
February 12, 2018: AIDS
https://www.readbyqxmd.com/read/29437904/a-computational-study-for-rational-hiv-1-non-nucleoside-reverse-transcriptase-inhibitor-selection-and-discovery-of-novel-allosteric-pockets-for-inhibitor-design
#2
Ron Zhi-Hui Chiang, Samuel Ken-En Gan, Chinh Tran-To Su
HIV drug resistant mutations that render the current Highly Active Anti-Retroviral Therapy cocktail drugs ineffective are increasingly reported. To study the mechanisms of these mutations in conferring drug resistance, we computationally analyzed fourteen Reverse Transcriptase (RT) structures of HIV-1 on the following parameters: drug-binding pocket volume, allosteric effects caused by the mutations, and structural thermal stability. We constructed structural correlation-based networks of the mutant RT-drug complexes and the analyses support the use of Efavirenz as the first-line drug, given that cross-resistance is least likely to develop from Efavirenz-resistant mutations...
February 5, 2018: Bioscience Reports
https://www.readbyqxmd.com/read/29434868/cytotoxic-effect-of-efavirenz-in-bxpc-3-pancreatic-cancer-cells-is-based-on-oxidative-stress-and-is-synergistic-with-ionizing-radiation
#3
Markus Hecht, Thomas Harrer, Verena Körber, Eric O Sarpong, Fabian Moser, Nora Fiebig, Manuela Schwegler, Michael Stürzl, Rainer Fietkau, Luitpold V Distel
The non-nucleoside reverse transcriptase inhibitor (NNRTI) Efavirenz is frequently used in human immunodeficiency virus treatment, but also efficient against cancer in mouse models. Its radiosensitizing effect makes it a promising drug for combination with radiotherapy. The efficacy of Efavirenz combined with irradiation was assessed with immunostaining of DNA-damage markers and colony formation assays in BxPC-3 pancreatic cancer cells. Gene expression and protein phosphorylation of the Efavirenz-sensitive BxPC-3 cells was compared to the resistant primary fibroblasts SBL-5...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29430850/probing-ligand-structure-activity-relationships-in-pregnane-x-receptor-pxr-efavirenz-and-8-hydroxyefavirenz-exhibit-divergence-in-activation
#4
Bhargavi Narayanan, Julie Lade, Carley J S Heck, Kevin D Dietz, Herschel V Wade, Namandje N Bumpus
Efavirenz (EFV), an antiretroviral that interacts clinically with co-administered drugs via activation of the pregnane X receptor (PXR), is extensively metabolized by the cytochromes P450. We tested whether its primary metabolite, 8-hydroxyEFV (8-OHEFV) can activate PXR and potentially contribute to PXR-mediated drug-drug interactions attributed to EFV. Luciferase reporter assays revealed that despite only differing from EFV by an oxygen atom, 8-OHEFV did not activate PXR. Corroborating this, treatment with EFV for 72 h elevated the mRNA abundance of the PXR target gene, Cyp3a11, an approximate 28-fold in primary hepatocytes isolated from PXR-humanized mice while treatment with 8-OHEFV did not result in a change in Cyp3a11 mRNA levels...
February 11, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29426975/study-the-influence-of-formulation-process-parameters-on-solubility-and-dissolution-enhancement-of-efavirenz-solid-solutions-prepared-by-hot-melt-extrusion-a-qbd-methodology
#5
Jaywant Pawar, Dilipkumar Suryawanshi, Kailas Moravkar, Rahul Aware, Vasant Shetty, Mohammed Maniruzzaman, Purnima Amin
The current study investigates the dissolution rate performance of amorphous solid solutions of a poorly water-soluble drug, efavirenz (EFV), in amorphous Soluplus® (SOL) and Kollidon® VA 64 (KVA64) polymeric systems. For the purpose of the study, various formulations with varying drug loadings of 30, 50, and 70% w/w were developed via hot-melt extrusion processing and adopting a Box-Behnken design of experiment (DoE) approach. The polymers were selected based on the Hansen solubility parameter calculation and the prediction of the possible drug-polymer miscibility...
February 9, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29426120/contaminants-of-emerging-concern-in-the-hartbeespoort-dam-catchment-and-the-umngeni-river-estuary-2016-pollution-incident-south-africa
#6
Cornelius Rimayi, David Odusanya, Jana M Weiss, Jacob de Boer, Luke Chimuka
A quantitative assessment of pollutants of emerging concern in the Hartbeespoort Dam catchment area was conducted using liquid chromatography-tandem mass spectrometry (LC-MS/MS) to establish the occurrence, source and distribution of 15 environmental pollutants, including 10 pharmaceuticals, 1 pesticide and 4 steroid hormones. Seasonal sampling was conducted in the Hartbeespoort Lake using sub-surface grab sampling to determine the lake's ecological status and obtain data for establishment of progressive operational monitoring...
February 2, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29424697/patterns-of-efavirenz-use-as-first-line-antiretroviral-therapy-in-the-united-states-1999-2015
#7
Angela M Bengtson, Brian W Pence, Ellen F Eaton, Jessie K Edwards, Joseph J Eron, William C Mathews, Katie Mollan, Richard D Moore, Connall O'Cleirigh, Elvin Geng, Michael J Mugavero
BACKGROUND: Efavirenz has been a mainstay of antiretroviral therapy (ART) for over 15 years in the US. Its association with neuropsychiatric side effects may influence clinical prescribing and management. METHODS: We included HIV-infected adults enrolled in care at 7 sites across the US, who initiated combination ART between 1999 and 2015. We examined the proportion initiating and continuing on efavirenz, overall and by mental health status. Log binomial and Cox models were used to estimate associations between mental health, clinical, and sociodemographic characteristics and initiating or switching from efavirenz as first line ART...
February 9, 2018: Antiviral Therapy
https://www.readbyqxmd.com/read/29421849/a-validated-liquid-chromatography-tandem-mass-spectrometry-method-for-the-analysis-of-efavirenz-in-0-2-mg-hair-samples-from-hiv-infected-patients
#8
Jenna Johnston, Catherine Orrell, Peter Smith, Anton Joubert, Lubbe Wiesner
RATIONALE: Drug levels in hair provide a longer window of detection, compared to plasma drug levels, and therefore hair analysis has the advantage of assessing adherence over a longer period of time. No methods for the analysis of antiretroviral drugs in hair currently exist in South Africa, and worldwide there is only one validated method for the determination of efavirenz in hair that has been published. METHODS: Efavirenz was extracted from 0.2 mg of hair through a simultaneous pulverization and extraction step...
February 8, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29412463/the-drug-drug-interaction-profile-of-presatovir
#9
Yan Xin, Winnie Weng, Bernard P Murray, Eugene J Eisenberg, Jason W Chien, John Ling, Jeffrey A Silverman
Respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infections in young children. Presatovir (previously GS-5806) is a novel, orally administered RSV fusion inhibitor with a favorable safety profile and proven antiviral efficacy in preclinical and clinical studies. In vitro, presatovir is a substrate of the efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) and hepatic uptake transporters organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 and is slowly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5...
February 7, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29397261/using-microfluidic-platforms-to-develop-cns-targeted-polymeric-nanoparticles-for-hiv-therapy
#10
Cláudia Martins, Francisca Araújo, Maria João Gomes, Carlos Fernandes, Rute Nunes, Wei Li, Hélder A Santos, Fernanda Borges, Bruno Sarmento
The human immunodeficiency virus (HIV) uses the brain as reservoir, which turns it as a promising target to fight this pathology. Nanoparticles (NPs) of poly(lactic-co-glycolic) acid (PLGA) are potential carriers of anti-HIV drugs to the brain, since most of these antiretrovirals, as efavirenz (EFV), cannot surpass the blood-brain barrier (BBB). Forasmuch as the conventional production methods lack precise control over the final properties of particles, microfluidics emerged as a prospective alternative. This study aimed at developing EFV-loaded PLGA NPs through a conventional and microfluidic method, targeted to the BBB, in order to treat HIV neuropathology...
January 31, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29395300/effect-of-body-weight-and-composition-on-efavirenz-atazanavir-or-darunavir-concentration
#11
Célia Lloret-Linares, Yasmin Rahmoun, Amanda Lopes, Dorothée Chopin, Guy Simoneau, Andrew Green, Brigitte Delhotal, Hélène Sauvageon, Stéphane Mouly, Jean-François Bergmann, Pierre-Olivier Sellier
BACKGROUND: To compare the steady state plasma concentrations (Css) of three antiretroviral drugs in both normal and overweight patients, and to determine the relationship between Css and fat mass (FM) or lean body mass. METHODS: Patients treated for more than 6 months once daily with one of the antiretroviral drugs: efavirenz (EFV) 600mg, atazanavir boosted with ritonavir (ATV-r) 300mg/100mg, or darunavir boosted with ritonavir (DRV-r) 800mg/100mg, combined with two nucleoside analogues, were enrolled prospectively...
November 2, 2017: Thérapie
https://www.readbyqxmd.com/read/29389578/a-novel-uv-photolysis-approach-with-acetone-and-isopropyl-alcohol-for-the-rapid-determination-of-fluoride-in-organofluorine-containing-drugs-by-spectrophotometry
#12
Venkata Balarama Krishna Mullapudi, Karunasagar Dheram
A UV photolysis decomposition (UVPD) method for the determination of fluoride in fluorine containing pharmaceuticals by spectrophotometry is reported. It is based on the use of high intensity UV-irradiation in the presence of a digesting solution comprising a mixture of acetone and isopropanol. For the optimization of the UVPD procedure, three bulk drugs (levofloxacin, nebivolol and efavirenz) were chosen as representatives of three diverse compounds containing a single fluorine atom, two fluorine atoms, and trifluoromethyl groups respectively...
January 2018: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/29384848/economic-evaluation-of-weekends-off-antiretroviral-therapy-for-young-people-in-11-countries
#13
Luis Enrique Tierrablanca, Jessica Ochalek, Deborah Ford, Ab Babiker, Diana Gibb, Karina Butler, Anna Turkova, Susan Griffin, Paul Revill
OBJECTIVES: To analyze the cost effectiveness of short-cycle therapy (SCT), where patients take antiretroviral (ARV) drugs 5 consecutive days a week and have 2 days off, as an alternative to continuous ARV therapy for young people infected with human immunodeficiency virus (HIV) and taking efavirenz-based first-line ARV drugs. METHODS: We conduct a hierarchical cost-effectiveness analysis based on data on clinical outcomes and resource use from the BREATHER trial...
February 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29378397/en-route-to-2-cyclobuten-1-yl-3-trifluoromethyl-1h-indole
#14
Martin Gazvoda, Marko Krivec, Zdenko Casar, Janez Košmrlj
A six-step synthetic route from 4-chloro-2-methylaniline to 5-chloro-2-(cyclobut-1-en-1-yl)-3-(trifluoromethyl)-1H-indole (1) has been reported. Compound 1 is a key impurity of reverse transcriptase inhibitor efavirenz, an important anti-HIV/AIDS drug. Synthetic challenges, dead ends and detours are discussed.
January 29, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29372000/highly-active-antiretroviral-therapy-alters-sperm-parameters-and-testicular-antioxidant-status-in-diet-induced-obese-rats
#15
Ibukun P Oyeyipo, Bongekile T Skosana, Frans P Everson, Hans Strijdom, Stefan S du Plessis
The efficacy of highly active antiretroviral therapy (HAART) has led to an increase demand for therapeutic use, thereby necessitating investigation into drug toxicity. This study was designed to investigate the in vivo effects of HAART on sperm parameters and testicular oxidative stress in lean and obese rats. Wistar rats (males, n = 40, weighing 180~200 g) were assigned randomly into 4 groups and treated accordingly for 16 weeks as follows: Control (C): lean group fed with standard rat chow; Diet induced obesity (DIO): obese animals fed a high caloric diet; C + ART: lean animals treated with HAART; DIO + ART: obese animals treated with HAART...
January 2018: Toxicological Research
https://www.readbyqxmd.com/read/29371638/characterization-of-nanodiamond-based-anti-hiv-drug-delivery-to-the-brain
#16
Upal Roy, Vadym Drozd, Andriy Durygin, Jesse Rodriguez, Paul Barber, Venkata Atluri, Xiaohua Liu, Thomas G Voss, Surendra Saxena, Madhavan Nair
Human Immunodeficiency Virus Type 1 (HIV-1) remains one of the leading causes of death worldwide. Present combination antiretroviral therapy has substantially improved HIV-1 related pathology. However, delivery of therapeutic agents to the HIV reservoir organ like Central nervous system (CNS) remains a major challenge primarily due to the ineffective transmigration of drugs through Blood Brain Barrier (BBB). The recent advent of nanomedicine-based drug delivery has stimulated the development of innovative systems for drug delivery...
January 25, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29365101/physiologically-based-pharmacokinetic-modelling-prediction-of-the-effects-of-dose-adjustment-in-drug-drug-interactions-between-levonorgestrel-contraceptive-implants-and-efavirenz-based-art
#17
Owain Roberts, Rajith K R Rajoli, David J Back, Andrew Owen, Kristin M Darin, Courtney V Fletcher, Mohammed Lamorde, Kimberly K Scarsi, Marco Siccardi
Background: HIV-positive women receiving efavirenz-based ART and levonorgestrel contraceptive implants are at risk of low levonorgestrel exposure and unintended pregnancy. Objectives: To investigate clinically applicable dose-adjustment strategies to overcome the known drug-drug interaction (DDI) between levonorgestrel and efavirenz, using a physiologically based pharmacokinetic (PBPK) modelling-based approach. Methods: A PBPK model was qualified against clinical data to predict levonorgestrel plasma concentrations when standard-dose (150 mg) levonorgestrel implants were administered alone (control group), as well as when standard-dose or increased-dose (300 mg) levonorgestrel implants were coadministered with either 600 or 400 mg of efavirenz...
January 22, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29351416/acute-and-chronic-resistance-training-downregulates-select-line-1-retrotransposon-activity-markers-in-human-skeletal-muscle
#18
Matthew A Romero, C Brooks Mobley, Petey W Mumford, Paul A Roberson, Cody T Haun, Wesley C Kephart, James C Healy, Darren T Beck, Kaelin C Young, Jeffrey S Martin, Christopher M Lockwood, Michael D Roberts
Herein, we examined if acute or chronic resistance exercise affected markers of skeletal muscle LINE-1 retrotransposon activity. In study 1, 10 resistance-trained college-aged males performed three consecutive daily back squat sessions, and vastus lateralis biopsies were taken prior to (Pre), 2 h following session 1 (Post1), and 3 days following session 3 (Post2). In study 2, 13 untrained college-aged males performed a full-body resistance training program (3 d/wk), and vastus lateralis biopsies were taken prior to (week 0) and ~72 h following training cessation (week 12)...
December 20, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29351338/stockouts-of-hiv-commodities-in-public-health-facilities-in-kinshasa-barriers-to-end-hiv
#19
Tinne Gils, Claire Bossard, Kristien Verdonck, Philip Owiti, Ilse Casteels, Maria Mashako, Gilles Van Cutsem, Tom Ellman
Stockouts of HIV commodities increase the risk of treatment interruption, antiretroviral resistance, treatment failure, morbidity and mortality. The study objective was to assess the magnitude and duration of stockouts of HIV medicines and diagnostic tests in public facilities in Kinshasa, Democratic Republic of the Congo. This was a cross-sectional survey involving visits to facilities and warehouses in April and May 2015. All zonal warehouses, all public facilities with more than 200 patients on antiretroviral treatment (ART) (high-burden facilities) and a purposive sample of facilities with 200 or fewer patients (low-burden facilities) in Kinshasa were selected...
2018: PloS One
https://www.readbyqxmd.com/read/29349445/discovery-of-novel-diarylpyrimidines-as-potent-hiv-1-nnrtis-by-investigating-the-chemical-space-of-a-less-explored-hydrophobic-channel
#20
Zhongxia Zhou, Tao Liu, Dongwei Kang, Zhipeng Huo, Gaochan Wu, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu
A new series of diarylpyrimidines (DAPYs) were designed, synthesized and evaluated as novel HIV-1 NNRTIs to further explore the chemical space surrounding the "hydrophobic channel" of the NNRTI binding pocket (NNIBP), guided by the comprehensive analysis of X-ray structural biology data of HIV-1 RT/NNRTI complexes and molecular modeling. Encouragingly, most of the synthesized DAPYs were found to be active against the HIV-1 wild-type (WT) strain with EC50 values ranging from 3 nM to 63 nM, and displayed significantly reduced cytotoxicity compared with etravirine (ETV) and rilpivirine (RPV)...
January 19, 2018: Organic & Biomolecular Chemistry
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