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Pharmacokinetics and pharmacodynamics of the dual FII/FX inhibitor BIBT 986 in endotoxin-induced coagulation

Introduction

BIBT 986 is a dual inhibitor of factors Xa and IIa. The aim of this study was to compare with placebo the effect of three doses of BIBT 986 on coagulation, platelet activation and inflammation.

Methods

This was a prospective, randomized, double-blind, placebo-controlled, parallel-group dose escalation trial in 48 healthy male volunteers. Participants received one of three doses of BIBT 986 or placebo intravenously together with a bolus infusion of 2 ng/kg lipopolysaccharide (LPS).

Results

BIBT 986 dose-dependently changed global coagulation parameters and in vivo markers of thrombin generation and action: BIBT 986 doses, which prolonged activated partial thromboplastin time by 100%, completely suppressed the LPS-induced increases in prothrombin fragment, thrombin-antithrombin complexes and D-dimer, which were 6.1, 14.5, and 3.5-fold in the placebo group, respectively. BIBT 986 did not influence inflammation, fibrinolysis, or platelet activation.

Conclusion

BIBT 986 is a potent anticoagulant in the human endotoxemia model.

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Correspondence to Bernd Jilma.

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Open Access This article is published under license to BioMed Central Ltd. This is an Open Access article is distributed under the terms of the Creative Commons Attribution License ( https://creativecommons.org/licenses/by/2.0 ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Leitner, J.M., Jilma, B., Mayr, F.B. et al. Pharmacokinetics and pharmacodynamics of the dual FII/FX inhibitor BIBT 986 in endotoxin-induced coagulation. BMC Pharmacol 7, A29 (2007). https://doi.org/10.1186/1471-2210-7-S2-A29

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  • DOI: https://doi.org/10.1186/1471-2210-7-S2-A29

Keywords

  • Placebo
  • Thrombin
  • Prothrombin
  • Platelet Activation
  • Partial Thromboplastin Time