Nirog is developing a class of compounds that inhibit thrombin through a novel mechanism of action with good safety pharmacology and functional activity in coagulation assays.

Nirog's compounds are unique not only in their mechanism of action, but also due to their structural characteristics. Most thrombin active site inhibitors, such as argatroban and dabigatran, are substrate-derived and rely on an amidine motif for activity. Nirog's inhibitors are structurally unique in that they do not rely on an amidine moiety for affinity. Although it has been well established that the amidine group can impart excellent affinity for thrombin, its use often comes at a high cost such as poor oral bioavailability. For example argatroban, which was approved by the FDA in 2000, must be administered intravenously due to its poor oral bioavailability, minimizing its therapeutic potential. While the profile for dabigatran (Pradaxa) is somewhat improved, oral administration still requires the offending groups be masked in the double pro-drug dabigatran etexilate.

Due to their unique nature, Nirog's family of thrombin inhibitors are potential first‐in‐class anti-coagulants and are expected to exhibit novel pharmacology. In addition to hemostatic disorders, thrombin is also implicated in inflammation, cancer, fibrosis and CNS diseases, all of which represent new opportunities for this new class of compound.

Program