Tolerability, pharmacokinetics, and pharmacodynamics of DX-9065a, a new synthetic potent anticoagulant and specific factor Xa inhibitor, in healthy male volunteers
| Autor: | Masami Fujita, Hirohisa Yamada, Takashi Inoue, Yasuko Terada, Satoshi Kunitada, Nobuyuki Murayama, Makoto Tanaka, Yasuo Ikeda |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Adult
Male Bleeding Time medicine.drug_mechanism_of_action medicine.drug_class Factor Xa Inhibitor Naphthalenes Pharmacology Asian People Double-Blind Method Japan Pharmacokinetics Reference Values Bleeding time medicine Humans Pharmacology (medical) Dosing Adverse effect Analysis of Variance medicine.diagnostic_test business.industry Anticoagulant Anticoagulants Tolerability Area Under Curve Pharmacodynamics Injections Intravenous Linear Models Propionates business Factor Xa Inhibitors |
| Zdroj: | Clinical Pharmacology & Therapeutics. 66:258-264 |
| ISSN: | 1532-6535 0009-9236 |
| DOI: | 10.1016/s0009-9236(99)70033-0 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text