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.