We designed this study in sows to investigate the enzyme inhibitory action of gabexate mesylate (GM) directly in the pancreatic juice. We studied 16 sows, each weighing about 130 kg. The pancreatic duct was identified and cannulated to collect the pancreatic juice. Sows in the treated group received intravenous GM infusion at a dose of 1000 mg over 24 h. Control sows underwent the same sampling schedule while receiving physiological solution. GM inhibited the two pancreatic enzymes amylase and phospholipase A(2) (PA(2)) in pancreatic juice. Thus, the enzyme inhibition in the pancreatic gland itself and the central role of (PA(2)) inhibition in enzyme cascade responsible for activating other proteases confirm the therapeutic use of GM in acute pancreatitis.