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Tolerability, pharmacokinetics, and pharmacodynamics of DX‐9065a, a new synthetic potent anticoagulant and specific factor Xa inhibitor, in healthy male volunteers
Author(s) -
Murayama Nobuyuki,
Tanaka Makoto,
Kunitada Satoshi,
Yamada Hirohisa,
Inoue Takashi,
Terada Yasuko,
Fujita Masami,
Ikeda Yasuo
Publication year - 1999
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/s0009-9236(99)70033-0
Subject(s) - pharmacokinetics , pharmacodynamics , pharmacology , tolerability , anticoagulant , chemistry , dosing , oral administration , medicine , adverse effect
Objective The aim of this study was to assess the tolerability, pharmacokinetic and pharmacodynamic properties of DX‐9065a, a novel low‐molecule specific factor Xa inhibitor in healthy male volunteers. Methods DX‐9065a was intravenously administered to healthy male Japanese volunteers at doses of 0.625 to 30 mg. The drug concentrations in plasma and urine were measured and pharmacokinetic parameters were calculated. Coagulation time and bleeding time were also measured. Results No serious adverse event was observed during or after administration of DX‐9065a. The pharmacokinetics of DX‐9065a in human subjects after intravenous dosing was linear. The simulated plasma concentrations of DX‐9065 were well in accordance with the observed values. Though prolongation of coagulation times was dependent on plasma concentration of DX‐9065, bleeding time did not increase even at the highest plasma concentration of 1640 ng/mL. Conclusions DX‐9065a had a good correlation between linear pharmacokinetics and pharmacodynamics after intravenous administration in humans. Clinical Pharmacology & Therapeutics (1999) 66 , 258–264; doi: