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https://www.readbyqxmd.com/read/28642370/in-vitro-cytochrome-p450-46a1-cyp46a1-activation-by-neuroactive-compounds
#1
Natalia Mast, Kyle W Anderson, Kevin M Johnson, Thanh T N Phan, F Peter Guengerich, Irina A Pikuleva
Cytochrome P450 46A1 (CYP46A1, cholesterol 24-hydroxylase) is the enzyme responsible for the majority of cholesterol elimination from the brain. Previously, we found that the anti-HIV drug efavirenz (EFV) can pharmacologically activate CYP46A1 in mice. Herein, we investigated whether CYP46A1 could also be activated by endogenous compounds, including major neurotransmitters. In vitro experiments with purified recombinant CYP46A1 indicated that CYP46A1 is activated by L-glutamate (L-Glu), L-aspartate, γ-aminobutyric acid, and acetylcholine, with L-Glu eliciting the highest increase (3-fold) in CYP46A1-mediated cholesterol 24-hydroxylation...
June 22, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28638661/efficacy-and-tolerability-of-tenofovir-disoproxil-fumarate-based-regimen-as-compared-to-zidovudine-based-regimens-a-systematic-review-and-meta-analysis
#2
REVIEW
Tegene Legese Dadi, Adane Teshome Kefale, Teshale Ayele Mega, Muktar Sano Kedir, Habtamu Acho Addo, Tessema Tsehay Biru
BACKGROUND: Although tenofovir (TDF)/emtricitabine (FTC)/efavirenz (EFV) and zidovudine (ZDV)/lamivudine (3TC)/efavirenz (EFV) are used as preferred first line regimen, their head-to-head comparison in terms of their efficacy and tolerability was limited. This review aimed to synthesize the best available evidence on the comparative efficacy and tolerability of the two regimens. METHODS: Seven sites and databases in addition to Google search until August 20, 2016, were searched...
2017: AIDS Research and Treatment
https://www.readbyqxmd.com/read/28628334/chiral-indolylarylsulfone-non-nucleoside-reverse-transcriptase-inhibitors-as-new-potent-and-broad-spectrum-anti-hiv-1-agents
#3
Valeria Famiglini, Giuseppe La Regina, Antonio Coluccia, Domiziana Masci, Andrea Brancale, Roger Badia, Eva Riveira Muñoz, Jose A Este, Emmanuele Crespan, Alessandro Brambilla, Giovanni Maga, Myriam Catalano, Cristina Limatola, Francesca Romana Romana Formica, Roberto Cirilli, Ettore Novellino, Romano Silvestri
We designed and synthesized a series of chiral indolyarylsulfones (IASs) as new HIV-1 NNRTIs. The new IASs 8-37 showed potent inhibition of the HIV-1 WT NL4-3 strain and of the mutant K103N, Y181C, Y188L and K103N-Y181C HIV-1 strains. Six racemic mixtures, 8, 23-25, 31 and 33, were separated at semipreparative level into their pure enantiomers. The (R)-8 enantiomer bearing the chiral (α-methylbenzyl) was superior to the (S)-counterpart. IAS derivatives bearing the (S) alanine unit, (S)-23, (S,R)-25, (S)-31 and (S)-33, were remarkably more potent than the corresponding (R)-enantiomers...
June 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28627427/144-week-efficacy-and-safety-of-a-once-daily-single-tablet-regimen-of-tenofovir-lamivudine-and-efavirenz-among-arv-na%C3%A3-ve-and-arv-experienced-hiv-1-infected-thai-adults
#4
Anchalee Avihingsanon, Wirach Maek-A-Nantawat, Sivaporn Gatechompol, Vorapot Sapsirisavat, Wanida Thiansanguankul, Jiratchaya Sophonphan, Narujakorn Thammajaruk, Sasiwimol Ubolyam, David M Burger, Kiat Ruxrungtham
OBJECTIVES: To assess the efficacy and safety of a new single tablet regimen(STR) of tenofovir disoproxil fumarate(TDF) 300mg, lamivudine(3TC) 300mg and efavirenz(EFV) 600mg in HIV-infected Thais. METHODS: This was a 144 week, prospective study among 51 treatment naïve and 49 experienced patients on separated pill of TDF, 3TC and EFV with HIV RNA<50 copies/ml. CD4, HIV RNA, liver, renal functions and lipid profiles were assessed at baseline, weeks 12, 24, 48 and then every 24 weeks...
June 13, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28622951/population-approach-to-efavirenz-therapy
#5
Hélder Duarte, João Paulo Cruz, Natália Aniceto, Ana Clara Ribeiro, Ana Fernandes, Paulo Paixão, Francisco Antunes, José Morais
Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor commonly used as first line therapy in the treatment of human immunodeficiency virus, with a narrow therapeutic range and a high between-subject variability which can lead to central nervous system toxicity or therapeutic failure. To characterize the sources of variability and better predict EFV steady state plasma concentrations, a population pharmacokinetic model was developed form 96 HIV positive individuals, using a nonlinear mixed effect method with Monolix® software...
June 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28608515/efavirenz-clearances-in-vitro-and-in-vivo-in-six-cynomolgus-monkeys-associated-with-polymorphic-cytochrome-p450-2c9-and-simulated-by-individual-physiologically-based-pharmacokinetic-models
#6
Masahiro Utoh, Tomonori Miura, Takashi Kusama, Shotaro Uehara, Makiko Shimizu, Yasuhiro Uno, Hiroshi Yamazaki
Cynomolgus monkey cytochrome P450 2C9 (formerly known as P450 2C43) variation was reportedly associated with metabolic clearance of the antiretroviral drug efavirenz in vivo (of three wild-type, one heterozygote, and two homozygote animals), being unlikely in the case of human P450 2B6-dependent efavirenz clearance. In this study, the liver microsomal elimination rates of efavirenz for the same individual animals previously treated with intravenous/oral administrations of efavirenz showed significant reductions associated with the P450 2C9 p...
June 13, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28584489/influence-of-milling-process-on-efavirenz-solubility
#7
Erizal Zaini, Deni Wahyu, Maria Dona Octavia, Lili Fitriani
INTRODUCTION: The aim of this study was to investigate the influence of the milling process on the solubility of efavirenz. MATERIALS AND METHODS: Milling process was done using Nanomilling for 30, 60, and 180 min. Intact and milled efavirenz were characterized by powder X-ray diffraction, scanning electron microscopy (SEM), spectroscopy infrared (IR), differential scanning calorimetry (DSC), and solubility test. RESULTS: The X-ray diffractogram showed a decline on peak intensity of milled efavirenz compared to intact efavirenz...
January 2017: Journal of Pharmacy & Bioallied Sciences
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
#8
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/28575936/solid-crystal-suspension-of-efavirenz-using-hot-melt-extrusion-exploring-the-role-of-crystalline-polyols-in-improving-solubility-and-dissolution-rate
#9
Jaywant N Pawar, Ritesh A Fule, Mohammed Maniruzzaman, Purnima D Amin
Poor aqueous solubility of drugs has emerged as a major issue for pharmaceutical scientists from many decades. The current study explores the manufacture and development of a thermodynamically stabilized solid crystal suspension (SCS) of poorly water soluble drug efavirenz via hot melt extrusion. Efavirenz is a non-nucleoside reverse transcriptase inhibitor and belongs to BCS class II. The SCS was prepared using pearlitol and xylitol as a crystalline carrier. The drug-excipient blend was processed by hot melt extrusion with up to 50% (w/w) drug loading...
September 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28570367/antiretroviral-dose-optimization-the-future-of-efavirenz-400%C3%A2-mg-dosing
#10
Marta Boffito, Mohammed Lamorde, Melynda Watkins, Anton Pozniak
PURPOSE OF REVIEW: Antiretroviral (ARV) therapy costs in low-income and middle-income countries are major concerns, and lower doses of first-line treatment components, when possible, would save millions of dollars, which could be used to treat more people living with HIV. RECENT FINDINGS: The Encore-1 study, followed by a detailed pharmacokinetic analysis of efavirenz 400 versus 600 mg once daily, produced enough information for the most recent ARV treatment WHO guidelines to include efavirenz 400 mg among agents used for first-line treatment...
July 2017: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/28569550/ultra-deep-sequencing-analysis-on-hiv-drug-resistant-associated-mutations-among-hiv-infected-individuals-first-report-from-the-philippines
#11
Ivo Novita SahBandar, Genesis Samonte, Elizabeth Telan, Nalyn Siripong, Mahdi Belcaid, David Schanzenbach, Susan Leano, Haorile Chagan-Yasutan, Toshio Hattori, Cecilia Shikuma, Lishomwa C Ndhlovu
OBJECTIVE: A sharp increase in the number of people living with HIV (PLHIV) has been documented in the Philippines. In response, the government has instituted antiretroviral therapy (ART) nationwide through HIV treatment hubs. However, no data presently exists on the status of ART drug-resistant-associated mutations (DRMs). In this study, we aim to analyze DRM profiles in the Philippines and provide comprehensive data on DRMs to guide treatment decisions and prevent viral failures. DESIGN AND METHODS: We conducted a cross-sectional study in 119 volunteers tested positive for HIV from over 8,000 participants screened for HIV across the nation through 2013 Integrated HIV Behavioral and Serologic Surveillance (IHBSS) program...
June 1, 2017: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/28567199/frequent-malaria-illness-episodes-in-two-malawian-patients-on-antiretroviral-therapy-soon-after-stopping-cotrimoxazole-preventive-therapy
#12
Wongani Js Nyangulu, Edson Mwinjiwa, Titus H Divala, Randy G Mungwira, Osward Nyirenda, Maxwell Kanjala, Gillian Mbambo, Jane Mallewa, Terrie E Taylor, Matthew B Laurens, Miriam K Laufer, Joep J van Oosterhout
We describe two Malawian adults on successful antiretroviral therapy who experienced frequent malaria episodes after stopping cotrimoxazole prophylaxis. We argue that, in addition to stopping cotrimoxazole, diminished malaria immunity and drug interactions between efavirenz and artemether-lumefantrine may have played a causative role in the recurrent malaria our patients experienced.
March 2017: Malawi Medical Journal: the Journal of Medical Association of Malawi
https://www.readbyqxmd.com/read/28559276/population-pharmacokinetic-model-linking-plasma-and-peripheral-blood-mononuclear-cells-pbmcs-concentrations-of-efavirenz-and-its-metabolite-8-hydroxy-efavirenz-in-hiv-patients
#13
Abiy Habtewold, Eleni Aklillu, Eyasu Makonnen, Getnet Yimer, Leif Bertilsson, Jürgen Burhenne, Joel S Owen
Objectives: To characterize the population PK of EFV and 8-hydroxy-efavirenz (8OHEFV) in plasma and peripheral blood mononuclear cells (PBMCs) and explore covariates affecting the PK parameters.Methods: Fifty-one patients had steady-state 0-24h plasma with corresponding PBMC concentrations of EFV and 8OHEFV, while 261 patients had 1 or 2 sparse concentrations at 16±1h post-dose at weeks 4 and/or 16. Pharmacogenetic markers CYP2B6*6, CYP3A5 (*3 &*6);, UGT2B7*2, ABCB1 (3435C<T, 3842A<G), OATP1B1 (*1B & *5), presence of rifampicin-based anti-TB regimen, baseline body weight and organ function values; and demographic factors were explored as covariates...
May 30, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28557187/automated-high-throughput-analysis-of-antiretroviral-drugs-in-dried-blood-spots
#14
U Duthaler, B Berger, S Erb, M Battegay, E Letang, S Gaugler, S Krähenbühl, M Haschke
For therapeutic drug monitoring (TDM) in remote settings, dried blood spots (DBS) are particularly advantageous, as blood sample collection and handling is uncomplicated. The aim of this study was to develop and validate an automated extraction method for the analysis of nevirapine, efavirenz, and lopinavir in DBS samples. Automated extraction was performed with methanol:water (70:30 v/v), using a DBS-MS 500 autosampler coupled to a LC-MS/MS system. The autosampler used digital images of each DBS to position the extraction head, sprayed 10 μL internal standard (IS) onto each DBS and extracted a 4 mm disk (Ø) from the centre of each spot by unilateral flow using 25 μl extraction solvent...
May 29, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28556627/a-mathematical-model-to-predict-hiv-virological-failure-and-elucidate-the-role-of-lymph-node-drug-penetration
#15
S Sanche, N Sheehan, T Mesplède, M A Wainberg, J Li, F Nekka
Preventing virological failure following HIV treatment remains a difficult task that is further complicated by the emergence of drug resistance. We have developed a mathematical model able to explain and predict HIV virological outcomes for various compounds and patients' drug intake patterns. Compared to current approaches, this model considers, altogether, drug penetration into lymph nodes, a refined adherence representation accounting for the propensity for long drug holidays, population pharmacokinetic and pharmacodynamic variability, drug interaction, and crossresistance...
May 27, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28539254/prevalence-of-primary-resistance-among-acutely-recently-hiv-infected-patients-in-rio-de-janeiro-brazil
#16
Ana Cristina G Ferreira, Lara E Coelho, Eduarda Grinsztejn, Carlos S de Jesus, Monick L Guimarães, Valdilea G Veloso, Beatriz Grinsztejn, Sandra W Cardoso
INTRODUCTION: The widespread use of antiretroviral therapy (ART) increased the transmission of antiretroviral resistant HIV strains. ART initiation during acute/recent HIV infection limits HIV reservoirs and improves immune response in HIV infected individuals. Transmitted drug resistance (TDR) may jeopardize the early goals of early ART among acute/recent HIV infected patients. METHODS: Patients with acute/recent HIV infection who underwent resistance test before ART initiation were included in this analysis...
May 21, 2017: Brazilian Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28538284/the-advance-study-a-groundbreaking-trial-to-evaluate-a-candidate-universal-antiretroviral-regimen
#17
Willem D F Venter, Polly Clayden, Celicia Serenata
PURPOSE OF REVIEW: Current WHO-recommended first-line therapy in low-income and middle-income countries has been very successful in saving millions of lives but still has toxicity concerns and a low barrier to resistance. RECENT FINDINGS: Two candidate antiretrovirals may substantially transform first-line therapy in low-income and middle-income countries, yielding a safer, more robust and cheaper regimen. Tenofovir alafenamide carries toxicity and cost benefits over tenofovir disoproxil fumarate...
July 2017: Current Opinion in HIV and AIDS
https://www.readbyqxmd.com/read/28530033/concomitant-contraceptive-implant-and-efavirenz-use-in-women-living-with-hiv-perspectives-on-current-evidence-and-policy-implications-for-family-planning-and-hiv-treatment-guidelines
#18
REVIEW
Rena C Patel, Chelsea Morroni, Kimberly K Scarsi, Tabitha Sripipatana, James Kiarie, Craig R Cohen
INTRODUCTION: Preventing unintended pregnancies is important among all women, including those living with HIV. Increasing numbers of women, including HIV-positive women, choose progestin-containing subdermal implants, which are one of the most effective forms of contraception. However, drug-drug interactions between contraceptive hormones and efavirenz-based antiretroviral therapy (ART) may reduce implant effectiveness. We present four inter-related perspectives on this issue. DISCUSSION: First, as a case study, we discuss how limited data prompted country-level guidance against the use of implants among women concomitantly using efavirenz in South Africa and its subsequent negative effects on the use of implants in general...
May 11, 2017: Journal of the International AIDS Society
https://www.readbyqxmd.com/read/28523633/synthesis-comparison-and-optimization-of-a-humic-acid-quat10-polyelectrolyte-complex-by-complexation-precipitation-versus-extrusion-spheronization
#19
Margaret Siyawamwaya, Yahya E Choonara, Pradeep Kumar, Pierre P D Kondiah, Lisa C du Toit, Viness Pillay
A novel humic acid and polyquaternium-10 polyelectrolyte complex (PEC) was synthesized utilizing two methods and the solubility and permeability of efavirenz (EFV) were established. Complexation-precipitation and extrusion-spheronization were used to synthesize and compare the drug-loaded PECs. The chemical integrity, thermo-mechanical differences, and morphology between the drug-loaded PECs produced by the two methods were assessed by attenuated total reflectance-Fourier transform infrared, differential scanning calorimetry, and SEM...
May 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28522147/cardiovascular-risk-in-advanced-na%C3%A3-ve-hiv-infected-patients-starting-antiretroviral-therapy-comparison-of-three-different-regimens-prevaleat-ii-cohort
#20
Paolo Maggi, Chiara Bellacosa, Armando Leone, Anna Volpe, Elena Delfina Ricci, Nicoletta Ladisa, Stefania Cicalini, Elisabetta Grilli, Rosaria Viglietti, Antonio Chirianni, Lara Ines Bellazzi, Renato Maserati, Canio Martinelli, Paola Corsi, Benedetto Maurizio Celesia, Federica Sozio, Gioacchino Angarano
BACKGROUND AND AIMS: PREVALEAT (PREmature VAscular LEsions and Antiretroviral Therapy) II is a multicenter, longitudinal cohort study aimed at the evaluation of cardiovascular risk among advanced HIV-positive, treatment-naïve patients starting their first therapy. We hypothesized that these patients, present a higher cardiovascular (CV) risk. METHODS: The study included all consecutive naïve patients with less than 200 CD4 cells/ml starting antiretroviral therapy...
May 5, 2017: Atherosclerosis
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