camostat mesilate / Generic mfg. - LARVOL DELTA

Searching for Novel Antiviral Agents as COVID19 Treatments: Guanidino Diaryl Thioureas. (PubMed, ChemMedChem) - "The findings suggest that reversible inhibitors may be suboptimal for TMPRSS2 targeting, as camostat and nafamostat exert their effects through irreversible covalent binding. Future efforts should focus on developing irreversible TMPRSS2 inhibitors to enhance antiviral efficacy against SARS-CoV-2."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Camostat mesylate restores intestinal barrier integrity and attenuated protein loss in experimental protein-losing enteropathy. (PubMed, Biochem Pharmacol) - "In a patient with Fontan-associated PLE, fecal A1AT decreased from 370.80 mg/dL to 254.90 mg/dL over 6 months of CM treatment, and serum albumin in a patient with Fontan-associated PLE increased from 1.9 g/dL to 4.2 g/dL over 21 months. These findings demonstrated that camostat mesylate improved intestinal barrier function and clinical outcomes, highlighting its potential for managing PLE following the Fontan operation."

Journal • Cardiovascular • Gastroenterology • Gastrointestinal Disorder • Heart Failure • Immunology • CLDN7 • TJP1

Therapeutic Potential of Tubular Serine Protease Inhibitors in Proteinuria. (PubMed, Am J Physiol Renal Physiol) - "Serine protease inhibitors, such as aprotinin, camostat mesylate, and nafamostat mesylate, as well as off-target effects of amiloride, have shown promise in preclinical and early clinical studies by mitigating these pathological processes. We identify key knowledge gaps, including the need for mechanistic pharmacodynamic trials, biomarker-guided patient selection using urinary serine protease activity, and long-term efficacy and safety studies. Serine protease inhibitors are a promising, underexplored therapeutic strategy in proteinuric conditions that may complement existing treatments by targeting specific pathogenic mechanisms involved in disease progression."

Journal • Chronic Kidney Disease • Fibrosis • Immunology • Inflammation • Nephrology • Renal Disease

A Bifunctional SARS-CoV-2 Entry Inhibitor Targeting the Host Protease TMPRSS2 and Viral Spike Protein HR1 Region. (PubMed, Int J Mol Sci) - "Herein, we report a series of bifunctional SARS-CoV-2 entry inhibitors formed by covalently linking a TMPRSS2 inhibitor, Camostat (Cm), and an HR1-targeting peptide fusion inhibitor IPB19 via a poly (ethylene glycol) (PEG) linker...We confirm that IP4X and IP4Z exhibit a dual-targeting mechanism by binding to both TMPRSS2 and HR1 region of S protein. These findings highlight the potential of the bifunctional inhibitors for further development as a novel multitarget therapy against SARS-CoV-2 infection and enrich the understanding of S-mediated entry of SARS-CoV-2 into host cells."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Difference in the inhibitory mechanism against TMPRSS2 between camostat and nafamostat: implications for drug design. (PubMed, Phys Chem Chem Phys) - "And finally, the novel TMPRSS2 inhibitor with potentially better performance was identified based on the principle of the lowest binding free energy. This work not only elucidates the inhibitory mechanisms of camostat and nafamostat, showing valuable theoretical insights, but also proposes a viable strategy for future molecular design, thereby exhibiting promising application prospects."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • TMPRSS2

Synergistic antiviral activity of a cathepsin B/L inhibitor and a TMPRSS2 inhibitor against SARS-CoV-2 in vitro and in vivo. (PubMed, Virology) - "The TMPRSS2 inhibitor, camostat, exhibited strong antiviral activity against WT virus but not del2, while the cathepsin B/L inhibitor, K11777, exhibited potent antiviral activity against the del2 virus...In summary, our study characterized K11777 as an inhibitor of S2' cleavage by cathepsins, highlighting the critical role of the S2' site in SARS-CoV-2 cellular entry. This research sheds light on the infection process and has implications for potential therapeutic interventions for SARS-CoV-2 infection."

Journal • Preclinical • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • CTSB • CTSS

C-Terminal Analogues of Camostat Retain TMPRSS2 Protease Inhibition: New Synthetic Directions for Antiviral Repurposing of Guanidinium-Based Drugs in Respiratory Infections. (PubMed, Int J Mol Sci) - "These function and binding data offer new directions for the synthesis of further analogues of camostat and of other guanidinium-based protease inhibitors that have yet to be refined via structure-activity relationship studies. Further investigation will support tailoring this class of drugs for repurposing in antiviral therapy."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Dummy imprinted electrochemical sensor for the selective detection of camostat mesylate. (PubMed, Mikrochim Acta) - "The developed sensor was also effectively used to measure CAM in commercial serum samples. In summary, the designed sensors demonstrated high sensitivity, selectivity, repeatability, and reproducibility against the CAM molecule."

Journal

Development of an inhalable dry powder formulation for inhibition of SARS-CoV-2. (PubMed, Int J Pharm X) - "Camostat was spray-dried together with the mucolytic agent N-acetylcysteine to produce co-amorphous microparticles with sufficient solubility after deposition. The IC50 values of the two dry powder formulations tested on a HEK293T/ACE2-TMPRSS2 cell line were 0.008 μg/mL and 0.019 μg/mL, respectively, which is at least 100 times lower than the cytotoxic concentration. This dry powder formulation serves as a prototype microparticle matrix for incorporating nanoscale drug carriers in the future."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

ACE-2 blockade and TMPRSS2 inhibition mitigate SARS-CoV-2 severity following cigarette smoke exposure in airway epithelial cells in vitro. (PubMed, Mol Ther Nucleic Acids) - "Knockdown of ACE-2 via an antisense oligonucleotide (ASO) reduced SARS-CoV-2 viral load and infection in CSE-exposed ferret airway cells that was augmented by co-administration of camostat mesylate to block TMPRSS2 activity. Smoking increases SARS-CoV-2 infection via upregulation of ACE2 and TMPRSS2."

Journal • Preclinical • Chronic Obstructive Pulmonary Disease • Immunology • Infectious Disease • Novel Coronavirus Disease • Pulmonary Disease • Respiratory Diseases • TMPRSS2

TMPRSS2: A Key Host Factor in SARS-CoV-2 Infection and Potential Therapeutic Target. (PubMed, Medeni Med J) - "Several TMPRSS2 inhibitors, including serine protease inhibitors, such as camostat mesylate and nafamostat, have demonstarted promise in blocking viral entry. The presence of TMPRSS2-ERG gene fusion, commonly found in prostate cancer, has also been linked to altered COVID-19 susceptibility, suggesting a complex interplay between viral infection and cancer biology. This review also discusses future perspectives, including large-scale genomic studies to identify high-risk individuals, the development of next-generation TMPRSS2 inhibitors, and potential broad-spectrum antiviral therapies targeting TMPRSS2."

Journal • Genito-urinary Cancer • Infectious Disease • Novel Coronavirus Disease • Oncology • Prostate Cancer • Respiratory Diseases • Solid Tumor • ERG • TMPRSS2

Role of CCK1 receptor in metabolic benefits of intestinal enteropeptidase inhibition in mice. (PubMed, PLoS One) - "Chronic inhibition of EP and trypsin (EP/T) with camostat (Foipan, FOY-305) or its active metabolite (FOY-251) causes weight loss in obese mice by reducing intestinal protein absorption and suppression of food intake, however, the mechanisms leading to appetite suppression are not well understood...In CCKR1 KO mice, FOY-251 caused greater weight loss, and increased protein calorie loss relative to that in WT mice, while having no effect on glycemic control or FGF21. Hence, CCK1R-dependent and -independent mechanisms modulate the metabolic effects of EP/T inhibition and may play a role in maintaining weight loss by this mechanism."

Journal • Preclinical • Obesity • FGF21

Formulation and In-Vitro Testing of Nebulized Camostat Mesylate Loaded Nanoliposomes for the Treatment of SARS-CoV- 2 Infection. (PubMed, AAPS PharmSciTech) - "Camo-pegNLs showed a significant antiviral effect on Vero cells compared to no treatment group (p < 0.01). An efficacious nebulized Camo-pegNLs suspension product was successfully developed for direct lung delivery to Camo-pegNLs to treat the SARS-CoV- 2 infection."

Journal • Preclinical • Infectious Disease • Novel Coronavirus Disease • TMPRSS2

Trypstatin as a Novel TMPRSS2 Inhibitor with Broad-Spectrum Efficacy against Corona and Influenza Viruses. (PubMed, Adv Sci (Weinh)) - "Trypstatin inhibits TMPRSS2 and related proteases with high potency, exhibiting half-maximal inhibitory concentration values in the nanomolar range, comparable to the small molecule inhibitor camostat mesylate...In vivo, intranasal administration of Trypstatin to SARS-CoV-2-infected Syrian hamsters reduces viral titers and alleviates clinical symptoms. These findings highlight Trypstatin's potential as a broad-spectrum antiviral agent against TMPRSS2-dependent respiratory viruses."

Journal • Infectious Disease • Influenza • Novel Coronavirus Disease • Respiratory Diseases

CamoCO-19: The Impact of Camostat Mesilate on COVID-19 Infection (clinicaltrials.gov) - P1/2 | N=206 | Completed | Sponsor: University of Aarhus | Recruiting ➔ Completed | Phase classification: P2a ➔ P1/2 | N=580 ➔ 206

Enrollment change • Phase classification • Trial completion • Infectious Disease • Novel Coronavirus Disease

Phase 2 Open-label, Single-arm, Multi-center Clinical Trial to Evaluate the Efficacy and Safety of Camostat Mesylate in Patients with Protein-losing Enteropathy After Fontan Operation. (PubMed, Pediatr Cardiol) - P2 | "CM demonstrated significant reductions in gastrointestinal protein losses, particularly in patients with baseline diarrhea. Trial registration NCT05474664."

Journal • P2 data • Gastrointestinal Disorder

Synergistic Antiviral Activity of Xanthan Gum and Camostat Against Influenza Virus Infection. (PubMed, Viruses) - "The results demonstrated that in the combination-treated groups, XG and camostat exhibited significantly higher cell viability at lower concentrations compared to the single-treatment groups for influenza A H1N1, A H3N2, and B type. These results indicate that XG possesses potential capabilities in inhibiting respiratory viruses and may be utilized in conjunction with existing antiviral treatments."

Journal • Infectious Disease • Influenza • Respiratory Diseases

CLU/PROK2 in chronic Hepatitis B: an exploratory study on its role as a potential diagnostic biomarker and therapeutic target with persistent positive in HBV DNA level receiving entecavir treatment (APASL 2025) - "Molecular docking and virtual screening pinpointed Camostat mesylate, c- Kit-IN-1, and Mocetinostat as the top drug candidates for targeting CLU and PROK2. Elevated CLU and PROK2 levels are associated with an increased risk of CHB, and this enzyme is notably overexpressed in CHB patients' serum and liver tissues. CLU and PROK2 could potentially act as a diagnostic biomarker, providing new avenues for diagnosing and treating CHB. Table and Figure:Figure 1.Figure 3."

Biomarker • Chronic Kidney Disease • Focal Segmental Glomerulosclerosis • Glomerulonephritis • Hepatitis B • Hepatology • Infectious Disease • Inflammation • Nephrology • Renal Disease • CTSS • ITGB3

SARS-CoV-2 infection of human lung ALI cultures reveals basal cells as relevant targets. (PubMed, J Infect Dis) - "Collectively, our data emphasize the critical role of basal cells in facilitating SARS-CoV-2 dissemination within the upper respiratory tract and their substantial contribution to the epithelial immune response. Furthermore, our results highlight the potential of local application of Camostat mesylate as an effective strategy for inhibiting SARS-CoV-2 infection and mitigating associated immune activation early on."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

CamKid: Effect Camostat for Kidney Protection in Chronic Kidney Disease (clinicaltrials.gov) - P2 | N=40 | Recruiting | Sponsor: Odense University Hospital

New P2 trial • Chronic Kidney Disease • Nephrology • Renal Disease

Imaging flow cytometry reveals the mechanism of equine arteritis virus entry and internalization. (PubMed, Sci Rep) - "Moreover, we evaluated the effectiveness of two inhibitors targeting cellular factors involved in facilitating viral entry: ammonium chloride, which disrupts endocytosis, and camostat mesylate, which inhibits the activity of serine proteases. The results demonstrated a clear distinction between effective and ineffective inhibitors. This study highlighted the potential of imaging flow cytometry to advance the study of viral entry and the evaluation of antiviral agents."

Journal • Infectious Disease

The Identification of Insect Specific iAANAT Inhibitors. (PubMed, Arch Biochem Biophys) - "We found a series of guanidines, amidines, and a hydroxamate, structurally related to diminazene, also inhibit the iAANATs, including camostat, gabexate, nafamostate, and panobinostat. Also, we report that adipoyl-CoA is a substrate for AmNAT1 and DcNAT and that succinoyl-CoA is a substrate for DcNAT. These results contribute to a growing body of data suggesting that N-dicarboxyacyl-amines are metabolites in insects and other organisms."

Journal

A Glimpse for the subsistence from pandemic SARS-CoV-2 infection. (PubMed, Bioorg Chem) - "Although some drug regimens and vaccines have shown safety in trials, none have been entirely successful yet. This review highlights, some of the potential antibodies (tocilizumab, Sarilumab, Avdoralimab, Lenzilumab, Interferon (alfa /beta /gamma)) screened against SARS-CoV-2 and the most promising drugs (Favipiravir, Hydroxychloroquine, Niclosamide, Ribavirin, Baricitinib, Remdesivir, Arbidol Losartan, Ritonavir, Lopinavir, Baloxavir, Nitazoxanide, Camostat) in various stages of development with their synthetic protocol and their clinical projects are discussed to counter COVID -19."

Journal • Review • Cardiovascular • Gastrointestinal Disorder • Infectious Disease • Nephrology • Novel Coronavirus Disease • Pneumonia • Respiratory Diseases

Camostat Mesylate for Protein-losing Enteropathy After Fontan Operation (clinicaltrials.gov) - P2 | N=19 | Completed | Sponsor: Seoul National University Hospital | Not yet recruiting ➔ Completed | N=30 ➔ 19

Enrollment change • Trial completion

Development of a new platform for testing antiviral drugs using coronavirus-infected human nasal mucosa organoids (PubMed, Nan Fang Yi Ke Da Xue Xue Bao) - "Human nasal mucosa organoids with SARS-CoV-2 infection can serve as platforms for screening and testing antiviral drugs, particularly those intended for nasal administration."

Journal • Infectious Disease • Novel Coronavirus Disease • Otorhinolaryngology • Respiratory Diseases