Antithrombotics prevent blood from clotting and help treat a wide spectrum of diseases ranging from deep vein thrombosis, pulmonary embolism, myocardial infarction and ischemic stroke. With the introduction of the first generation of oral once‐a‐day antithrombotics, the annual world market for such drugs is predicted to reach $24 billion per year, growing from just $6.5 billion in 2001.

A New Class of Inhibitors

Verseon has designed a class of compounds that inhibit thrombin through a novel mechanism of action. These compounds present a unique coagulation and dose response profile in functional assays and promise much lower bleeding liability than that of current drugs. As such, these compounds constitute a novel class of pharmacological therapeutics.

Most thrombin active site inhibitors, such as argatroban and dabigatran, are substrate‐derived and rely on the highly basic guanidine or benzamidine motifs for activity. Verseon's inhibitors are structurally unique in that they do not incorporate either of these moieties. Although it has been well established that the guanidine and benzamidine groups can impart excellent affinity for thrombin, their use often comes at a high cost of poor oral bioavailability. For example argatroban, which was approved by the FDA in 2000, must be administered intravenously due to its very poor oral bioavailability, minimizing its therapeutic potential. While the profile for dabigatran is somewhat improved, oral administration still requires the offending groups be masked in the double prodrug dabigatran etexilate (Pradaxa), which manages to only reach a poor oral bioavailability of 3-7%.