Other substances

Camostat mesylate

A serine protease inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Camostat (mesylate) is a serine protease inhibitor. It has anti-inflammatory, antifibrotic, and potential antiviral activities (NCIt). Data of Ou et al. (2021) suggets that camostat blocks TMPRSS2 mediated viral entry at the cell membrane but does not impede TMPRSS2 mediated entry in endosomes.

Camostat mesylate on DrugBank
Camostat mesylate on PubChem
Camostat on Wikipedia

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Supporting references

Link	Tested on	Impact factor	Notes	Publication date
The anticoagulant nafamostat potently inhibits SARS-CoV-2 infection in vitro: an existing drug with multiple possible therapeutic effects Preprint	lung epithelium-derived Calu-3 cells		10-fold less active than nafamostat mesylate	Apr/23/2020
Alpha 1 Antitrypsin is an Inhibitor of the SARS-CoV2-Priming Protease TMPRSS2 TMPRSS2 Preprint	HEK-293T cell culture		inhibited TMPRSS2 proteolytic function	Oct/07/2020
Generation of human bronchial organoids for SARS-CoV-2 research Preprint	human bronchial organoids			May/26/2020
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing Small molecule	in silico	42.78		Apr/30/2020
SARS-CoV-2 and SARS-CoV differ in their cell tropism and drug sensitivity profiles Preprint	CaCo-2 cells		limited activity	Apr/05/2020
An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19 Preprint	in vitro			Jun/23/2020
Computational drug re-purposing targeting the spike glycoprotein of SARS-CoV-2 as an effective strategy to neutralize COVID-19 Spike protein Small molecule In silico	in silico	3.26	Predicted to bind the SARS-CoV-2 spike protein RBD.	Nov/06/2020
Hydroxychloroquine-mediated inhibition of SARS-CoV-2 entry is attenuated by TMPRSS2 Spike protein TMPRSS2 Cathepsin L In vitro Mechanism	hACE2-HEK293T cells; hACE2-H1299 cells; hACE2-H1975 cells; Vero cells; Calu-3 cells; SARS-CoV-2 S pseudovirus	6.22	Acts synergistically with <a href=	Jan/19/2021
Spontaneous binding of potential COVID-19 drugs (Camostat and Nafamostat) to human serine protease TMPRSS2 TMPRSS2 Small molecule In silico	in silico	6.02	Predicted to bind the active site of the TMPRSS2 protease (with less specificity than nafamostat).	Dec/28/2020
SARS-CoV-2 variants B.1.351 and P.1 escape from neutralizing antibodies Spike protein RNA Small molecule Peptide In vitro Antibody Mixed substance	Caco-2 cells; Vero cells; Sera of vaccinated individuals; (VSV) SARS-CoV-2 Spike-pseudotyped virus (WT, B.1.1.7, B.1.351, ant P.1 variants)	38.64	Camostat displayed in vitro inhibition of SARS-CoV-2 Spike-pseudotyped virus infection for all tested emergent Spike variants (B.1.1.7, B.1.351, and P.1).	Mar/20/2021
Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2 Small molecule In vitro Screening	Huh7.5 cells; Calu-3 cells; primary normal human bronchial epithelial cells; iPSC-derived AT2 cells; SARS-CoV-2 strain USA WA1/2020	8.11	Camostat inhibited SARS-CoV-2 infection in Calu-3 cells but not in Vero or Huh7.5 cells.	Mar/23/2021
Structure-based phylogeny identifies Avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice Small molecule Enzyme assay Peptide Animal model In vitro In silico	in silico; in vitro enzyme assay; Calu-3 2B4 cells; hACE2-BALB/c mice; (VSV) SARS-CoV-2 Spike pseudovirus; SARS-CoV-2 live virus	11.86	Camostat mesylate inhibited TMPRSS2 in vitro with an IC50 of ca. 1.01 nM. It inhibited pseudoviral entry in Calu-3 cells with an EC50 of ca. 0.7 μM. The compound significantly reduced viral replication in cell culture (more than a ten-fold decrease in viral RNA signal with a 1 μM dose). It significantly reduced lung viral loads in mice after a viral challenge.	Apr/12/2021

AI-suggested references

Link	Publication date
Structural Basis of SARS-CoV-2- and SARS-CoV-Receptor Binding and Small-Molecule Blockers as Potential Therapeutics.	Jun/25/2020
Low risk of the TMPRSS2 inhibitor camostat mesylate and its metabolite GBPA to act as perpetrators of drug-drug interactions.	Feb/27/2021
Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety.	Nov/22/2020
Camostat Mesylate May Reduce Severity of Coronavirus Disease 2019 Sepsis: A First Observation	Mar/23/2022
Human airway lineages derived from pluripotent stem cells reveal the epithelial responses to SARS-CoV-2 infection	May/23/2020
Virtual drug repurposing study against SARS-CoV-2 TMPRSS2 target	Jun/21/2020
The TMPRSS2 Inhibitor Nafamostat Reduces SARS-CoV-2 Pulmonary Infection in Mouse Models of COVID-19	Feb/11/2022
On a knife's edge of a COVID-19 pandemic: is containment still possible?	Mar/09/2020
Computational screening of phytochemicals from three medicinal plants as inhibitors of transmembrane protease serine 2 implicated in SARS-CoV-2 infection.	Sep/29/2021
Structural Basis of Covalent Inhibitory Mechanism of TMPRSS2-Related Serine Proteases by Camostat	Jan/31/2022
Inhibition of SARS-CoV-2 entry through the ACE2/TMPRSS2 pathway: a promising approach for uncovering early COVID-19 drug therapies	Jul/21/2020
Semi-Mechanistic Pharmacokinetic-Pharmacodynamic Model of Camostat Mesylate-Predicted Efficacy against SARS-CoV-2 in COVID-19	Apr/12/2022
Pharmacological Therapeutics Targeting RNA-Dependent RNA Polymerase, Proteinase and Spike Protein: From Mechanistic Studies to Clinical Trials for COVID-19	Jan/17/2022
Strong Binding of Leupeptin with TMPRSS2 Protease May Be an Alternative to Camostat and Nafamostat for SARS-CoV-2 Repurposed Drug: Evaluation from Molecular Docking and Molecular Dynamics Simulations	Jan/29/2021
Structural insights and inhibition mechanism of TMPRSS2 by experimentally known inhibitors Camostat mesylate, Nafamostat and Bromhexine hydrochloride to control SARS-coronavirus-2: A molecular modeling approach.	May/26/2021
Pharmacological Modulators of Autophagy as a Potential Strategy for the Treatment of COVID-19.	Apr/15/2021
Establishment of a pseudovirus neutralization assay based on SARS-CoV-2 S protein incorporated into lentiviral particles.	Jan/03/2022
Repurposing Therapeutics for Potential Treatment of SARS-CoV-2: A Review	Jun/30/2020
The Anticoagulant Nafamostat Potently Inhibits SARS-CoV-2 S Protein-Mediated Fusion in a Cell Fusion Assay System and Viral Infection In Vitro in a Cell-Type-Dependent Manner	Oct/20/2021
Virtual Screening of Natural Products against Type II Transmembrane Serine Protease (TMPRSS2), the Priming Agent of Coronavirus 2 (SARS-CoV-2)	May/12/2020
Synergistic Block of SARS-CoV-2 Infection by Combined Drug Inhibition of the Host Entry Factors PIKfyve Kinase and TMPRSS2 Protease	Aug/18/2021
Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity	Mar/04/2021
In Silico Molecular Characterization of Human TMPRSS2 Protease Polymorphic Variants and Associated SARS-CoV-2 Susceptibility	Oct/08/2021
Metadichol : A Novel Nanolipid Formulation That Inhibits SARS-CoV-2 and a Multitude of Pathological Viruses In Vitro	Jan/15/2022
Topical TMPRSS2 inhibition prevents SARS-CoV-2 infection in differentiated human airway cultures	Jul/23/2020

Clinical trials

ID	Title	Status	Phase	Start date	Completion date
NCT04353284	Camostat Mesylate in COVID-19 Outpatients	Completed	Phase 2	Jun/09/2020	Apr/22/2021
Alternative id - 2000027971 Interventions - Drug: Camostat Mesilate\|Other: Placebo Study type - Interventional Study results - No Results Available Locations - Yale University, New Haven, Connecticut, United States Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)\|Primary Purpose: Treatment Enrollment - 74 Age - 18 Years and older (Adult, Older Adult) Outcome measures - Change in SARS-COV-2 viral load\|Change in positive COVID-19 status\|Change in COVID-19 symptom severity\|Change in COVID-19 symptom frequency\|Change in body temperature
NCT04435015	The Utility of Camostat Mesylate in Patients With COVID-19 Associated Coagulopathy (CAC) and Cardiovascular Complications	Not yet recruiting	Phase 1\|Phase 2	Nov/01/2021	Dec/31/2021
Alternative id - 2000028279 Interventions - Drug: Camostat Mesylate\|Drug: Microcrystalline Cellulose, NF Study type - Interventional Study results - No Results Available Locations - Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)\|Primary Purpose: Treatment Enrollment - 200 Age - 18 Years and older (Adult, Older Adult) Outcome measures - Percent change in plasma D-Dimer\|Overall Safety and adverse event\|Change in plasma Fibrinogen levels\|Change in plasma troponin\|New onset cardiomyopathy\|Duration of intubation\|Length of stay in the intensive care unit\|Time to discharge from hospital\|Occurrence of major adverse cardiovascular events
NCT04355052	Open Label Study to Compare Efficacy, Safety and Tolerability of Hydroxychloroquine Combined With Azithromycin Compared to Hydroxychloroquine Combined With Camostat Mesylate and to "no Treatment" in SARS CoV 2 Virus	Recruiting	Phase 3	Apr/11/2020	Dec/11/2020
Alternative id - 7092-20-SMC Interventions - Drug: hydroxychloroquine in combination with camostat mesylate\|Drug: Hydroxychloroquine in combination of Azithromycin Study type - Interventional Study results - No Results Available Locations - Sheba Medical Center, Ramat Gan, Israel\|Sheba Medical Center, Tel HaShomer, Israel Study designs - Allocation: Randomized\|Intervention Model: Single Group Assignment\|Masking: None (Open Label)\|Primary Purpose: Treatment Enrollment - 250 Age - 18 Years to 120 Years (Adult, Older Adult) Outcome measures - clinical state as reflected by NEWS scoring\|positive PCR\|prevention of ICU\|prevention of assisted ventilation\|prevention of ECMO\|death
NCT04608266	CAMOVID : Evaluation of Efficacy and Safety of Camostat Mesylate for the Treatment of SARS-CoV-2 Infection - COVID-19 in Ambulatory Adult Patients	Terminated	Phase 3	Dec/03/2020	Dec/02/2021
Alternative id - APHP200702 Interventions - Drug: Camostat Mesylate\|Drug: Placebo Study type - Interventional Study results - No Results Available Locations - Centre Hospitalier Victor Dupouy, Argenteuil, France\|AP-HP Hôpital Henri Mondor, Créteil, France\|Centre Hospitalier Sud Ile de France - Melun, Melun, France\|AP-HP Hôpital Bichat, Paris, France\|APHP - Saint Louis, Paris, France\|Centre de Santé Richerand, Paris, France Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)\|Primary Purpose: Treatment Enrollment - 70 Age - 18 Years and older (Adult, Older Adult) Outcome measures - Hospitalization for COVID-19 deterioration or death without hospitalization\|Adverse events\|Serious adverse events\|Investigational medication discontinuation\|Hospitalization for COVID-19 deterioration or death without hospitalization, evaluated by independent adjudication comittee\|Clinical improvement using the Word Health Organization (WHO) COVID-19 scale\|Need for intensive care\|Duration of hospitalization\|Need for invasive mechanical ventilation for severe COVID-19\|Need for oxygen therapy for COVID-19\|Overall survival\|Duration of symptoms\|SARS-CoV-2 virological assessment\|SARS-CoV-2 serological assessment\|Peripheral blood lymphocyte phenotyping\|Acute kidney failure\|Renal function\|Concentration of urea in blood\|Concentration of potassium in blood\|Liver function\|Liver function (2)
NCT04681430	Reconvalescent Plasma/Camostat Mesylate Early in SARS-CoV-2 Q-PCR (COVID-19) Positive High-risk Individuals	Completed	Phase 2	Jan/08/2021	Oct/29/2021
Alternative id - RES-Q-HR\|2020-004695-18 Interventions - Biological: Convalescent plasma\|Drug: Camostat Mesilate\|Drug: Placebo for Camostat Mesilate\|Other: Standard of Care (SoC) Study type - Interventional Study results - No Results Available Locations - Abteilung Infektiologie Klinik für Innere Medizin II Department Innere Medizin Universitätsklinikum Freiburg, Freiburg im Breisgau, Baden-Württemberg, Germany\|Klinik und Poliklinik für Innere Medizin II Klinikum rechts der Isar Technische Universität München, München, Bavaria, Germany\|Universitätsklinikum Frankfurt Medizinische Klinik 2: Hämatologie, Onkologie, Hämostaseologie, Rheumatologie, Infektiologie/HIV, Frankfurt am Main, Hessen, Germany\|Universitätsklinikum Düsseldorf Klinik für Hepatologie und Infektiologie, Duesseldorf, North Rhine Westphalia, Germany\|Klinikum Dortmund, Dortmund, North Rhine-Westphalia, Germany\|Universitätsklinikum Essen, Essen, North Rhine-Westphalia, Germany Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)\|Primary Purpose: Treatment Enrollment - 22 Age - 18 Years and older (Adult, Older Adult) Outcome measures - WHO ordinal Covid-19 scale up to day 28\|Cumulative number WHO categories 4b-8\|Cumulative number WHO categories 3-4a\|Not hospitalized\|All-cause mortality\|Reinfection\|Secondary sclerosing cholangitis (SSC)\|chronic pulmonary disease as sequelae from COVID-19\|patients with remdesivir treatment\|COVID-19 WHO status of patients at start of remdesivir treatment\|patients with dexamethasone treatment\|COVID-19 WHO status of patients at start of dexamethasone treatment\|resolution of COVID-19 symptoms\|negative SARS-CoV-2-PCR test\|Oxygen therapy\|COVID-19 pneumonia\|Percentage of participants requiring mechanical ventilation\|Number of ventilation days per participant up to day 90\|hospital stay and intensive care\|Mortality\|SAEs\|Grade 3/4 AEs\|SARS-CoV-2 antibody IgA concentrations\|SARS-CoV-2 antibody IgG concentrations\|SARS-CoV-2 neutralizing antibody titers\|Plasma treatment screening failures

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