Regado Biosciences’ has an extensive pipeline of antithrombotic agents for the treatment of cardiovascular disease consisting of therapeutic aptamers and their active control agent partners.

REG1: Regado’s lead candidate, the REG1 Anticoagulation System, is a two-component system comprising a Factor IXa inhibitor anticoagulant and its specific active control agent.  REG1 is being developed for use in patients suffering from acute coronary syndrome (ACS), including those who undergo coronary revascularization procedures, which include percutaneous coronary intervention (PCI) and coronary artery bypass grafting (CABG).  These procedures put patients at risk for therapy-related bleeding complications.  REG1 is designed to increase therapeutic flexibility while reducing side effects and improving outcomes experienced by patients in this setting.

REG2: Regado has initiated a Phase 1 trial using a subcutaneous formulation of pegnivacogin (aka RB006) paired with an IV bolus formulation of
anivamersen (aka RB007) for eventual application in venous thrombosis indications.  Subcutaneous administration of RB006 is anticipated to provide a therapeutic profile complementary to the IV formulation, with a slow onset of activity and duration of effect of several days, ideally suited to venous prophylactic indications, while still maintaining the benefit of active control by IV RB007 administration.

REG3: Regado’s lead anti-platelet candidate, REG3, consists of a specific GPVI inhibitor and its active control agent (RB571 and RB515, respectively).  GPVI, the platelet-specific major collagen receptor, has been implicated in a wide range of platelet-mediated diseases including ACS, rheumatoid arthritis and diabetic vasculopathy.  REG3 is planned to enter phase 1 human clinical testing in 2013.

Anti-platelet program:  Regado  is conducting discovery efforts to identify an aptamer:control agent pair for clinical applications in the area of antiplatelet therapy.  Current programs are focused on validated platelet receptor targets involved in platelet adhesion and activation.  Such receptors typically represent challenging targets for the discovery of small molecule inhibitors, but are ideally suited to the development of aptamer inhibitors designed to block the protein-protein interactions which occur between these receptors and their ligands.  Such a drug, in combination with a specific active control agent would provide unprecedented control of antiplatelet therapy to physicians.