In Phase I Clinical Evaluation Anticoagulant Inhibits Clotting Factor IXa;
Matched Antidote Rapidly Reverses Anticoagulant Effect
ORLANDO, Fla., Nov. 6 /PRNewswire/ -- Regado Biosciences today presented encouraging data from Phase Ia and Phase Ib dose escalation studies of the Company's REG1 Anticoagulation System. REG1 is a two-component system consisting of an aptamer-based anticoagulant, RB006, and its matched antidote, RB007, which binds to and neutralizes RB006. The data showed RB006 completely inhibited the activity of Factor IXa, a protein essential to blood clotting, and RB006's activity was rapidly and safely reversed by RB007 in the Phase I studies. Confirming previously reported Phase I results, these data were presented at the American Heart Association's 2007 Scientific Sessions, currently being held in Orlando, Florida.
"These Phase I results are encouraging, and this system should be evaluated further in confirmatory Phase II and III clinical studies. Experienced clinicians recognize the importance of being able to titrate the intensity of anticoagulation according to specific patient needs. Current drugs do not offer an optimal level of control or flexibility," said Richard C. Becker, M.D., Professor of Medicine, Duke University Medical Center, and Director, Duke Cardiovascular Thrombosis Center, Duke Clinical Research Institute. "Should additional well-controlled clinical studies confirm these data, REG1 may have potential for broad applications in clinical practice settings from the emergency room to the operating room."
Scientists from the Duke Clinical Research Institute and Regado analyzed REG1 pharmacokinetics and dosing data from 134 subjects enrolled in two of the three Phase I studies. The Phase Ia study enrolled 84 healthy volunteers; the Phase Ib study enrolled 50 patients with stable coronary artery disease who were receiving aspirin with or without clopidogrel. The results of the analysis showed an intravenous (IV) bolus injection of RB006 achieved in both study populations a prompt, consistent, and dose-dependent prolongation of activated partial thromboplastin time (aPTT), a well-accepted surrogate marker of the blood's ability to clot. In addition, a 1 mg/kg dose of RB006 resulted in 100 percent Factor IXa inhibition. The studies also demonstrated an IV bolus injection of RB007 administered in a 2:1 antidote:drug ratio successfully reversed prolonged aPTT within a median of one minute, with no rebound increase up to seven days. Despite dual antiplatelet use in 19 subjects, there were no major bleeding or other serious adverse events observed in either study.
"Our Phase I studies consistently have confirmed the two major attributes of the REG1 system, the ability to rapidly anticoagulate and then reverse this effect," stated Doug Gooding, Chief Executive Officer of Regado Biosciences. "We are confident later-stage clinical testing will further confirm our belief REG1 has the potential to be a first-in-class antidote-reversible therapeutic system, which could transform the way anticoagulation is approached in coronary revascularization procedures and other acute care settings."
REVERSAL-PCI, a multi-center, open-label, randomized Phase IIa clinical study of the REG1 anticoagulation system, is enrolling 26 patients undergoing elective percutaneous coronary intervention (PCI) to assess whether REG1 can replace standard heparin therapy during the performance of coronary balloon angioplasty dilatation and stenting in patients at low risk for complications associated with therapy-related bleeding or heart attack.
About REG1 Anticoagulation System
Regado's lead product candidate, REG1, is the first specific, direct-acting, antidote-controlled anticoagulant ever described. Regado is developing REG1 for use in patients suffering from acute coronary syndrome who undergo coronary revascularization procedures. These procedures, which include coronary artery bypass grafting (CABG) and percutaneous coronary intervention (PCI), put patients at a high-risk for therapy-related bleeding complications. REG1 is being developed initially to increase therapeutic flexibility and improve patient outcomes in coronary revascularization procedures.
REG1 is a two-component system, consisting of an aptamer-based anticoagulant and its matched antidote. The REG1 anticoagulant component (RB006) is a single-stranded, nucleic acid aptamer. RB006 selectively and potently binds to and inhibits Factor IXa, a protein that is critical to blood coagulation. The antidote component, RB007, is a complementary nucleic acid that binds to and neutralizes RB006. The binding of RB007 to RB006 causes the predictable and rapid reversal of RB006 that allows the patient's blood to return to normal.
About Regado Biosciences
Regado Biosciences is pioneering a new therapeutic field with the discovery and development of drug:antidote systems. Regado's drug:antidote systems are designed to give physicians the ability to fine-tune the therapeutic effect desired for each patient and in each setting. A spin-out of the Department of Surgery at Duke University Medical Center, Regado was created to answer the therapeutic needs identified by its scientific founders.
The Company's proprietary platform technology enables the discovery of oligonucleotide-based drug-antidote pairs to any target protein. Regado initially is focusing its discovery and development efforts on acute care injectable antithrombotics, a multi-billion dollar market in need of therapeutics with improved safety profiles. Potential future indications for Regado's technology include acute coronary syndromes and other coronary revascularization procedures that would benefit from the availability of an antidote-reversible agent.
|SOURCE Regado Biosciences|
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