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Chemical Compound Review

FUT 175     [[6-[4-[(amino-azaniumyl...

Synonyms: LS-35885, AC1L1I2F, AC1Q22LB, 82956-11-4, UNII-1D2T74921W, ...
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Disease relevance of Nafamostat

  • A synthetic serine protease inhibitor, nafamostat mesilate (NM), which is commonly used for the treatment of pancreatitis and disseminated intravascular coagulation in Japan, also inhibited the secretion of prostasin in M-1 cells [1].
  • Potassium secretion in the CCD is tightly linked to sodium reabsorption through EnaC; therefore, NM-induced decrease in prostasin secretion and subsequent inhibition of ENaC activity could account for the side effects of hyponatremia and/or hyperkalemia that are found sometimes in patients treated with NM [1].
  • FUT-175 dose-dependently inhibited the classical pathway of complement in a hemolysis protection assay of sensitized sheep erythrocytes with guinea pig serum or by cell-lysis assay of mouse fibroblasts with human serum [2].
  • Thus, the co-administration of FUT-175 with retroviruses may make retrovirus-mediated in vivo gene transfer feasible for the treatment of patients [2].
  • Protective effects of FUT-175 on acute massive hepatic necrosis induced in mice following endotoxin injection and immunization with liver proteins [3].

High impact information on Nafamostat


Chemical compound and disease context of Nafamostat


Biological context of Nafamostat


Anatomical context of Nafamostat

  • We examined the effect of the synthetic serine protease inhibitor FUT-175 (developed as a potent inhibitor of thrombin and the complement system) on vascular lesions using balloon dilatation-induced neointimal formation in the carotid artery of rats [6].
  • The enzymatic activity of human cytotoxic T-lymphocyte granzyme A and cytolysis mediated by cytotoxic T-lymphocytes are potently inhibited by a synthetic antiprotease, FUT-175 [16].
  • METHODS AND RESULTS: In the clinical study, 20 patients who underwent coronary artery bypass grafting were divided into 2 groups: group F, in which patients were treated with a serine protease inhibitor (FUT-175, 2 mg/kg per hour) during cardiopulmonary bypass, and group C (untreated patients) [17].
  • Both heating of the serum and adding NM to the medium decreased damage of porcine hepatocytes [18].
  • Intravenous administration of FUT-175 at a dose of 3 or 10 mg/kg inhibited intravascular hemolysis of mouse erythrocytes regardless of whether it was administered before or after injection of human serum [15].

Associations of Nafamostat with other chemical compounds


Gene context of Nafamostat

  • FUT-175 inhibits the production of IL-6 and IL-8 in human monocytes [22].
  • These data suggest that FUT-175 may reduce the pathological inflammatory conditions associated with enhanced production of proinflammatory cytokines including IL-6 and IL-8 [22].
  • FUT-175 was found to inhibit, in an intense, specific and reversible way, the enzyme activities of trypsin, C1r, C1s, thrombin, kallikrein and plasmin with IC50 values of the order of 10(-6)-10(-8) M [23].
  • FUT-175 also inhibited complement-mediated hemolysis, including both classical and alternative pathways, sites of inhibition being on C1r and C1s as evidenced by the intermediate-cell technique [23].
  • Serum HGF levels on day 0 and day 7 were significantly higher in Group NM than those in Group C [24].

Analytical, diagnostic and therapeutic context of Nafamostat

  • Blood concentrations of FUT-175 and activated clotting time increased after cooling, peaking at 2050 +/- 1190 ng/mL and 2136 +/- 983 seconds at the lowest temperature and recovered after rewarming to values of 166 +/- 118 ng/mL and 510 +/- 148 seconds, respectively, at the end of CPB [4].
  • Three groups of these rats (n=8, each) were treated with daily intraperitoneal injections of 1 of the following doses of FUT-175: 0.5, 1.0, or 2.0 mg/d in 1 mL of saline for 7 consecutive days [6].
  • The incidence of a delayed ischemic neurological deficit significantly decreased from 55% in the control group to 13% in all patients treated with FUT-175 and to 7% in the patients treated with higher doses (P less than 0.05) [25].
  • NM thus appears to be a useful and safe anti-coagulant not only for hemodialysis but also for MP in high bleeding risk patients [26].
  • Nafamostat mesilate (FUT-175) is a strong protease inhibitor and is used as an anticoagulant in extracorporeal circulation [27].


  1. Inhibition of prostasin secretion by serine protease inhibitors in the kidney. Iwashita, K., Kitamura, K., Narikiyo, T., Adachi, M., Shiraishi, N., Miyoshi, T., Nagano, J., Tuyen, d.o. .G., Nonoguchi, H., Tomita, K. J. Am. Soc. Nephrol. (2003) [Pubmed]
  2. FUT-175, a synthetic inhibitor of the complement pathway, protects against the inactivation of infectious retroviruses by human serum. Miyao, Y., Ikenaka, K., Kishima, H., Tamura, M., Nakamura, K., Kurumi, M., Hayakawa, T., Shimizu, K. Hum. Gene Ther. (1997) [Pubmed]
  3. Protective effects of FUT-175 on acute massive hepatic necrosis induced in mice following endotoxin injection and immunization with liver proteins. Ogawa, M., Mori, Y., Ueda, S., Mori, T., Makino, Y., Hori, J., Ohto, M., Wakashin, M. J. Hepatol. (1993) [Pubmed]
  4. Nafamostat mesilate reduces blood loss during open heart surgery. Murase, M., Usui, A., Tomita, Y., Maeda, M., Koyama, T., Abe, T. Circulation (1993) [Pubmed]
  5. Effects of complement activation in the isolated heart. Role of the terminal complement components. Homeister, J.W., Satoh, P., Lucchesi, B.R. Circ. Res. (1992) [Pubmed]
  6. Prevention of neointimal formation by a serine protease inhibitor, FUT-175, after carotid balloon injury in rats. Sawada, M., Yanamoto, H., Nagata, I., Hashimoto, N., Nakahara, I., Akiyama, Y., Kikuchi, H., Macdonald, R.L. Stroke (1999) [Pubmed]
  7. Nafamstat mesilate attenuates pulmonary hypertension in heparin-protamine reactions. Kreil, E., Montalescot, G., Greene, E., Fitzgibbon, C., Robinson, D., Chenoweth, D., Zapol, W.M. J. Appl. Physiol. (1989) [Pubmed]
  8. Preventive effect of synthetic serine protease inhibitor, FUT-175, on cerebral vasospasm in rabbits. Yanamoto, H., Kikuchi, H., Okamoto, S., Nozaki, K. Neurosurgery (1992) [Pubmed]
  9. Platelet involvement in the nephritis of acute serum sickness in rabbits: protection by dipyridamole and FUT-175. Koyama, A., Inage, H., Sano, M., Narita, M., Tojo, S., Neild, G.H., Cameron, J.S. Clin. Exp. Immunol. (1985) [Pubmed]
  10. Blood platelet function in canine acute pancreatitis with reference to treatment with Nafamostat mesilate (FUT-175). Lukaszyk, A., Bodzenta-Lukaszyk, A., Gabryelewicz, A., Bielawiec, M. Thromb. Res. (1992) [Pubmed]
  11. Pharmacological studies of FUT-175, nafamostat mesilate. V. Effects on the pancreatic enzymes and experimental acute pancreatitis in rats. Iwaki, M., Ino, Y., Motoyoshi, A., Ozeki, M., Sato, T., Kurumi, M., Aoyama, T. Jpn. J. Pharmacol. (1986) [Pubmed]
  12. The influence of a serine protease inhibitor, nafamostat mesilate, on plasma coagulation, and platelet activation during experimental Extracorporeal Life Support (ECLS). Mellgren, K., Skogby, M., Friberg, L.G., Tengborn, L., Wadenvik, H. Thromb. Haemost. (1998) [Pubmed]
  13. Nafamostat mesilate reduces blood-foreign surface reactions similar to biocompatible materials. Usui, A., Hiroura, M., Kawamura, M., Hibi, M., Yoshida, K., Murakami, F., Tomita, Y., Ooshima, H., Murase, M. Ann. Thorac. Surg. (1996) [Pubmed]
  14. Studies on the effects of primary therapy for DIC following circulatory arrest. Takemoto, Y., Tanaka, S., Tanabe, J., Nakamura, Y., Kohama, A., Shibata, S. Am. J. Hematol. (1986) [Pubmed]
  15. Inhibitory effects of FUT-175, a new synthetic protease inhibitor, on intravascular hemolysis by human serum in mice. Ino, Y., Sato, T., Suzuki, S., Iwaki, M., Yoshikawa, T. Int. J. Immunopharmacol. (1987) [Pubmed]
  16. The enzymatic activity of human cytotoxic T-lymphocyte granzyme A and cytolysis mediated by cytotoxic T-lymphocytes are potently inhibited by a synthetic antiprotease, FUT-175. Poe, M., Wu, J.K., Blake, J.T., Zweerink, H.J., Sigal, N.H. Arch. Biochem. Biophys. (1991) [Pubmed]
  17. Interleukin-6 derived from hypoxic myocytes promotes neutrophil-mediated reperfusion injury in myocardium. Sawa, Y., Ichikawa, H., Kagisaki, K., Ohata, T., Matsuda, H. J. Thorac. Cardiovasc. Surg. (1998) [Pubmed]
  18. Modulation of immunologic reactions between cultured porcine hepatocytes and human sera. Hasegawa, H., Shimada, M., Gion, T., Ijima, H., Nakazawa, K., Funatsu, K., Sugimachi, K. ASAIO journal (American Society for Artificial Internal Organs : 1992) (1999) [Pubmed]
  19. Trypsin-like protease of mites: purification and characterization of trypsin-like protease from mite faecal extract Dermatophagoides farinae. Relationship between trypsin-like protease and Der f III. Ando, T., Homma, R., Ino, Y., Ito, G., Miyahara, A., Yanagihara, T., Kimura, H., Ikeda, S., Yamakawa, H., Iwaki, M. Clin. Exp. Allergy (1993) [Pubmed]
  20. CCK independently activates intracellular trypsinogen and NF-kappaB in rat pancreatic acinar cells. Han, B., Ji, B., Logsdon, C.D. Am. J. Physiol., Cell Physiol. (2001) [Pubmed]
  21. Human complement-activating immunoglobulin (Ig)G3 antibodies are essential for porcine endothelial cell activation. Saethre, M., Lea, T., Borgen, M.S., Fiane, A.E., Michaelsen, T.E., Thorsby, E., Haraldsen, G., Mollnes, T.E. Xenotransplantation (2006) [Pubmed]
  22. FUT-175 inhibits the production of IL-6 and IL-8 in human monocytes. Sugita, H., Ishiko, T., Ikei, S., Hirota, M., Ogawa, M. Res. Commun. Mol. Pathol. Pharmacol. (1999) [Pubmed]
  23. Pharmacological studies of FUT-175, nafamstat mesilate. I. Inhibition of protease activity in in vitro and in vivo experiments. Aoyama, T., Ino, Y., Ozeki, M., Oda, M., Sato, T., Koshiyama, Y., Suzuki, S., Fujita, M. Jpn. J. Pharmacol. (1984) [Pubmed]
  24. The role of a protease inhibitor against hepatectomy. Gotohda, N., Iwagaki, H., Ozaki, M., Konishi, M., Nakagohri, T., Takahashi, S., Yagi, T., Kinoshita, T., Tanaka, N. Hepatogastroenterology (2006) [Pubmed]
  25. Therapeutic trial of cerebral vasospasm with the serine protease inhibitor, FUT-175, administered in the acute stage after subarachnoid hemorrhage. Yanamoto, H., Kikuchi, H., Sato, M., Shimizu, Y., Yoneda, S., Okamoto, S. Neurosurgery (1992) [Pubmed]
  26. Nafamostat as anti-coagulant for membrane plasmapheresis in high bleeding risk patients. Kinugasa, E., Akizawa, T., Nakashima, Y., Wakasa, M., Koshikawa, S. The International journal of artificial organs. (1992) [Pubmed]
  27. Plasma collection using nafamostat mesilate and dipyridamole as an anticoagulant. Hiraishi, M., Yamazaki, Z., Ichikawa, K., Kanai, F., Idezuki, Y., Onishi, K., Takahama, T., Inoue, N. The International journal of artificial organs. (1988) [Pubmed]
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