"I see great potential for chemistry to come forth and find new leads and new drugs and eventually compounds that will end up on the market." - Stephen Hanessian, Ph.D., University of Montreal.
Cardiovascular disease (CVD) is a major cause of death and disability and of rising health care cost around the world. CVD is known to claim about 1 in every 2.5 deaths in the United States. Further it has been estimated that more than 2,600 Americans die of CVD each day, which is about 1 death every 33 seconds. Ischemic Heart disease (IHD), which is also known as coronary artery disease (CAD), whose pathogenesis is often attributed to atherosclerosis of the pericardial vessels, has been found to be responsible for 48% of deaths from CVD.
Thrombosis remains one of the most significant causes of cardiovascular events like acute coronary syndrome (ACS), myocardial infarction, stroke, pulmonary embolism, deep vein thrombosis, peripheral arterial disease etc. Although there are several marketed therapies they are often associated with unwanted side effects. The vastness of the clinical problem clearly indicates the need for novel, safer and effective antithrombotic agents.
Led by an outstanding team of scientists, Medicure's Antithrombotic Discovery Program focuses on the design of compounds which exert dual anticoagulant /antiplatelet effects. The objective of Medicure's Antithrombotic Discovery Program is to develop new chemical entities with commercial potential to meet unmet cardiovascular and cerebrovascular needs. The program capitalizes on Medicure's well-established capabilities in the areas of medicinal chemistry, pharmacology, and pharmacokinetic evaluation, through a development program with CanAm Bioresearch Inc., and in collaboration with the Thrombosis Research Group, Loyola University Medical Centre, Montreal Heart Institute, and University of Alberta. Medicure’s library of dual acting anticoagulant/antiplatelet inhibitors is based on the vitamin B6 molecular structure.
Preliminary results have shown significant potential for four lead compounds in this program, MC-45301, MC-45308, MC-45350 and MC-45403 in preventing blood clots. These compounds demonstrate simultaneous anti-platelet (GPIIb/IIIa) and anti-coagulant (FIIa) effects, which could make them a major player in the management of cardiovascular diseases. Currently there are no drugs in the clinic or under development which possess these unique properties.
In addition to the dual inhibitor program, Medicure has an interest in developing novel Tissue Factor/Factor VIIa inhibitors for the management of thromboembolic disorders. Several novel potent molecules have been identified and further optimization is in progress.
To date, the Antithrombotic Discovery Program has produced hundreds of new chemical entities and several new leads have been generated for pre-clinical development.
Anti-Ischemics Program
One approach being undertaken is the design and synthesis of modified MC-1 mimetics to address ischemic and reperfusion injury. Medicure’s library of novel anti-ischemics includes MC-5422, a novel agent that has displayed potent capabilities of reducing damage from ischemic reperfusion and provides certain important advantages over the parent compound. Medicure’s library of anti-ischemics has been screened to evaluate their biological effect and may also provide benefit in other related and unrelated conditions.
