Camostat

Pharmacology

It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). For chronic pancreatitis camostat's typical dose is 600 mg daily, for postoperative reflux esophagitis 300 mg are taken. The daily dose is split in 3 doses and taken after each meal.

Side effects

As side effects allergic reactions including anaphylaxis, hypersensitivity, hyperkalemia, platelet and leukocyte depletion, liver dysfunction, jaundice have been reported.

COVID-19

Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. Another in vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19. It is currently in many Phase 1 and Phase 2 clinical trials.

Camostat decreased CRP levels better compared to Lopinavir/Ritonavir in a small study of mild COVID-19 patients. Camostat decreased COVID-19 severity, improved inflammatory markers and oxygenation compared to hydroxychloroquine treated patients.

A study of 205 COVID-19 patients treated with Camostat, carried out at Aarhus University Hospital in Denmark and concluding in April 2021, showed no noticeable effects of Camostat on duration of hospitalisation or severity of the cases, but noted that higher doses (the study used 600 mg Camostat daily dosage) might still have a possible effect.

On July 1, 2021, the AIDS Clinical Trials Group announced that the Camostat group on the "ACTIV-2 Outpatient Monoclonal Antibodies and Other Therapies Trial" would not be moving forward to Phase 3. The trial demonstrated no safety concerns but also no changes in viral shedding or symptom improvement.

References

References

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7. (2015). "The serine protease inhibitor camostat mesilate attenuates the progression of chronic kidney disease through its antioxidant effects". Nephron.
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10. (June 2012). "Simultaneous treatment of human bronchial epithelial cells with serine and cysteine protease inhibitors prevents severe acute respiratory syndrome coronavirus entry". Journal of Virology.
11. (April 2020). "SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor". Cell.
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15. (2020-12-15). "Foistar(Camostat mesylate) associated with the significant decrease in CRP levels compared to Kaletra(Lopinavir/Ritonavir) treatment in Korean mild COVID-19 pneumonic patients.".
16. (November 2020). "Camostat Mesylate May Reduce Severity of Coronavirus Disease 2019 Sepsis: A First Observation". Critical Care Explorations.
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18. "ACTG announces Camostat will not advance to phase 3 in outpatient treatment study for COVID-19".