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Etravirine

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https://www.readbyqxmd.com/read/29846602/prevalence-of-drug-resistance-in-children-recently-diagnosed-with-hiv-1-infection-in-france-2006-17-impact-on-susceptibility-to-first-line-strategies
#1
Pierre Frange, Véronique Avettand-Fenoel, Florence Veber, Stéphane Blanche, Marie-Laure Chaix
Objectives: To describe the prevalence of transmitted drug resistance (TDR) among 84 children newly diagnosed with HIV in France in 2006-17. Methods: HIV-1 resistance-associated mutations (RAMs) were characterized using both the 2009 Stanford list of mutations and the 2017 French National Agency for AIDS Research (ANRS) algorithm. A genotypic susceptibility score (GSS) was estimated for each first-line recommended ART combination. Results: Patients were mainly infected through mother-to-child transmission (MTCT) (73/84; 86...
May 29, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29846589/dynamics-of-drug-resistance-associated-mutations-in-hiv-1-dna-reverse-transcriptase-sequence-during-effective-art
#2
A Nouchi, T Nguyen, M A Valantin, A Simon, S Sayon, R Agher, V Calvez, C Katlama, A G Marcelin, C Soulie
Objectives: To investigate the dynamics of HIV-1 variants archived in cells harbouring drug resistance-associated mutations (DRAMs) to lamivudine/emtricitabine, etravirine and rilpivirine in patients under effective ART free from selective pressure on these DRAMs, in order to assess the possibility of recycling molecules with resistance history. Patients and methods: We studied 25 patients with at least one DRAM to lamivudine/emtricitabine, etravirine and/or rilpivirine identified on an RNA sequence in their history and with virological control for at least 5 years under a regimen excluding all drugs from the resistant class...
May 29, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29797570/emergence-of-uncommon-hiv-1-non-b-subtypes-and-circulating-recombinant-forms-and-trends-in-transmission-of-antiretroviral-drug-resistance-in-patients-with-primary-infection-during-the-2013-2015-period-in-marseille-southeastern-france
#3
Catherine Tamalet, Hervé Tissot-Dupont, Anne Motte, Christian Tourrès, Catherine Dhiver, Isabelle Ravaux, Isabelle Poizot-Martin, Thérèse Dieng, Christelle Tomei, Sylvie Bregigeon, Olivia Zaegel-Faucher, Hélène Laroche, Sarah Aherfi, Saadia Mokhtari, Hervé Chaudet, Amelie Ménard, Philippe Brouqui, Andreas Stein, Philippe Colson
Primary HIV-1 infections (PHI) with non-B subtypes are increasing in developed countries while transmission of HIV-1 harboring antiretroviral resistance-associated mutations (RAMs) remains a concern. This study assessed non-B HIV-1 subtypes and RAMs prevalence among patients with PHI in university hospitals of Marseille, Southeastern France, in 2005-2015 (11 years). HIV-1 sequences were obtained by in-house protocols from 115 patients with PHI, including 38 for the 2013-2015 period. On the basis of the phylogenetic analysis of the reverse transcriptase region, non-B subtypes were identified in 31% of these patients...
May 24, 2018: Journal of Medical Virology
https://www.readbyqxmd.com/read/29732907/prevalence-of-rilpivirine-and-etravirine-resistance-mutations-in-hiv-1-subtype-c-infected-patients-failing-nevirapine-or-efavirenz-based-combination-antiretroviral-therapy-in-botswana
#4
Thabo Diphoko, Simani Gaseitsiwe, Ishmael Kasvosve, Sikhulile Moyo, Harriet Okatch, Rosemary Musonda, Mark Wainberg, Joseph Makhema, Richard Marlink, Vladimir Novitsky, Max Essex
Rilpivirine (RPV) and Etravirine (ETR) are approved second-generation non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV treatment. There is a cross-resistance HIV mutation profile between first- and second-generation NNRTI drugs. We determined the prevalence of HIV-1 drug resistance mutations (DRMs) to RPV and ETR in Botswana. A total of 168 HIV-1 polymerase gene sequences from participants failing nevirapine (NVP)- or efavirenz (EFV)-containing regimens were analyzed for DRMs using the Stanford University HIV drug resistance database...
June 12, 2018: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/29592839/high-resolution-mass-spectrometry-based-methodologies-for-identification-of-etravirine-bioactivation-to-reactive-metabolites-in-vitro-and-in-vivo-approaches
#5
Ana L A Godinho, Inês L Martins, João Nunes, Catarina Charneira, Jorge Grilo, Diogo M Silva, Sofia A Pereira, Karina Soto, M Conceição Oliveira, M Matilde Marques, Cristina C Jacob, Alexandra M M Antunes
Drug bioactivation to reactive metabolites capable of covalent adduct formation with bionucleophiles is a major cause of drug-induced adverse reactions. Therefore, elucidation of reactive metabolites is essential to unravel the toxicity mechanisms induced by drugs and thereby identify patient subgroups at higher risk. Etravirine (ETR) was the first second-generation Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) to be approved, as a therapeutic option for HIV-infected patients who developed resistance to the first-generation NNRTIs...
July 1, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29550449/hiv-care-in-central-and-eastern-europe-how-close-are-we-to-the-target
#6
Deniz Gokengin, Cristiana Oprea, Josip Begovac, Andrzej Horban, Arzu Nazlı Zeka, Dalibor Sedlacek, Bayjanov Allabergan, Esmira A Almamedova, Tatevik Balayan, Denes Banhegyi, Pavlina Bukovinova, Nikoloz Chkhartishvili, Alymbaeva Damira, Edona Deva, Ivaylo Elenkov, Luljeta Gashi, Dafina Gexha-Bunjaku, Vesna Hadciosmanovic, Arjan Harxhi, Tiberiu Holban, Djorje Jevtovic, David Jilich, Justyna Kowalska, Djhamal Kuvatova, Natalya Ladnaia, Adkhamjon Mamatkulov, Aleksandra Marjanovic, Maria Nikolova, Mario Poljak, Kristi Rüütel, Azzaden Shunnar, Milena Stevanovic, Zhanna Trumova, Oleg Yurin
OBJECTIVES: The aim of this survey was to describe the current status of HIV care in the countries of Central and Eastern Europe and to investigate how close the region is to achieving the UNAIDS 2020 target of 90-90-90. METHODS: In 2014, data were collected from 24 Central and Eastern European countries using a 38-item questionnaire. RESULTS: All countries reported mandatory screening of blood and organ donors for HIV. Other groups subjected to targeted screening included people who inject drugs (PWID) (15/24, 62...
May 2018: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/29469716/associated-conditions-in-patients-with-multiple-dermatofibromas-case-reports-and-literature-review
#7
Surget V Beatrous, Ryan R Riahi, Stratton B Grisoli, Philip R Cohen
Dermatofibromas are benign, fibrohistiocytic, dermal tumors. Solitary dermatofibromas may be incidental findings, whereas multiple dermatofibromas may be associated with systemic conditions or previous therapies. Two women and one man with multiple dermatofibromas and an associated systemic condition, immunosuppression, or both, are described. Nine dermatofibromas developed in a woman with hypothyroidism, optic neuritis, and Arnold Chiari I malformation. Five dermatofibromas developed in a woman with breast cancer who had received several systemic antineoplastic therapies...
September 22, 2017: Dermatology Online Journal
https://www.readbyqxmd.com/read/29429441/characteristics-and-early-outcomes-of-children-and-adolescents-treated-with-darunavir-ritonavir-raltegravir-or-etravirine-containing-antiretroviral-therapy-in-the-western-cape-province-of-south-africa
#8
J Nuttall, V Pillay
BACKGROUND: There is an increasing need for third-line treatment regimens in HIV-infected children with antiretroviral treatment (ART) failure. Data are limited on darunavir/ritonavir (DRV/r)-, raltegravir (RAL)- and etravirine (ETR)-containing regimens in treatment-experienced children from resource-constrained settings receiving these drugs as part of routine care. OBJECTIVE: To describe the characteristics and early outcomes of treatment-experienced children (<20 years of age) in the Western Cape Province of South Africa treated with DRV/r-, RAL- or ETR-containing regimens...
February 1, 2018: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
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
#9
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)...
February 7, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29237008/pharmacokinetics-of-darunavir-cobicistat-and-etravirine-alone-and-co-administered-in-hiv-infected-patients
#10
José Moltó, Adrian Curran, Cristina Miranda, Elizabeth Challenger, José Ramón Santos, Esteban Ribera, Saye Khoo, Marta Valle, Bonaventura Clotet
Objectives: To determine the effect of etravirine on the pharmacokinetics of darunavir/cobicistat and vice versa. Safety and tolerability of this combination were also evaluated. Methods: Open-label, fixed-sequence trial in two cohorts of HIV-infected patients on therapy with darunavir/cobicistat 800/150 mg once daily (DRV cohort; n = 15) or etravirine 400 mg once daily (ETR cohort; n = 15). Etravirine or darunavir/cobicistat were added on days 1-14 and 1-7 in participants in the DRV or ETR cohort, respectively...
December 11, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29201980/experimental-data-of-co-crystals-of-etravirine-and-l-tartaric-acid
#11
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-in-vitro-and-in-vivo
#12
Morrie Lam, Natalia Mast, Irina A Pikuleva
Cytochrome P450 27A1 (CYP27A1) is a ubiquitous enzyme that hydroxylates cholesterol and other sterols. Complete CYP27A1 deficiency owing 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 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...
February 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29156381/structure-based-methods-to-predict-mutational-resistance-to-diarylpyrimidine-non-nucleoside-reverse-transcriptase-inhibitors
#13
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...
January 2018: 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
#14
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
#15
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...
November 10, 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
#16
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
#17
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
#18
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
#19
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
#20
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
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