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Oseltamivir

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https://www.readbyqxmd.com/read/28214542/several-hpept1-transported-drugs-are-substrates-of-the-escherichia-coli-proton-coupled-oligopeptide-transporter-ydgr
#1
Bala K Prabhala, Nanda G Aduri, Mazhar Iqbal, Moazur Rahman, Michael Gajhede, Paul R Hansen, Osman Mirza
Proton-dependent oligopeptide transporters (POTs) are secondary active transporters found in all kingdoms of life. POTs utilize the proton electrochemical gradient for the uptake of nutrient dipeptides and tripeptides. The human POT hPepT1 is known to transport a number of drugs. As part of ongoing studies on substrate specificities of POTs from Escherichia coli, our aim in this study was to investigate whether bacterial POTs could also transport these drugs. For this, we selected the common orally administered drugs sulpiride, bestatin, valacyclovir, ampicillin and oseltamivir, that are all transported by hPepT1...
February 16, 2017: Research in Microbiology
https://www.readbyqxmd.com/read/28205506/prospective-surveillance-of-antiviral-resistance-in-hospitalized-infants-less-than-12-months-of-age-with-a-h3n2-influenza-infection-and-treated-with-oseltamivir
#2
Barbara Rath, Xi Chen, Vera Spies, Susann Muehlhans, Patrick Obermeier, Franziska Tief, Lea Seeber, Katharina Karsch, Jeanette Milde, Heino Skopnik, Brunhilde Schweiger, Susanne C Duwe
BACKGROUND: Infants exhibit elevated influenza virus loads and prolonged viral shedding, which may increase the risk for resistance development, especially in cases of suboptimal exposure to antiviral therapy. METHODS: We performed a prospective surveillance of hospitalized infants undergoing oseltamivir therapy during the 2008-2009 and 2011-2012 influenza seasons at two paediatric hospitals in Germany. A total of 37 infants less than one year of age with laboratory confirmed influenza A(H3N2) infection received oseltamivir as per physician's order for 5 days (2008-2009 season: 2mg/kg BID; 2011-2012 season: 2...
February 16, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28195559/selection-of-multi-drug-resistant-influenza-a-and-b-viruses-under-zanamivir-pressure-and-their-replication-fitness-in-ferrets
#3
Ding Yuan Oh, Jacqueline Panozzo, Sophie Vitesnik, Rubaiyea Farrukee, David Piedrafita, Jennifer Mosse, Aeron C Hurt
BACKGROUND: Intravenous zanamivir has been used to treat patients with severe influenza. Because the majority of cases (including immunocompromised patients) require the drug for an extended period of treatment, there is a higher risk that the virus will develop resistance. Therefore, knowing the possible amino acid substitutions that may arise in recently circulating influenza strains under prolonged zanamivir exposure and their impact on antiviral susceptibility is important. METHODS: Influenza A(H1N1)pdm09, A(H3N2) and B virus were serially passaged under increasing zanamivir pressure in vitro...
February 14, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28188897/unmasking-survival-biases-in-observational-treatment-studies-of-influenza-patients
#4
Martin Wolkewitz, Martin Schumacher
BACKGROUND: Several observational studies reported that Oseltamivir (Tamiflu) reduced mortality in infected and hospitalized patients. Due to the restriction of observation to hospital stay and time-dependent treatment assignment, such findings were prone to common types of survival bias (length, time-dependent and competing risk bias). METHODS: British hospital data from the FLU-CIN study group were used which included 1391 patients with confirmed pandemic influenza A/H1N1 2009 infection...
February 7, 2017: Journal of Clinical Epidemiology
https://www.readbyqxmd.com/read/28182988/design-in-silico-studies-synthesis-and-in%C3%A2-vitro-evaluation-of-oseltamivir-derivatives-as-inhibitors-of-neuraminidase-from-influenza-a-virus-h1n1
#5
Rocío M Neri-Bazán, Jazmín García-Machorro, David Méndez-Luna, Luis E Tolentino-López, Federico Martínez-Ramos, Itzia I Padilla-Martínez, Leopoldo Aguilar-Faisal, Marvin A Soriano-Ursúa, José G Trujillo-Ferrara, M Jonathan Fragoso-Vázquez, Blanca L Barrón, José Correa-Basurto
Since the neuraminidase (NA) enzyme of the influenza A virus plays a key role in the process of release of new viral particles from a host cell, it is often a target for new drug design. The emergence of NA mutations, such as H275Y, has led to great resistance against neuraminidase inhibitors, including oseltamivir and zanamivir. Hence, we herein designed a set of derivatives by modifying the amine and/or carboxylic groups of oseltamivir. After being screened for their physicochemical (Lipinski's rule) and toxicological properties, the remaining compounds were submitted to molecular and theoretical studies...
January 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28182419/expeditious-lead-optimization-of-isoxazole-containing-influenza-a-virus-m2-s31n-inhibitors-using-the-suzuki-miyaura-cross-coupling-reaction
#6
Fang Li, Yanmei Hu, Yuanxiang Wang, Chunlong Ma, Jun Wang
The existence of multidrug-resistant influenza viruses, coupled with the continuously antigenic shift and antigenic drift of influenza viruses, necessitates the development of the next-generation of influenza antivirals. As the AM2-S31N mutant persists in more than 95% of current circulating influenza A viruses, targeting the AM2-S31N proton channel appears to be a logical and valid approach to combating drug resistance. Starting from compound 1, an isoxazole compound with potent AM2-S31N channel blockage and antiviral activity, in this study we report an expeditious synthetic strategy that allows us to promptly explore the structure-activity relationships of isoxazole-containing AM2-S31N inhibitors...
February 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28179375/quantitative-prediction-of-human-renal-clearance-and-drug-drug-interactions-of-organic-anion-transporter-substrates-using-in-vitro-transport-data
#7
Sumathy Mathialagan, Mary A Piotrowski, David A Tess, Bo Feng, John Litchfiled, Manthena V Varma
Organic anion transporters (OATs) play an important role in the renal secretion of drugs, and their functional change can result in pharmacokinetic variability. In this study, we applied transport rates measured using OAT-transfected human embryonic kidney cells to predict human renal secretory and total renal clearance of 31 diverse drugs. Selective substrates to OAT1 (tenofovir), OAT2 (acyclovir and ganciclovir) and OAT3 (benzylpenicillin, oseltamivir acid) were used to obtain relative activity factors (RAFs) for these individual transporters by relating in vitro transport clearance to in vivo secretory clearance...
February 8, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28176519/-favipiravir-a-new-concept-of-antiviral-drug-against-influenza-viruses
#8
REVIEW
J Reina, N Reina
Favipiravir (T-705) is a new antiviral drug with strong inhibitory activity on RNA-dependent RNA polymerase of most RNA virus genome. All the influenza viruses have been shown fully sensitive to this new antiviral, including genetic strains to neuraminidase inhibitors (oseltamivir) resistance. Its mechanism of action lies in blocking viral replication and induction of lethal mutagenesis which determines the loss of infective activity of influenza viruses. Its activity is particularly intense in the respiratory tract, decreasing the viral load to non-infectious levels...
February 8, 2017: Revista Española de Quimioterapia: Publicación Oficial de la Sociedad Española de Quimioterapia
https://www.readbyqxmd.com/read/28176362/interdisciplinary-pharmacometrics-linking-oseltamivir-pharmacology-influenza-epidemiology-and-health-economics-to-inform-antiviral-use-in-pandemics
#9
M A Kamal, P F Smith, N Chaiyakunapruk, D B C Wu, C Pratoomsoot, K K C Lee, H Y Chong, R E Nelson, K Nieforth, G Dall, S Toovey, D C M Kong, A Kamauu, C M Kirkpatrick, C R Rayner
AIM: A modular interdisciplinary platform was developed to investigate the economic impact of oseltamivir treatment by dosage regimen under simulated influenza pandemic scenarios. METHODS: The pharmacology module consisted of a pharmacokinetic distribution of oseltamivir carboxylate AUC0-24h at steady state (simulated for 75 mg and 150 mg BID regimens for 5 days) and a pharmacodynamic distribution of viral shedding duration (Tshed ) obtained from phase II influenza inoculation data...
February 8, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28170438/the-effective-rate-of-influenza-reassortment-is-limited-during-human-infection
#10
Ashley Sobel Leonard, Micah T McClain, Gavin J D Smith, David E Wentworth, Rebecca A Halpin, Xudong Lin, Amy Ransier, Timothy B Stockwell, Suman R Das, Anthony S Gilbert, Rob Lambkin-Williams, Geoffrey S Ginsburg, Christopher W Woods, Katia Koelle, Christopher J R Illingworth
We characterise the evolutionary dynamics of influenza infection described by viral sequence data collected from two challenge studies conducted in human hosts. Viral sequence data were collected at regular intervals from infected hosts. Changes in the sequence data observed across time show that the within-host evolution of the virus was driven by the reversion of variants acquired during previous passaging of the virus. Treatment of some patients with oseltamivir on the first day of infection did not lead to the emergence of drug resistance variants in patients...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28159370/development-and-application-of-an-in-cell-cleanup-pressurized-liquid-extraction-with-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-to-detect-prohibited-antiviral-agents-sensitively-in-livestock-and-poultry-feces
#11
Huizhen Wu, Jianmei Wang, Hua Yang, Guoqin Li, Yinhuan Zeng, Wei Xia, Zuguang Li, Mingrong Qian
An in-cell cleanup pressurized liquid extraction was developed to analyze prohibited antiviral agents in livestock and poultry feces. Extraction and cleanup were integrated into one step. The extraction was performed using methanol-acetonitrile (1:1, v/v) with 0.5% glacial acetic acid at 90°C, and 0.75g of PSA was used as the adsorbent during the extraction procedure. Under optimal conditions, the average recoveries for 11 antiviral drugs were 71.5-112.5% at three spiked levels (20, 40, and 100μgkg(-1)). The detection limits and detection quantitations of the analysis method for the eleven antiviral drugs were 0...
March 10, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28155963/stereoisomers-of-oseltamivir-synthesis-in-silico-prediction-and-biological-evaluation
#12
Viktória Hajzer, Roman Fišera, Attila Latika, Július Durmis, Jakub Kollár, Vladimír Frecer, Zuzana Tučeková, Stanislav Miertuš, František Kostolanský, Eva Varečková, Radovan Šebesta
Oseltamivir is an important antiviral drug, which possess three chirality centers in its structure. From eight possible stereoisomers, only two have been synthesized and evaluated so far. We describe herein the stereoselective synthesis, computational activity prediction and biological testing of another three diastereoisomers of oseltamivir. These isomers have been synthesized using stereoselective organocatalytic Michael addition, cyclization and reduction. Their binding to viral neuraminidase N1 of influenza A virus was evaluated by quantum-chemical calculations and their anti-influenza activities were tested by an in vitro virus-inhibition assay...
February 3, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28146320/influenza-antivirals-currently-in-late-phase-clinical-trial
#13
Paulina Koszalka, Danielle Tilmanis, Aeron C Hurt
Influenza antiviral drugs are important for the control of influenza, most specifically for the treatment of influenza patients with severe disease following infection with a seasonal influenza virus, a newly emerging influenza strain, or in the event of a pandemic. Many influenza antivirals that are currently under investigation in late stage clinical trials differ in their mechanism of action compared to drugs currently licensed for the treatment of influenza. Nitazoxanide and DAS181 target components of the host cell and alter the ability of the virus to replicate efficiently, while small molecule drugs such as T705, JNJ63623872 and S-033188 bind to the viral polymerase complex and restrict viral replication...
February 1, 2017: Influenza and Other Respiratory Viruses
https://www.readbyqxmd.com/read/28128091/development-of-oseltamivir-and-zanamivir-resistance-in-influenza-a-h1n1-pdm09-virus-denmark-2014
#14
Ramona Trebbien, Svend Stenvang Pedersen, Kristine Vorborg, Kristina Træholt Franck, Thea Kølsen Fischer
Antiviral treatment of immunocompromised patients with prolonged influenza virus infection can lead to multidrug resistance. This study reveals the selection of antiviral resistance mutations in influenza A(H1N1)pdm09 virus in an immunocompromised patient during a 6-month period. The patient was treated with two courses of oseltamivir (5 days and 2 months, respectively), with the first course starting at symptom onset, and subsequently zanamivir (2 months and 10 days, respectively). Respiratory samples were investigated by Sanger and next generation sequencing (NGS) and, for NGS data, low-frequency-variant-detection analysis was performed...
January 19, 2017: Euro Surveillance: Bulletin Européen sur les Maladies Transmissibles, European Communicable Disease Bulletin
https://www.readbyqxmd.com/read/28115874/optic-neuritis-and-acute-anterior-uveitis-associated-with-influenza-a-infection-a-case-report
#15
Hayate Nakagawa, Hidetaka Noma, Osamu Kotake, Ryosuke Motohashi, Kanako Yasuda, Masahiko Shimura
BACKGROUND: A few reports have described ocular complications of influenza A infection, such as impaired ocular movement, parasympathetic ocular nerve, keratitis, macular lesion, and frosted branch angiitis. We encountered a rare case of acute anterior uveitis and optic neuritis associated with influenza A infection. CASE PRESENTATION: A 70-year-old man presented with symptoms of upper respiratory tract infection. A rapid diagnostic test showed a positive result for influenza A...
2017: International Medical Case Reports Journal
https://www.readbyqxmd.com/read/28112927/selective-inhibitors-of-human-liver-carboxylesterase-based-on-a-%C3%AE-lapachone-scaffold-novel-reagents-for-reaction-profiling
#16
M Jason Hatfield, Jingwen Chen, Ellie M Fratt, Liying Chi, John C Bollinger, Randall J Binder, John Bowling, Janice L Hyatt, Jerrod Scarborough, Cynthia Jeffries, Philip M Potter
Carboxylesterases (CEs) are ubiquitous enzymes that are responsible for the metabolism of xenobiotics, including drugs such as irinotecan and oseltamivir. Inhibition of CEs significantly modulates the efficacy of such agents. We report here that β-lapachone is a potent, reversible CE inhibitor with Ki values in the nanomolar range. A series of amino and phenoxy analogues have been synthesized, and although the former are very poor inhibitors, the latter compounds are highly effective in modulating CE activity...
February 7, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28105854/t-705-favipiravir-suppresses-tumor-necrosis-factor-%C3%AE-production-in-response-to-influenza-virus-infection-a-beneficial-feature-of-t-705-as-an-anti-influenza-drug
#17
T Tanaka, T Kamiyama, T Daikoku, K Takahashi, N Nomura, M Kurokawa, K Shiraki
Influenza virus infection induces the production of various cytokines, which play important roles in the pathogenesis of infection. Among the cytokines induced by influenza, tumor necrosis factor (TNF)-α production has been correlated with the severity of lung lesions. We investigated the effects of T-705 (Favipiravir, 6-fluoro-3-hydroxy-2-pyrazinecarboxamide) on cytokine production due to influenza virus infection in vitro and in vivo, compared with oseltamivir or GS 4071, an active form of oseltamivir. TNF-α production in mouse macrophage-derived P388D1 cells infected with the influenza virus was lower following treatment with T-705 at concentrations of 0...
January 25, 2017: Acta Virologica
https://www.readbyqxmd.com/read/28101187/severe-pneumonia-due-to-infection-with-candida-krusei-in-a-case-of-suspected-middle-east-respiratory-syndrome-a-case-report-and-literature-review
#18
Mingming Tan, Junwei Wang, Peiyang Hu, Bin Wang, Wanghua Xu, Jiao Chen
Candida krusei (C. krusei) pneumonia is a rare infection that is frequently associated with a poor outcome. The present study reports an unusual case of C. krusei pneumonia that was initially suspected to be a Middle East respiratory syndrome (MERS) case. A 64-year-old Saudi Arabian male patient was admitted to our hospital with complaints of cough and dyspnea that persisted for 6 days. The patient presented fever (oral temperature, 38.5°C) and slight tachypnea (25 respirations/min). A chest computerized tomography demonstrated unclear lung fields, diffuse pathological changes in the two lungs and multiple lymphadenectasis in the retrocaval and para-aortic arch area...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28094141/intravenous-zanamivir-or-oral-oseltamivir-for-hospitalised-patients-with-influenza-an-international-randomised-double-blind-double-dummy-phase-3-trial
#19
Francisco M Marty, Joan Vidal-Puigserver, Carol Clark, Sandeep K Gupta, Esperanza Merino, Denis Garot, Marianne J Chapman, Frédérique Jacobs, Eduardo Rodriguez-Noriega, Petr Husa, Denise Shortino, Helen A Watson, Phillip J Yates, Amanda F Peppercorn
BACKGROUND: Neuraminidase inhibitors are effective for the treatment of acute uncomplicated influenza. However, there is an unmet need for intravenous treatment for patients admitted to hospital with severe influenza. We studied whether intravenous zanamivir was a suitable treatment in this setting. METHODS: In this international, randomised, double-blind, double-dummy, phase 3 trial, we recruited patients aged 16 years or older with severe influenza admitted to 97 hospitals from 26 countries...
February 2017: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/28067324/the-in-vivo-efficacy-of-neuraminidase-inhibitors-cannot-be-determined-from-the-decay-rates-of-influenza-viral-titers-observed-in-treated-patients
#20
John Palmer, Hana M Dobrovolny, Catherine A A Beauchemin
Antiviral therapy is a first line of defence against new influenza strains. Current pandemic preparations involve stock- piling oseltamivir, an oral neuraminidase inhibitor (NAI), so rapidly determining the effectiveness of NAIs against new viral strains is vital for deciding how to use the stockpile. Previous studies have shown that it is possible to extract the drug efficacy of antivirals from the viral decay rate of chronic infections. In the present work, we use a nonlinear mathematical model representing the course of an influenza infection to explore the possibility of extracting NAI drug efficacy using only the observed viral titer decay rates seen in patients...
January 9, 2017: Scientific Reports
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