REG-1, a regimen comprising RB-006, a Factor IXa antagonist, and its oligonucleotide active control agent RB-007 for the potential treatment of arterial thrombosis.

Abstract

REG-1, under development by Regado Biosciences Inc, is an intravenously administered anticoagulant system comprising the Factor IXa-inhibiting aptamer RB-006 and its complementary active control oligonucleotide, RB-007, for the potential treatment of arterial thrombosis. The evolution of anticoagulant therapy for the prevention and acute treatment of thrombotic disorders has progressed at a relatively modest pace considering the scope of the problem and the current understanding of platelet biology, coagulation proteases and vascular science, and their role in protective hemostasis and pathological thrombosis. This drug profile highlights a novel field of anticoagulant therapy referred to as aptamers (derived from the Latin aptus - to fit) and, in particular, the aptamer/active control agent system REG-1, which demonstrated efficacy as an anticoagulant in preclinical studies. In phase I clinical trials in healthy volunteers and patients with stable coronary artery disease, RB-006 inhibited Factor IXa activity, an effect that was titratibly reversible by the application of RB-007. In a phase IIa trial, REG-1 was well tolerated in patients undergoing elective percutaneous coronary intervention, and the treatment was successful with no procedural complications. At the time of publication, an extensive phase IIb trial in patients with acute coronary syndrome undergoing cardiac catheterization was ongoing.