Patomostat mesilate

Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease

Research Areas >> Inflammation/Immunology

IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)[1]

Patamostat mesylate (intravenous infusion) at 0.03-0.3 mg/kg in rats or at 0.3-3.0 mg/kg in rabbits reduces mortality after the induction of pancreatitis in a dose-dependent manner[1]. Patamostat mesylate (1.0-3.0 mg/kg; intravenous infusion) reduces the increases of serum trypsin and lipase activities in dogs with pancreatitis[1]. Patamostat mesylate (2 mg/kg per h; continuous infusion) improves almost all parameters, including mortality rate, serum and ascitic fluid amylase levels, plasma endotoxin and serum FDP levels, and distribution of lysosomal enzyme in male Wistar rats[2]. Animal Model: Male Wistar rats weighing about 350 g[2] Dosage: 2 mg/kg Administration: Continuous infusion per h for 1 h Result: Significantly improved the survival rate.

[1]. K Miyamoto, et al. [Effects of E-3123, a New Protease Inhibitor, on Several Protease Activities and on Experimental Acute Pancreatitis]. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93.

[2]. T Hirano, et al. Protective Effect of a Cephalosporin, Shiomarin, Plus a New Potent Protease Inhibitor, E3123, on Rat Taurocholate-Induced Pancreatitis. J Gastroenterol Hepatol. Jan-Feb 1993;8(1):52-9.