About: Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system

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About: Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system
Creator	Jin, Dong-Yan Yuen, Kwok-Yung Chu, Hin Lu, Gang Ye, Zi-Wei Yuan, Shuofeng Cai, Jian-Piao Chan, Chris Wen, Kun Chan, Y Cao, Jianli Chan, Jasper Chik, Kenn Liang, R Chen, Lin-Lei Tsang, Jessica Cai, Wen Ccy, Chan Jfw, Chan Jol, Tsang Kkh, Chik Liang, Ronghui Tang, Kaiming
source	Elsevier; Medline; PMC
abstract	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) 1.13-2.01µM). 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.
has issue date	2020-05-28(xsd:dateTime)
bibo:doi	10.1016/j.phrs.2020.104960
bibo:pmid	32473310
has license	no-cc
sha1sum (hex)	9ad519eab4388637307c920a1d88a4941bde6a60
schema:url	https://doi.org/10.1016/j.phrs.2020.104960
resource representing a document's title	Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system
has PubMed Central identifier	PMC7254006
has PubMed identifier	32473310
schema:publication	Pharmacol Res
resource representing a document's body	covid:9ad519eab4388637307c920a1d88a4941bde6a60#body_text
is schema:about of	named entity 'anti-parasitic' named entity 'severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)' named entity 'exceeded' named entity 'potent' named entity 'number' named entity 'chloroquine' named entity 'screen' named entity 'COVID-19' covid:arg/9ad519eab4388637307c920a1d88a4941bde6a60 named entity 'retinoid' named entity 'Cetilistat' named entity 'case fatality rate' named entity 'effective' named entity 'synthetic' named entity 'hydroxychloroquine' named entity 'EC50' named entity 'demonstrated' named entity 'patients' named entity 'potential' named entity 'bexarotene' named entity 'lipase' named entity 'limited' named entity 'Bexarotene' named entity 'cetilistat' named entity 'abiraterone' named entity 'chloroquine' named entity 'FDA' named entity 'anti-parasitic' named entity 'severe acute respiratory syndrome coronavirus 2' named entity 'diiodohydroxyquinoline' named entity 'COVID-19' named entity 'hydroxychloroquine' named entity 'nafamostat' named entity 'steroid' named entity 'bexarotene' named entity 'diiodohydroxyquinoline' named entity 'abiraterone' named entity 'SARS-CoV-2' named entity 'SARS-CoV-2' named entity 'immunocompromised' named entity 'bexarotene' named entity 'EC50' named entity 'hydroxychloroquine' named entity 'amino acid' named entity 'screening assay' named entity 'A71' named entity 'abiraterone acetate' named entity 'chronic pancreatitis' named entity 'antivirals' named entity 'Cmax' named entity 'SARS-CoV-2' named entity 'culture medium' named entity 'monoclonal antibody' named entity 'MOI' named entity 'SARS-CoV' named entity 'coronaviruses' named entity 'receptor binding' named entity 'azithromycin' named entity 'nucleocapsid protein'

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