[Pharmacokinetics studies of nafamostat mesilate (FUT), a synthetic protease inhibitor, which has been used for the treatments of DIC and acute pancreatitis, and as an anticoagulant in extracorporeal circulation].
Nafamostat mesilate (FUT) was first reported by Fujii et al, in 1981 as a synthetic protease inhibitor. FUT has been reported as a drug for the treatments of DIC (disseminated intravascular coagulation) and acute pancreatitis and as an anticoagulant in extracorporeal circulation. FUT has a structure of ester conjugate of p-guanidinobenzoic acid and 6-amidino-2-naphthol. In in vivo, this ester site was found as the reaction center as well as the site for the catabolic changes. Plasma half life (t1/2 beta) of FUT was about 23.1 min, compared to about 55 seconds of the related compound, FOY. The inhibitory activity of FUT on the protease was found to be due to the mis-reading of serine protease in vivo.
Tsukagoshi
S
S
Cancer Institute, Japanese Foundation for Cancer Research.
D000208:Acute Disease; D000328:Adult; D000925:Anticoagulants; D001550:Benzamidines; D004211:Disseminated Intravascular Coagulation / Q000188:drug therapy; D005112:Extracorporeal Circulation; D006146:Guanidines / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D008099:Liver / Q000378:metabolism; D008297:Male; D010195:Pancreatitis / Q000188:drug therapy; D011480:Protease Inhibitors / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology
D000925:Anticoagulants; D001550:Benzamidines; D006146:Guanidines; D011480:Protease Inhibitors; C032855:nafamostat