Verseon’s scientific journey to highly promising therapeutic candidates for cardiovascular disease appears in European Journal of Medicinal Chemistry
Verseon is delighted to announce that the European Journal of Medicinal Chemistry has published a paper (www.sciencedirect.com/science/article/abs/pii/S0223523422007577) describing the company’s groundbreaking research that led to promising novel drug candidates for cardiovascular disease. Cardiovascular disease is the leading cause of death and disability in the world. Hundreds of millions of patients worldwide need anticoagulants to prevent clots that lead to life-threatening events like strokes, heart attacks, and pulmonary embolisms.
However, currently prescribed so-called novel oral anticoagulants (NOACs) carry well-documented risks of major bleeds, which in many cases require hospitalization and can be life threatening. Developing drugs that prevent unwanted clots while preserving the body’s ability to stop excessive bleeding is the “Holy Grail” of anticoagulant drug programs. Verseon is developing a new generation of anticoagulants called PROACs (Precision Oral Anticoagulants) that address this significant unmet medical need.
The peer-reviewed paper documents how Verseon’s medicinal chemistry team optimized various physicochemical properties — including potency, selectivity, and in vivo stability — of compounds from a novel class called N-acylpyrazoles. The resulting reversible covalent thrombin inhibitors are highly effective at preventing clots in vivo. Yet unlike NOACs, they do not inhibit thrombin-mediated activation of platelets, a critical step to stop injury-induced bleeding. Because of their unique mechanism of action, Verseon’s drug candidates have demonstrated comparable efficacy to NOACs but with far lower bleeding risks in animal tests. The first lead candidate from this program is currently in clinical trials.
“We are pleased to publish the discovery of this novel class of direct thrombin inhibitors with unique pharmacology,” commented Dr. David Kita, Verseon’s Chief Scientific Officer. “We look forward to describing further work behind the development of our first PROAC clinical candidate (VE-1902), which we expect will address a significant unmet medical need affecting a very large number of cardiovascular patients worldwide.”
The scientific paper, entitled “Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors,” is available at https://doi.org/10.1016/j.ejmech.2022.114855.
Verseon International Corporation (www.verseon.com) is redefining delay, prevention, and treatment of disease. Using its unique physics- and AI-based molecule-engineering platform, Verseon is rolling out a steady stream of life-changing medicines. Each of the company’s drug programs features multiple novel candidates with unique therapeutic properties. Verseon’s pipeline currently includes seven drug programs spanning major cardiometabolic diseases and cancers.
Verseon’s precision oral anticoagulants (PROACs) are potent, highly selective, reversible covalent inhibitors of thrombin. PROACs have shown excellent efficacy in multiple preclinical studies. The fact that PROACs do not disrupt platelet function and demonstrate correspondingly low bleeding risk makes them excellent candidates for use in long-term combination anticoagulant-antiplatelet therapy. The first development candidate, VE-1902, is currently in clinical trials. Among other unique properties of PROACs, VE-1902 has very low renal clearance, a highly desirable feature for patients with impaired kidney function. Verseon also has a second anticoagulant development candidate, VE-2851, which is expected to enter clinical trials at a later date.