Remdesivir: Review of Pharmacology, Pre‐clinical Data, and Emerging Clinical Experience for COVID‐19

Jorgensen, Sarah C J; Kebriaei, Razieh; Dresser, Linda

doi:10.1002/phar.2429

Cited by 230 publications

(270 citation statements)

References 35 publications

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“…The low level of the parent drug could be due to the high esterase activities in mouse blood in the current study [17]. However, the level of RDV in human plasma was not low [18], which might be due to the species differences in esterase activities between humans and mice [17]. However, nucleoside metabolites were also the predominant components for other nucleoside prodrugs or in other species [7,19].…”

Section: Discussionmentioning

confidence: 65%

Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice

Yang

et al. 2020

Acta Pharmacol Sin

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Remdesivir (RDV) exerts anti-severe acute respiratory coronavirus 2 activity following metabolic activation in the target tissues. However, the pharmacokinetics and tissue distributions of the parent drug and its active metabolites have been poorly characterized to date. Blood and tissue levels were evaluated in the current study. After intravenous administration of 20 mg/kg RDV in mice, the concentrations of the parent drug, nucleotide monophosphate (RMP) and triphosphate (RTP), as well as nucleoside (RN), in the blood, heart, liver, lung, kidney, testis, and small intestine were quantified. In blood, RDV was rapidly and completely metabolized and was barely detected at 0.5 h, similar to RTP, while its metabolites RMP and RN exhibited higher blood levels with increased residence times. The area under the concentration versus time curve up to the last measured point in time (AUC 0-t) values of RMP and RN were 4558 and 136,572 h•nM, respectively. The maximum plasma concentration (C max) values of RMP and RN were 2896 nM and 35,819 nM, respectively. Moreover, RDV presented an extensive distribution, and the lung, liver and kidney showed high levels of the parent drug and metabolites. The metabolic stabilities of RDV and RMP were also evaluated using lung, liver, and kidney microsomes. RDV showed higher clearances in the liver and kidney than in the lung, with intrinsic clearance (CL int) values of 1740, 1253, and 127 mL/(min•g microsomal protein), respectively.

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Section: Discussionmentioning

confidence: 65%

Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice

Yang

et al. 2020

Acta Pharmacol Sin

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“…Nanotechnology can provide significant advantages in terms of its application in emergency viral diseases such as COVID-19 (Lembo et al, 2018). According to the Food and Drug Administration (FDA), nanoscale systems present different physicochemical and biological properties, compared to macro Abbasi-Oshaghi et al, 2020;Grein et al, 2020;Holshue et al, 2020;Jorgensen et al, 2020;Wang M. et al, 2020 Faviparivir…”

Section: Nano Insights Into Diagnosis Treatment and Prevention Of Cmentioning

confidence: 99%

Is Nanotechnology Helping in the Fight Against COVID-19?

Cardoso

Moreira

Comparetti

et al. 2020

Front. Nanotechnol.

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“…Vários estudos in vitro e pré-clínicos em animais tem demonstrado seu amplo espectro de ação antiviral, incluindo contra infecções promovidas por SARS-CoV-2. 71,95,[117][118][119] Estes achados promissores levaram o remdesivir a estudos clínicos com pacientes hospitalizados com casos graves de COVID-19. Os resultados já divulgados indicaram melhora clínica em 36 dos 53 pacientes (68%) tratados.…”

Section: Inibidores Da Rna Polimerase Dependente De Rnaunclassified

COVID-19: Physiopathology and Targets for Therapeutic Intervention

Almeida¹,

Oliveira²,

Avelar³

et al. 2020

Rev. Virtual Quim.

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The pandemic status of COVID-19 was recorded by the World Health Organization (WHO) on March 11, 2020. Since then, more than 10 million cases have been confirmed worldwide, with more than 500,000 reported deaths. Throughout this period, efforts by the global scientific community have focused on understanding the disease process and searching on preventive (e.g. vaccines) or therapeutic (e.g. drugs) alternatives of treatment for COVID-19. The present review portrays the historical aspects associated with the discovery of SARS-CoV-2, the etiological agent of COVID-19, describes the pathophysiological aspects of the disease, the viral replication process and discusses the main molecular targets subject to therapeutic intervention, aiming the design, discovery and development of new drugs to treat COVID-19. O status pandêmico da COVID-19 foi reconhecido pela Organização Mundial da Saúde (OMS) em 11 de março de 2020. Desde então mais de 20 milhões de casos foram confirmados no mundo, com mais de 900 mil mortes reportadas. Ao longo deste período a comunidade científica mundial tem debruçado esforços em entender o desenvolvimento da doença e buscar alternativas de tratamento preventivo (p. ex., vacinas) ou terapêutico (p. ex., fármacos) para a COVID-19. A presente revisão retrata os aspectos históricos associados a descoberta do SARS-CoV-2, agente etiológico da COVID-19, pontua o processo fisiopatológico da doença, as etapas de replicação viral e discute os alvos moleculares passíveis de intervenção terapêutica, visando o desenho, descoberta e desenvolvimento de fármacos para o tratamento da COVID-19.

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Remdesivir: Review of Pharmacology, Pre‐clinical Data, and Emerging Clinical Experience for COVID‐19

Cited by 230 publications

References 35 publications

Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice

Pharmacokinetics and tissue distribution of remdesivir and its metabolites nucleotide monophosphate, nucleotide triphosphate, and nucleoside in mice

Is Nanotechnology Helping in the Fight Against COVID-19?

COVID-19: Physiopathology and Targets for Therapeutic Intervention

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