Evaluation of the profibrinolytic properties of an anti-TAFI monoclonal antibody in a mouse thromboembolism model

Blood. 2011 Apr 28;117(17):4615-22. doi: 10.1182/blood-2010-08-303677. Epub 2011 Feb 22.

Abstract

The enhancement of fibrinolysis constitutes a promising approach to treat thrombotic diseases. Activated thrombin activatable fibrinolysis inhibitor (TAFIa) attenuates fibrinolysis and is an attractive target to develop profibrinolytic drugs. TAFI can be activated by thrombin, thrombin/thrombomodulin, or plasmin, but the in vivo physiologic TAFI activator(s) are unknown. Here, we generated and characterized MA-TCK26D6, a monoclonal antibody raised against human TAFI, and examined its profibrinolytic properties in vitro and in vivo. In vitro, MA-TCK26D6 showed a strong profibrinolytic effect caused by inhibition of the plasmin-mediated TAFI activation. In vivo, MA-TCK26D6 significantly decreased fibrin deposition in the lungs of thromboembolism-induced mice. Moreover, in the presence of MA-TCK26D6, plasmin-α(2)-antiplasmin complexes in plasma of thromboembolism-induced mice were significantly increased compared with a control antibody, indicative of an acceleration of fibrinolysis through MA-TCK26D6. In this study, we show that plasmin is an important TAFI activator that hampers in vitro clot lysis. Furthermore, this is the first report on an anti-TAFI monoclonal antibody that demonstrates a strong profibrinolytic effect in a mouse thromboembolism model.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / immunology*
  • Antibodies, Monoclonal / pharmacology*
  • Antibody Affinity / immunology
  • Antithrombin III / immunology
  • Carboxypeptidase B2 / immunology*
  • Carboxypeptidase B2 / metabolism
  • Cross Reactions / immunology
  • Disease Models, Animal
  • Fibrinolysis / immunology*
  • Humans
  • In Vitro Techniques
  • Lung / blood supply
  • Lung / immunology
  • Mice
  • Mice, Mutant Strains
  • Peptide Hydrolases / immunology
  • Species Specificity
  • Thromboembolism / immunology
  • Thromboembolism / metabolism
  • Thromboembolism / therapy*

Substances

  • Antibodies, Monoclonal
  • antithrombin III-protease complex
  • Antithrombin III
  • Peptide Hydrolases
  • Carboxypeptidase B2