The REG1 anticoagulation system: a novel actively controlled factor IX inhibitor using RNA aptamer technology for treatment of acute coronary syndrome

Abstract

Antithrombotic agents including anticoagulants and antiplatelets are the cornerstone of treatment of acute coronary syndromes. Currently available anticoagulants have several important limitations including unpredictable pharmacodynamics, immunogenicity, and difficulty in reversibility. A potent anticoagulant that has predictable efficacy, is easily reversible should the clinical need arise, and reduces ischemic events without an increase in bleeding risk would overcome many of the current limitations. Inhibition of factor IX in the coagulation cascade has shown promise as a target for development of a novel anticoagulant with a favorable bleeding risk. Aptamers are small oligonucleotides that can be developed to inhibit specific protein targets with high affinity and used as active drugs. Because aptamers are made of oligonucleotide sequences, they provide the code for their own complement (reversal agent) that can be developed and used to inhibit their function. The REG1 anticoagulation system is a novel, aptamer-based, factor IXa inhibitor that is being developed for use in patients undergoing percutaneous coronary intervention and the treatment of acute coronary syndrome.