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Related Experiment Videos

SR123781A, a synthetic heparin mimetic.

J M Herbert1, J P Hérault, A Bernat

  • 1Cardiovascular/Thrombosis Research Department, Sanofi-Synthélabo, Toulouse, France. jean-marc.herbert@sanofi-synthelabo.com

Thrombosis and Haemostasis
|May 25, 2001
PubMed
Summary

SR123781A, a synthetic hexadecasaccharide, effectively inhibits thrombin and factor Xa by potentiating antithrombin. This compound demonstrates a favorable antithrombotic/bleeding ratio, suggesting its potential for treating thrombotic diseases.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Antithrombotic agents are crucial for managing thrombotic diseases.
  • Heparin and its derivatives are widely used but can have limitations.
  • Novel anticoagulants with improved safety profiles are needed.

Purpose of the Study:

  • To synthesize and characterize SR123781A, a novel synthetic hexadecasaccharide.
  • To evaluate the antithrombotic efficacy and safety profile of SR123781A in preclinical models.

Main Methods:

  • Convergent synthesis of SR123781A from glucose.
  • In vitro assays to determine affinity for antithrombin (AT) and inhibition of factor Xa and thrombin.
  • Ex vivo and in vivo studies in animal models (rats, rabbits, baboons) to assess pharmacokinetic and pharmacodynamic properties, antithrombotic activity, and bleeding risk.

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Main Results:

  • SR123781A demonstrated high affinity for human AT and potent inhibition of factor Xa and thrombin.
  • The compound acted exclusively via AT, without affecting heparin cofactor II, and did not activate platelets.
  • In vivo studies showed prolonged anticoagulant activity and significant inhibition of both venous and arterial thrombosis with a favorable antithrombotic/bleeding ratio compared to heparin.

Conclusions:

  • SR123781A is a potent synthetic anticoagulant that functions via AT.
  • It exhibits a superior antithrombotic/bleeding profile compared to existing anticoagulants.
  • SR123781A represents a promising therapeutic candidate for the prevention and treatment of thrombotic disorders.