Peringatan Keamanan

Data regarding overdoses of camostat mesylate are not readily available, however common adverse effects include rash, pruritus, nausea, abnormal laboratory test values, and diarrhea.L13197

Camostat

DB13729

small molecule experimental

Deskripsi

Camostat mesylate, or FOY-305, is a synthetic serine protease inhibitor.A193842,A193848 It was first described in the literature in 1981, as part of research on the inhibition of skin tumors in mice.A198807 Camostat mesylate inhibits cholecystokinin, pro-inflammatory cytokines, and serine proteases, leading to it being investigated for multiple indications including the treatment of COVID-19.A198771,A198777,A193800

Camostat mesylate was first approved in Japan in January 2006.L13197

Struktur Molekul 2D

Berat 398.4125
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of camostat mesylate is 3.8-4.7h.[A193842]
Volume Distribusi The volume of distribution at steady state of camostat mesylate is 0.34-1.31L/kg.[A193842]
Klirens (Clearance) The clearance of camostat mesylate is 4.5-7.3mL/min/kg.[A193842]

Absorpsi

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.L13197

Metabolisme

Camostat mesylate is hydrolyzed by carboxyesterate to the active 4-(4-guanidinobenzoyloxy) phenylacetate.A193842,L13197 The active metabolite is further hydrolyzed by arylesterase to 4-guanidinobenzoic acid.A193842,L13197

Rute Eliminasi

Camostat mesylate is 89.8-95.6% eliminated in the urine and 1.0-1.7% eliminated in the feces.A193842

Interaksi Makanan

1 Data
  • 1. Take with food. Take after a meal.

Interaksi Obat

56 Data
Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Camostat.
Menadione Menadione may increase the thrombogenic activities of Camostat.
Tranexamic acid Tranexamic acid may increase the thrombogenic activities of Camostat.
Aminocaproic acid Aminocaproic acid may increase the thrombogenic activities of Camostat.
Aprotinin Aprotinin may increase the thrombogenic activities of Camostat.
Hydrogen peroxide Hydrogen peroxide may increase the thrombogenic activities of Camostat.
Aminomethylbenzoic acid Aminomethylbenzoic acid may increase the thrombogenic activities of Camostat.
Menadione bisulfite Camostat may increase the thrombogenic activities of Menadione bisulfite.
Fibrinogen human The therapeutic efficacy of Fibrinogen human can be increased when used in combination with Camostat.
Tretinoin The risk or severity of Thrombosis can be increased when Camostat is combined with Tretinoin.
Antihemophilic factor, human recombinant Camostat may increase the thrombogenic activities of Antihemophilic factor, human recombinant.
Coagulation factor VIIa Recombinant Human Camostat may increase the thrombogenic activities of Coagulation factor VIIa Recombinant Human.
Coagulation Factor IX (Recombinant) Camostat may increase the thrombogenic activities of Coagulation Factor IX (Recombinant).
Calcium Camostat may increase the thrombogenic activities of Calcium.
Pantothenic acid Camostat may increase the thrombogenic activities of Pantothenic acid.
Formic acid Camostat may increase the thrombogenic activities of Formic acid.
Platelet Activating Factor Camostat may increase the thrombogenic activities of Platelet Activating Factor.
Turoctocog alfa Camostat may increase the thrombogenic activities of Turoctocog alfa.
Catridecacog Camostat may increase the thrombogenic activities of Catridecacog.
Antihemophilic factor (recombinant), PEGylated Camostat may increase the thrombogenic activities of Antihemophilic factor (recombinant), PEGylated.
Prothrombin Camostat may increase the thrombogenic activities of Prothrombin.
Factor IX Complex (Human) Camostat may increase the thrombogenic activities of Factor IX Complex (Human).
Susoctocog alfa Camostat may increase the thrombogenic activities of Susoctocog alfa.
Eftrenonacog alfa Camostat may increase the thrombogenic activities of Eftrenonacog alfa.
Rusalatide acetate Camostat may increase the thrombogenic activities of Rusalatide acetate.
Vatreptacog alfa Camostat may increase the thrombogenic activities of Vatreptacog alfa.
Factor XIII (human) Camostat may increase the thrombogenic activities of Factor XIII (human).
Von Willebrand factor human Camostat may increase the thrombogenic activities of Von Willebrand factor human.
Coagulation factor X human Camostat may increase the thrombogenic activities of Coagulation factor X human.
Coagulation factor VII human Camostat may increase the thrombogenic activities of Coagulation factor VII human.
Anti-inhibitor coagulant complex Camostat may increase the thrombogenic activities of Anti-inhibitor coagulant complex.
Coagulation Factor IX Human Camostat may increase the thrombogenic activities of Coagulation Factor IX Human.
Antihemophilic factor human Camostat may increase the thrombogenic activities of Antihemophilic factor human.
Kallidinogenase Camostat may increase the thrombogenic activities of Kallidinogenase.
Trenonacog alfa Camostat may increase the thrombogenic activities of Trenonacog alfa.
Albutrepenonacog alfa Camostat may increase the thrombogenic activities of Albutrepenonacog alfa.
Emicizumab Camostat may increase the thrombogenic activities of Emicizumab.
Nonacog beta pegol Camostat may increase the thrombogenic activities of Nonacog beta pegol.
Moroctocog alfa Camostat may increase the thrombogenic activities of Moroctocog alfa.
Beroctocog alfa Camostat may increase the thrombogenic activities of Beroctocog alfa.
Andexanet alfa Camostat may increase the thrombogenic activities of Andexanet alfa.
Calcium cation Camostat may increase the thrombogenic activities of Calcium cation.
Damoctocog alfa pegol Camostat may increase the thrombogenic activities of Damoctocog alfa pegol.
Turoctocog alfa pegol Camostat may increase the thrombogenic activities of Turoctocog alfa pegol.
Alteplase The therapeutic efficacy of Camostat can be decreased when used in combination with Alteplase.
Urokinase The therapeutic efficacy of Camostat can be decreased when used in combination with Urokinase.
Reteplase The therapeutic efficacy of Camostat can be decreased when used in combination with Reteplase.
Anistreplase The therapeutic efficacy of Camostat can be decreased when used in combination with Anistreplase.
Tenecteplase The therapeutic efficacy of Camostat can be decreased when used in combination with Tenecteplase.
Streptokinase The therapeutic efficacy of Camostat can be decreased when used in combination with Streptokinase.
Lanoteplase The therapeutic efficacy of Camostat can be decreased when used in combination with Lanoteplase.
Amediplase The therapeutic efficacy of Camostat can be decreased when used in combination with Amediplase.
Saruplase The therapeutic efficacy of Camostat can be decreased when used in combination with Saruplase.
Protein S human Camostat may increase the thrombogenic activities of Protein S human.
Rurioctocog alfa pegol Camostat may increase the thrombogenic activities of Rurioctocog alfa pegol.
Etranacogene dezaparvovec Camostat may increase the thrombogenic activities of Etranacogene dezaparvovec.

Target Protein

Serine protease 1 PRSS1
Transmembrane protease serine 2 TMPRSS2
Suppressor of tumorigenicity 14 protein ST14
Cholecystokinin CCK

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32142651
    Hoffmann M, Kleine-Weber H, Schroeder S, Kruger N, Herrler T, Erichsen S, Schiergens TS, Herrler G, Wu NH, Nitsche A, Muller MA, Drosten C, Pohlmann S: SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor. Cell. 2020 Apr 16;181(2):271-280.e8. doi: 10.1016/j.cell.2020.02.052. Epub 2020 Mar 5.
  • PMID: 8165824
    Midgley I, Hood AJ, Proctor P, Chasseaud LF, Irons SR, Cheng KN, Brindley CJ, Bonn R: Metabolic fate of 14C-camostat mesylate in man, rat and dog after intravenous administration. Xenobiotica. 1994 Jan;24(1):79-92. doi: 10.3109/00498259409043223.
  • PMID: 27408783
    Ota S, Hara Y, Kanoh S, Shinoda M, Kawano S, Fujikura Y, Kawana A, Shinkai M: Acute eosinophilic pneumonia caused by camostat mesilate: The first case report. Respir Med Case Rep. 2016 Jun 16;19:21-3. doi: 10.1016/j.rmcr.2016.06.005. eCollection 2016.
  • PMID: 22038264
    Kitamura K, Tomita K: Proteolytic activation of the epithelial sodium channel and therapeutic application of a serine protease inhibitor for the treatment of salt-sensitive hypertension. Clin Exp Nephrol. 2012 Feb;16(1):44-8. doi: 10.1007/s10157-011-0506-1. Epub 2011 Nov 1.
  • PMID: 143965
    Tamura Y, Hirado M, Okamura K, Minato Y, Fujii S: Synthetic inhibitors of trypsin, plasmin, kallikrein, thrombin, C1r-, and C1 esterase. Biochim Biophys Acta. 1977 Oct 13;484(2):417-22.
  • PMID: 3562444
    Goke B, Printz H, Koop I, Rausch U, Richter G, Arnold R, Adler G: Endogenous CCK release and pancreatic growth in rats after feeding a proteinase inhibitor (camostate). Pancreas. 1986;1(6):509-15. doi: 10.1097/00006676-198611000-00008.
  • PMID: 15877292
    Jia D, Taguchi M, Otsuki M: Synthetic protease inhibitor camostat prevents and reverses dyslipidemia, insulin secretory defects, and histological abnormalities of the pancreas in genetically obese and diabetic rats. Metabolism. 2005 May;54(5):619-27. doi: 10.1016/j.metabol.2004.12.005.
  • PMID: 7341342
    Ohkoshi M: Inhibition of growth of 3-methylcholanthrene-induced mouse skin tumor by protease inhibitor N,N-dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)-phenylacetate methanesulfate. Gan. 1981 Dec;72(6):959-64.

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