Camostat
Camostat Uses, Dosage, Side Effects, Food Interaction and all others data.
Camostat mesylate, or FOY-305, is a synthetic serine protease inhibitor. It was first described in the literature in 1981, as part of research on the inhibition of skin tumors in mice. Camostat mesylate inhibits cholecystokinin, pro-inflammatory cytokines, and serine proteases, leading to it being investigated for multiple indications including the treatment of COVID-19.
Camostat mesylate was first approved in Japan in January 2006.
Camostat mesylate is a protease inhibitor used to treat chronic pancreatitis. The duration of action is not long, as it is typically given in 3 divided doses daily. Patients should be counselled regarding the risk of anaphylaxis, thrombocytopenia, hepatic dysfunction, and hyperkalemia.
Trade Name | Camostat |
Generic | Camostat |
Camostat Other Names | Camostat, Camostatum |
Type | |
Formula | C20H22N4O5 |
Weight | Average: 398.4125 Monoisotopic: 398.159019834 |
Protein binding | Camostat mesylate is 25.8-28.2% protein bound to human serum proteins in vitro. |
Groups | Experimental |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Camostat is a serine protease indicated in Japan to treat chronic pancreatitis.
Camostat mesylate is indicated in Japan to treat chronic pancreatitis and drug induced lung injury. It is also being investigated as a potential treatment for COVID-19.
How Camostat works
In rats, oral camostat mesylate may increase pancreatic secretions and hypertrophy by increasing cholecystokinin release. Administration in rats has also lead to lower levels of IL-1beta, IL-6, TNF-alpha, TGF-beta, and PSC. Similar activity is seem after administration in humans, leading to reduced pain and inflammation as well as improve the function of the pancrease in chronic pancreatitis.
In the case of SARS-CoV-2, camostat mesylate inhibits the action of the serine protease TMPRSS2, preventing the priming of the viral spike protein for attachment to ACE2, and entry into the cell.
Toxicity
Data regarding overdoses of camostat mesylate are not readily available, however common adverse effects include rash, pruritus, nausea, abnormal laboratory test values, and diarrhea.
Food Interaction
- Take with food. Take after a meal.
Volume of Distribution
The volume of distribution at steady state of camostat mesylate is 0.34-1.31L/kg.
Elimination Route
A 200mg oral dose of camostat mesylate leads to the active metabolite reaching a Cmax of 87.1 ± 29.5 ng/mL, with a Tmax of 40 min, and an AUC of 10,400 ± 1,400 ng*min/mL.
Half Life
The half life of camostat mesylate is 3.8-4.7h.
Clearance
The clearance of camostat mesylate is 4.5-7.3mL/min/kg.
Elimination Route
Camostat mesylate is 89.8-95.6% eliminated in the urine and 1.0-1.7% eliminated in the feces.
Innovators Monograph
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