camostat mesilate / Generic mfg. - LARVOL DELTA

Intelligent Programmable Membrane Nanosponge for Early Virus Blocking. (PubMed, Adv Sci (Weinh)) - "Herein, we engineered smart, programmable membrane-engineered nanosponges (ACNPs) displaying high-density ACE2 and encapsulating the viral entry inhibitor camostat...After intratracheal nebulization, ACNPs persist in the lungs for over 72 h, achieving over 92% viral clearance and 80%-100% survival. ACNPs also inhibit authentic HCoV-NL63 infection, offering a deployable, non-invasive, universal strategy for early intervention against pan ACE2-dependent coronaviruses and future "X viruses"."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Structure activity relationship guided activity based profiling reveals camostat in vivo selectivity in gut mucosa (ACS-Fall 2026) - "Together, these results demonstrate that integrating SAR informed probe design with chemoproteomics enables mechanistic deconvolution of in vivo target engagement and provides actionable guidance for optimizing serine protease inhibitor scaffolds. Medicinal Chemistry Impact: This work establishes a practical SAR workflow—design minimally perturbing clickable analogs, quantify tissue level engagement, and validate hits biochemically—to convert reversible covalent inhibitor potency into in vivo selectivity rules that guide scaffold optimization and derisk repurposing."

Preclinical • ST14

Structure activity relationship guided activity based profiling reveals camostat in vivo selectivity in gut mucosa | Poster Board #1769 (ACS-Fall 2026) - "Together, these results demonstrate that integrating SAR informed probe design with chemoproteomics enables mechanistic deconvolution of in vivo target engagement and provides actionable guidance for optimizing serine protease inhibitor scaffolds. Medicinal Chemistry Impact: This work establishes a practical SAR workflow—design minimally perturbing clickable analogs, quantify tissue level engagement, and validate hits biochemically—to convert reversible covalent inhibitor potency into in vivo selectivity rules that guide scaffold optimization and derisk repurposing."

Preclinical • ST14

Nicotine and cotinine enhance SARS-CoV-2 entry through distinct but complementary mechanisms in human respiratory epithelial cells. (PubMed, J Virol) - "In contrast, ACE2 and TMPRSS2 inhibitors (chloromethylketone and camostat) had limited effects on viral spike protein cleavage and only partially reduced the viral entry enhancement induced by nicotine and cotinine...These findings suggest that both tobacco smoking and E-cigarette vaping may exacerbate COVID-19 infection rates and severity and provide new insights into how nicotine and cotinine contribute to viral susceptibility. This research underscores the need for public health measures to address the heightened risk posed by tobacco smoking and E-cigarette vaping to encounter the SARS-CoV-2 infection."

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

Green-Synthesized Silver Nanoparticles from Zingiber officinale: Physicochemical Characterization, Antibacterial Activity, and TMPRSS2-Modulating Potential. (PubMed, Nanomaterials (Basel)) - "In a fluorometric enzyme assay, the silver nanoparticles inhibited TMPRSS2 activity in a concentration-dependent manner, achieving 51.24% inhibition at 100 µg/mL and an estimated IC50 of 40.06 µg/mL. Although the inhibitory activity was lower than that of Camostat, the findings suggest that ginger-mediated silver nanoparticles represent promising plant-based nano-bioactive systems for further investigation of TMPRSS2 modulation."

Journal • Infectious Disease

Individual patient data meta-analysis and systematic review evaluating camostat mesilate to treat COVID-19. (PubMed, J Clin Transl Sci) - "Camostat did not improve the rate of change in viral load (difference in rate of change = 0.11 Ct value/day higher, 95% credible interval 2.04 lower to 2.23 higher) or time to symptom resolution (hazard ratio = 0.87, 95% credible interval 0.51, 1.55) when compared to placebo. Despite its theoretically promising mode of action, camostat did not demonstrate a statistically significant virologic or clinical benefit in treating COVID-19, highlighting the complexity of drug repurposing in emergency health situations."

Journal • Retrospective data • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Application of a glyceride-mimetic prodrug strategy to deliver protease inhibitors to gut lymph to alleviate organ failure. (PubMed, J Control Release) - "We thus synthesised a series of gut lymph directing glyceride-mimetic prodrugs of 4-(4-guanidinobenzoyloxy) phenylacetic acid (GBPA), the active metabolite of the serine protease inhibitor camostat, and tested their pharmacokinetics and therapeutic utility in a rat model of AP...These findings demonstrate that lymph-targeted glyceride prodrugs of GBPA can attenuate organ injury in experimental AP. Future studies will determine the efficacy of the prodrugs in other ACIs such as hemorrhagic shock and sepsis."

Journal • Hematological Disorders • Hepatology • Infectious Disease • Liver Failure • Pancreatitis • Septic Shock

Temperature and developmental stage govern intestinal susceptibility to human coronavirus 229E. (PubMed, Proc Natl Acad Sci U S A) - "Furthermore, we show that camostat, a serine protease inhibitor, significantly reduces HCoV-229E replication in HIEs, confirming a critical role for host serine protease activity. Collectively, these findings establish HIEs as a relevant model for HCoV-229E-host interactions and reveal temperature- and age-dependent determinants governing intestinal permissiveness to this seasonal coronavirus."

Journal • Infectious Disease • Novel Coronavirus Disease • Pediatrics • Respiratory Diseases • STAT3

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

Enrollment open • Chronic Kidney Disease • Nephrology • Renal Disease

Camostat–polysaccharide dual-action nasal spray for mucosal barrier-driven prevention of viral infections (ESCMID Global 2026) - No abstract available

Infectious Disease

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

Trial completion • Chronic Kidney Disease • Nephrology • Renal Disease

SARS-CoV-2 infects human primary cytotrophoblasts mainly through a non-canonical entry route. (PubMed, Mol Hum Reprod) - "To investigate viral entry routes, cells were treated with Camostat mesylate (an inhibitor of the co-entry factor TMPRSS2) or chloroquine phosphate (an endosomal entry inhibitor) and viral fitness was assessed by plaque assays. Notably, JEG-3 cells represent an appropriate and convenient model for studying trophoblast infection by SARS-CoV-2, as they exhibit high permissiveness to the ancestral strain, and the SARS-CoV-2 entry pathway is similar to that in villous cytotrophoblasts. Overall, this study reveals that the cytotrophoblastic permissiveness to SARS-CoV-2 depends on the viral genetic nature and provides new insights into its entry route in human trophoblasts."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Impact of COVID-19 Monoclonal Antibody Therapy on Subsequent Vaccine-elicited SARS-CoV-2 Immune Responses. (PubMed, J Infect Dis) - P4 | "Prior anti-SARS-CoV-2 mAb treatment limits endogenous RBD-focused B-cell responses to later mRNA vaccination without measurably affecting T-cell immunity. Timing of vaccination after mAb therapy may matter and warrants study."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • CD4 • CD8

SARS-CoV-2 evolution enhances endocytic uptake while preserving TMPRSS2-dependent fusion. (PubMed, Front Immunol) - "Viral entry was investigated in four different human cell lines in the presence of camostat, an inhibitor of TMPRSS2-mediated fusion, and aloxistatin, a cathepsin protease inhibitor blocking viral endocytic entry (0.024-100 µM)...While replication in the upper airways and transmissibility are enhanced, the capacity to infect the lower respiratory tract is preserved, which may pose a risk for immunocompromised individuals. The combination of Δ69/Δ70, L452R, and mutations at position 486 may confer a selective advantage, as this constellation is now prevalent in nearly all circulating SARS-CoV-2 lineages."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

A Nasal Spray Combining Camostat with a Natural Polysaccharide for the Prevention of Viral Infection via Nasal Mucosal Barrier Formation and Entry Inhibition. (PubMed, Int J Mol Sci) - "Furthermore, suppression of transmembrane protease, serine 2 (TMPRSS2) expression, a key factor in influenza virus entry, was observed in mouse lung tissues. These findings suggest that the Camostat-Polysaccharide Dual-Action Nasal Spray (CPNS), currently under development, holds promise as a non-invasive, first-line barrier to prevent the initial infection and replication of respiratory viruses."

Journal • Infectious Disease • Influenza • Otorhinolaryngology • Respiratory Diseases • TMPRSS2

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 ) - "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