REG1 drug makes blood thinners safer by reversing bleeding, from Regado Biosciences

REG1, a new drug than can make the commonly used anti-blood clotting drugs safer by reversing its harmful side-effects has been developed by Regado Biosciences, Inc.

REG1 is an oligonucleotide modulators of blood coagulation factor aptamers.

Oligonucleotide modulators that hybridize under physiological conditions to a blood coagulation factor aptamer.

Oligonucleotide modulator REG1 specifically and rapidly reverses the anticoagulant and antithrombotic effects of the aptamer.

REG1, consists of two parenteral agents both administered by IV bolus, the first being a potent highly selective Factor IXa inhibitor (RB006) and the second being its complementary active control agent (RB007).  RB007 can be used to selectively completely or partially reverse the anticoagulant effect of RB006.

RB006 is a member of a class of compounds called aptamers.  Aptamers are single stranded oligonucleotides that adopt a specific conformation enabling direct, specific inhibition of the targeted protein.

Aptamers are formed from nucleic acids.  Aptamers’ pharmacologic activity can be controlled by a matched, complementary oligonucleotide active control agent (the Watson-Crick base pair complement of a fraction of the agent to be controlled), which can bind to the aptamer, removing it from its target and reversing it biologic effects.

Not many aptamer drugs are currently in market. Macugen, Pfizer’s drug for age-related macular degeneration, is the only aptamer drug approved for sale by the U.S. Food and Drug Administration, so far.

REG1 is intended for application in arterial thrombosis applications, initially in acute coronary syndrome patients undergoing percutaneous coronary intervention.

REG2, Regado’s second product candidate, consists of a subcutaneously administered formulation of RB006 paired with the IV bolus formulation of RB007.  REG2 is intended for use in venous thrombosis indications

Patients suffering from such conditions need to take blood thinners to prevent blood clots during surgery. But bleeding can occur as a common side effect while using blood thinner drugs.

REG compounds can be an effective antidote on hand would surgical treatments using blood thinners safer, researchers said.

REG compounds will be granted a patent soon, the European Patent Office (EPO) has informed the Regado Biosciences.

Regado also has certain U.S. patent applications and issued patents covering aspects of the REG1 system, including patents covering certain RNA aptamers to coagulation factors (e.g. US7,312,325) and aptamer modulation (e.g. US7,300,922) exclusively licensed from Duke University, as well as improved coagulation factor modulator systems (e.g., US7,304,041).

Regado Biosciences, Inc., a privately held company developing antithrombotic therapeutic aptamers with active control agents.

Regado Biosciences’ new therapeutic technology comprises a nuclease-stabilized RNA aptamer that can be controlled directly by its specific and complementary oligonucleotide active control agent.

Rigado’s technology is being applied to injectable antithrombotics, including anticoagulants and antiplatelet agents, a multi-billion dollar market in need of therapeutics with improved safety profiles and a greater degree of therapeutic control.

Regado’s technology is designed to give physicians the ability to actively and directly control each system’s therapeutic effect providing a safe and unique approach to personalized medicine, the company stated in the release.