YM-60828, a novel factor Xa inhibitor: separation of its antithrombotic effects from its prolongation of bleeding time

Eur J Pharmacol. 1997 Nov 27;339(2-3):141-6. doi: 10.1016/s0014-2999(97)01389-7.

Abstract

The antithrombotic effects of intravenous infusions of YM-60828 ([N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]-N-[(7-amidino-2-nap hthyl)methyl]sulfamoyl]acetic acid dihydrochloride), a novel factor Xa inhibitor, argatroban, heparin and dalteparin in an arterio-venous shunt model were studied in comparison with their effects on template bleeding time. In an arterio-venous shunt model, all agents exerted antithrombotic effects in a dose-dependent manner. ID50 values of YM-60828, argatroban, heparin and dalteparin were 0.0087 mg/kg/h. 0.027 mg/kg/h, 22 IU/kg/h and 11 IU/kg/h, respectively. In bleeding time studies, all agents prolonged bleeding time in a dose-dependent manner. Doses (ED2) of YM-60828, argatroban, heparin and dalteparin, which caused 2-fold prolongation of bleeding time in the saline group, were 3.0 mg/kg/h, 0.25 mg/kg/h, 18 IU/kg/h and 26 IU/kg/h. respectively. The risk-benefit ratio (ED2/ID50) of YM-60828 was much greater than that of the other agents. These data suggest that the antithrombotic effect of YM-60828 is separate from its prolongation of bleeding time and that YM-60828 is much safer than conventional anticoagulant agents.

MeSH terms

  • Animals
  • Anticoagulants / pharmacology
  • Antithrombins / pharmacology
  • Arginine / analogs & derivatives
  • Bleeding Time
  • Dalteparin / pharmacology
  • Factor Xa Inhibitors*
  • Fibrinolytic Agents / pharmacology
  • Heparin / pharmacology
  • Male
  • Naphthalenes / pharmacology*
  • Pipecolic Acids / pharmacology
  • Piperidines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Sulfonamides

Substances

  • Anticoagulants
  • Antithrombins
  • Factor Xa Inhibitors
  • Fibrinolytic Agents
  • Naphthalenes
  • Pipecolic Acids
  • Piperidines
  • Sulfonamides
  • YM 60828
  • Heparin
  • Arginine
  • argatroban
  • Dalteparin