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10.1016/j.phrs.2020.104960 http://scihub22266oqcxt.onion/10.1016/j.phrs.2020.104960 32473310!7254006!32473310     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=32473310&cmd=llinks): Failed to open stream: HTTP request failed! 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Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system |pdf=|usr=}}{{32473310}} gab.com Text Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system JO: Pharmacol Res http://www.kidney.de/pget.php?&tw=1&pmid=32473310 #FOAvip Coronavirus Disease 2019 (COVID-19) caused by the emerging severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with a crude case fatality rate of about 0.5-10 % depending on locality. A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ivermectin, exhibited anti-SARS-CoV-2 activity in vitro and/or in a small number of patients. However, their clinical use may be limited by anti-SARS-CoV-2 50 % maximal effective concentrations (EC(50)) that exceeded their achievable peak serum concentrations (Cmax), side effects, and/or availability. To find more immediately available COVID-19 antivirals, we established a two-tier drug screening system that combines SARS-CoV-2 enzyme-linked immunosorbent assay and cell viability assay, and applied it to screen a library consisting 1528 FDA-approved drugs. Cetilistat (anti-pancreatic lipase), diiodohydroxyquinoline (anti-parasitic), abiraterone acetate (synthetic androstane steroid), and bexarotene (antineoplastic retinoid) exhibited potent in vitro anti-SARS-CoV-2 activity (EC(50) 1.13-2.01 muM). Bexarotene demonstrated the highest Cmax:EC(50) ratio (1.69) which was higher than those of chloroquine, hydroxychloroquine, and ivermectin. These results demonstrated the efficacy of the two-tier screening system and identified potential COVID-19 treatments which can achieve effective levels if given by inhalation or systemically depending on their pharmacokinetics. Twit Text FOAVip Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system ????Pharmacol Res http://www.kidney.de/pget.php?&tw=1&pmid=32473310 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=32473310 #FOAvip English Wikipedia <ref>{{Cite pmid|32473310}}</ref> Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system #MMPMID32473310 Yuan S; Chan JFW; Chik KKH; Chan CCY; Tsang JOL; Liang R; Cao J; Tang K; Chen LL; Wen K; Cai JP; Ye ZW; Lu G; Chu H; Jin DY; Yuen KY Pharmacol Res 2020[Sep]; 159 (ä): 104960 PMID32473310show ga Coronavirus Disease 2019 (COVID-19) caused by the emerging severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with a crude case fatality rate of about 0.5-10 % depending on locality. A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ivermectin, exhibited anti-SARS-CoV-2 activity in vitro and/or in a small number of patients. However, their clinical use may be limited by anti-SARS-CoV-2 50 % maximal effective concentrations (EC(50)) that exceeded their achievable peak serum concentrations (Cmax), side effects, and/or availability. To find more immediately available COVID-19 antivirals, we established a two-tier drug screening system that combines SARS-CoV-2 enzyme-linked immunosorbent assay and cell viability assay, and applied it to screen a library consisting 1528 FDA-approved drugs. Cetilistat (anti-pancreatic lipase), diiodohydroxyquinoline (anti-parasitic), abiraterone acetate (synthetic androstane steroid), and bexarotene (antineoplastic retinoid) exhibited potent in vitro anti-SARS-CoV-2 activity (EC(50) 1.13-2.01 muM). Bexarotene demonstrated the highest Cmax:EC(50) ratio (1.69) which was higher than those of chloroquine, hydroxychloroquine, and ivermectin. These results demonstrated the efficacy of the two-tier screening system and identified potential COVID-19 treatments which can achieve effective levels if given by inhalation or systemically depending on their pharmacokinetics. |*Betacoronavirus/drug effects/physiology[MESH] |Androstenes/pharmacology[MESH] |Animals[MESH] |Antiviral Agents/*pharmacology[MESH] |Benzoxazines/pharmacology[MESH] |Bexarotene/pharmacology[MESH] |COVID-19[MESH] |COVID-19 Drug Treatment[MESH] |Caco-2 Cells[MESH] |Cell Survival/drug effects[MESH] |Chlorocebus aethiops[MESH] |Coronavirus Infections/*drug therapy/virology[MESH] |Cytopathogenic Effect, Viral/drug effects[MESH] |Databases, Pharmaceutical[MESH] |Drug Approval[MESH] |Drug Evaluation, Preclinical/*methods[MESH] |Drug Repositioning[MESH] |Enzyme-Linked Immunosorbent Assay[MESH] |Humans[MESH] |Iodoquinol/pharmacology[MESH] |Pandemics[MESH] |Pneumonia, Viral/*drug therapy/virology[MESH] |SARS-CoV-2[MESH] |United States[MESH] |United States Food and Drug Administration[MESH] |Vero Cells[MESH] |Viral Load/drug effects[MESH]Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohyd(epmc).pdf DeepDyve Pubget Overpricing