Development of argatroban, a direct thrombin inhibitor, and its clinical application

Takefumi Matsuo, Masanobu Koide, Kazuomi Kario

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36 Scopus citations


Argatroban, a direct thrombin inhibitor, is used clinically because of its safe and effective antithrombotic action. This drug of low molecular weight shows reversible inhibition of thrombin irrespective of whether thrombin is fibrin-bound or soluble. Optimal anticoagulant effects can easily be attained by monitoring with the activated partial thromboplastin time or whole-blood activated clotting time when a therapeutic range of argatroban equivalent to that of heparin is used. The antithrombotic action is simply detected with a chromogenic substrate assay. The clinical use of the drug in Japan was approved for the treatment of chronic peripheral arterial obstructive disease and acute ischemic stroke. For coronary artery disease in patients with deficiency of antithrombin activities attributable to either antithrombin III or heparin cofactor II deficiency, argatroban is effective as an anticoagulant. Acute coronary occlusion during and after percutaneous transluminal coronary angioplasty can be treated by argatroban as an alternative to heparin. The presence of platelets activated by a trace amount of thrombin is evidenced by modified methods of platelet aggregometry in acute ischemic stroke. Therefore, argatroban can render the platelets insensitive against the platelet hyperaggregation enhanced by thrombin.

Original languageEnglish
Pages (from-to)517-522
Number of pages6
JournalSeminars in Thrombosis and Hemostasis
Issue number6
StatePublished - 1997
Externally publishedYes


  • Acute ischemic stroke
  • Argatroban
  • Cardiovascular disease
  • Monitoring
  • Thrombin inhibitor


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