Medicure Reports Positive Preclinical Results for Novel Antithrombotic

Medicure has announced positive results from the preclinical studies of the company's discovery drug candidate, MC-45308.

The studies examined the anticoagulant and antiplatelet activities of MC-45308 in both in vitro and in vivo experiments. The anticoagulant effects of MC-45308 were evaluated with a series of recognized lab tests used to monitor the clotting ability of whole blood. The global anticoagulant assay, which measures activated clotting time, was used to compare MC-45308 to the clinically approved anticoagulants bivalirudin and argatroban (direct thrombin inhibitors) at concentrations of 5 mcg/mL. In this test, MC-45308 compared favorably to both bivalirudin and argatroban by prolonging the activated clotting time further when used at the same concentration.

A second set of experiments involved the rabbit venous stasis model of thrombosis, which is commonly used to screen therapeutic compounds for antithrombotic activities. In this model, MC-45308 was more effective than both bivalirudin and argatroban when administered intravenously at a dose of 250 mcg/kg, effecting an approximately 80 percent reduction in clot score. The comparative bleeding profile of MC-45308, bivalirudin and argatroban were similar in this model, suggesting that MC-45308 may share a similar safety profile.

When tested against a variety of clinically relevant agonists including ADP, collagen and ristocetin, MC-45308 inhibited aggregation induced by each of these agonists, with the most pronounced effect seen in ADP induced aggregation. Inhibition of ADP-induced platelet aggregation has proven to be an effective clinical strategy in the management of a number of cardiovascular indications, including acute coronary syndromes, peripheral arterial disease, myocardial infarction and stroke, as evidenced by the success of the antiplatelet drug clopidogrel.