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Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety

Research output: Contribution to journalReviewResearchpeer-review

Harvard

Breining, P, Frølund, AL, Højen, JF, Gunst, JD, Staerke, NB, Saedder, E, Cases-Thomas, M, Little, P, Nielsen, LP, Søgaard, OS & Kjolby, M 2021, 'Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety', Basic & clinical pharmacology & toxicology, vol. 128, no. 2, pp. 204-212. https://doi.org/10.1111/bcpt.13533

APA

Breining, P., Frølund, A. L., Højen, J. F., Gunst, J. D., Staerke, N. B., Saedder, E., Cases-Thomas, M., Little, P., Nielsen, L. P., Søgaard, O. S., & Kjolby, M. (2021). Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety. Basic & clinical pharmacology & toxicology, 128(2), 204-212. https://doi.org/10.1111/bcpt.13533

CBE

Breining P, Frølund AL, Højen JF, Gunst JD, Staerke NB, Saedder E, Cases-Thomas M, Little P, Nielsen LP, Søgaard OS, Kjolby M. 2021. Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety. Basic & clinical pharmacology & toxicology. 128(2):204-212. https://doi.org/10.1111/bcpt.13533

MLA

Vancouver

Author

Breining, Peter ; Frølund, Anne Lier ; Højen, Jesper Falkesgaard ; Gunst, Jesper Damsgaard ; Staerke, Nina B ; Saedder, Eva ; Cases-Thomas, Manuel ; Little, Paul ; Nielsen, Lars Peter ; Søgaard, Ole S ; Kjolby, Mads. / Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety. In: Basic & clinical pharmacology & toxicology. 2021 ; Vol. 128, No. 2. pp. 204-212.

Bibtex

@article{72f756ece0754287a33e1d301d2b4e53,
title = "Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety",
abstract = "The coronavirus responsible for COVID-19, SARS-CoV-2, utilizes a viral membrane spike protein for host cell entry. For the virus to engage in host membrane fusion, SARS-CoV-2 utilizes the human transmembrane surface protease, TMPRSS2, to cleave and activate the spike protein. Camostat mesylate, an orally available well-known serine protease inhibitor, is a potent inhibitor of TMPRSS2 and has been hypothesized as a potential antiviral drug against COVID-19. In vitro human cell and animal studies have shown that camostat mesylate inhibits virus-cell membrane fusion and hence viral replication. In mice, camostat mesylate treatment during acute infection with influenza, also dependent on TMPRSS2, leads to a reduced viral load. The decreased viral load may be associated with an improved patient outcome. Because camostat mesylate is administered as an oral drug, it may be used in outpatients as well as inpatients at all disease stages of SARS-CoV-2 infection if it is shown to be an effective antiviral agent. Clinical trials are currently ongoing to test whether this well-known drug could be repurposed and utilized to combat the current pandemic. In the following, we will review current knowledge on camostat mesylate mode of action, potential benefits as an antiviral agent and ongoing clinical trials.",
keywords = "&#160, &lt, Animals, Antiviral Agents/administration & dosage, Antiviral drugs&#160, COVID-19/drug therapy, Camostat mesylate, Drug Repositioning, Esters/administration & dosage, Guanidines/administration & dosage, Humans, Immunotoxicology, Infection&#160, Lung, Mice, Patient Safety, Respiratory toxicology, Serine Endopeptidases/drug effects, Serine Proteinase Inhibitors/administration & dosage, Viral infections, drug repurposing, pulmonary or respiratory system&#160, tmprss2, pulmonary or respiratory system < Respiratory toxicology, Infection < Immunotoxicology, Antiviral drugs < Viral infections",
author = "Peter Breining and Fr{\o}lund, {Anne Lier} and H{\o}jen, {Jesper Falkesgaard} and Gunst, {Jesper Damsgaard} and Staerke, {Nina B} and Eva Saedder and Manuel Cases-Thomas and Paul Little and Nielsen, {Lars Peter} and S{\o}gaard, {Ole S} and Mads Kjolby",
note = "{\textcopyright} 2020 The Authors. Basic & Clinical Pharmacology & Toxicology published by John Wiley & Sons Ltd on behalf of Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).",
year = "2021",
month = feb,
doi = "10.1111/bcpt.13533",
language = "English",
volume = "128",
pages = "204--212",
journal = "Basic & Clinical Pharmacology & Toxicology Online",
issn = "1742-7843",
publisher = "Wiley-Blackwell Publishing Ltd",
number = "2",

}

RIS

TY - JOUR

T1 - Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety

AU - Breining, Peter

AU - Frølund, Anne Lier

AU - Højen, Jesper Falkesgaard

AU - Gunst, Jesper Damsgaard

AU - Staerke, Nina B

AU - Saedder, Eva

AU - Cases-Thomas, Manuel

AU - Little, Paul

AU - Nielsen, Lars Peter

AU - Søgaard, Ole S

AU - Kjolby, Mads

N1 - © 2020 The Authors. Basic & Clinical Pharmacology & Toxicology published by John Wiley & Sons Ltd on behalf of Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).

PY - 2021/2

Y1 - 2021/2

N2 - The coronavirus responsible for COVID-19, SARS-CoV-2, utilizes a viral membrane spike protein for host cell entry. For the virus to engage in host membrane fusion, SARS-CoV-2 utilizes the human transmembrane surface protease, TMPRSS2, to cleave and activate the spike protein. Camostat mesylate, an orally available well-known serine protease inhibitor, is a potent inhibitor of TMPRSS2 and has been hypothesized as a potential antiviral drug against COVID-19. In vitro human cell and animal studies have shown that camostat mesylate inhibits virus-cell membrane fusion and hence viral replication. In mice, camostat mesylate treatment during acute infection with influenza, also dependent on TMPRSS2, leads to a reduced viral load. The decreased viral load may be associated with an improved patient outcome. Because camostat mesylate is administered as an oral drug, it may be used in outpatients as well as inpatients at all disease stages of SARS-CoV-2 infection if it is shown to be an effective antiviral agent. Clinical trials are currently ongoing to test whether this well-known drug could be repurposed and utilized to combat the current pandemic. In the following, we will review current knowledge on camostat mesylate mode of action, potential benefits as an antiviral agent and ongoing clinical trials.

AB - The coronavirus responsible for COVID-19, SARS-CoV-2, utilizes a viral membrane spike protein for host cell entry. For the virus to engage in host membrane fusion, SARS-CoV-2 utilizes the human transmembrane surface protease, TMPRSS2, to cleave and activate the spike protein. Camostat mesylate, an orally available well-known serine protease inhibitor, is a potent inhibitor of TMPRSS2 and has been hypothesized as a potential antiviral drug against COVID-19. In vitro human cell and animal studies have shown that camostat mesylate inhibits virus-cell membrane fusion and hence viral replication. In mice, camostat mesylate treatment during acute infection with influenza, also dependent on TMPRSS2, leads to a reduced viral load. The decreased viral load may be associated with an improved patient outcome. Because camostat mesylate is administered as an oral drug, it may be used in outpatients as well as inpatients at all disease stages of SARS-CoV-2 infection if it is shown to be an effective antiviral agent. Clinical trials are currently ongoing to test whether this well-known drug could be repurposed and utilized to combat the current pandemic. In the following, we will review current knowledge on camostat mesylate mode of action, potential benefits as an antiviral agent and ongoing clinical trials.

KW - &#160

KW - &lt

KW - Animals

KW - Antiviral Agents/administration & dosage

KW - Antiviral drugs&#160

KW - COVID-19/drug therapy

KW - Camostat mesylate

KW - Drug Repositioning

KW - Esters/administration & dosage

KW - Guanidines/administration & dosage

KW - Humans

KW - Immunotoxicology

KW - Infection&#160

KW - Lung

KW - Mice

KW - Patient Safety

KW - Respiratory toxicology

KW - Serine Endopeptidases/drug effects

KW - Serine Proteinase Inhibitors/administration & dosage

KW - Viral infections

KW - drug repurposing

KW - pulmonary or respiratory system&#160

KW - tmprss2

KW - pulmonary or respiratory system < Respiratory toxicology

KW - Infection < Immunotoxicology

KW - Antiviral drugs < Viral infections

UR - http://www.scopus.com/inward/record.url?scp=85096695751&partnerID=8YFLogxK

U2 - 10.1111/bcpt.13533

DO - 10.1111/bcpt.13533

M3 - Review

C2 - 33176395

VL - 128

SP - 204

EP - 212

JO - Basic & Clinical Pharmacology & Toxicology Online

JF - Basic & Clinical Pharmacology & Toxicology Online

SN - 1742-7843

IS - 2

ER -

ID: 61374702