Jun 07, 2018
FREMONT, Calif.—Verseon, a technology-based pharmaceutical company employing a computer-driven platform to develop a diverse drug pipeline, presented new preclinical data on its novel class of precision oral anticoagulants (PROACs) at this week’s BIO International Convention in Boston. Verseon’s PROACs demonstrate a unique combination of efficacy with lower bleeding in preclinical testing. This suggests that PROACs may be uniquely positioned to address a significant need for prolonged combination therapy with antiplatelet drugs.
Millions of patients worldwide could benefit from safe long-term co-dosing of an anticoagulant with one or more antiplatelet drugs (i.e. aspirin, PlavixTM) to prevent stroke or heart attack. However, current NOACs (novel oral anticoagulants) are not suitable for such therapy due to their high risk of bleeding.
In multiple preclinical studies, Verseon demonstrated that PROACs prevent the formation of blood clots but do not disrupt platelet function. This provides a biological explanation for the significantly reduced bleeding of PROACs compared to NOACs. In addition, this enables PROACs to more precisely influence the coagulation cascade, making them more suitable for co-administration with antiplatelet drugs.
At the BIO International Convention, Dr. Anirban Datta, Verseon’s Director of Discovery Biology, presented new ex vivo results for Verseon’s first PROAC clinical trial candidate, VE-1902. In healthy human volunteer blood, VE-1902 inhibits thrombin generation but without the prolonged delay in peak thrombin production observed with NOACs. At efficacious concentrations, VE-1902 is also a 500-fold weaker inhibitor of platelet activation than NOACs.
“These ex vivo findings further differentiate the unique anticoagulant properties of VE-1902 from NOACs,” said Dr. Datta. “We are very excited about these results and anticipate that they will be further confirmed in our first-in-human trial for VE-1902. We will use the assays performed on ex vivo human whole blood as biomarkers in the clinic for efficacy and bleeding risk.”
Verseon’s precision oral anticoagulants (PROACs) are potent, highly selective, reversible covalent inhibitors of thrombin. PROACs have shown excellent efficacy in multiple preclinical studies but do not disrupt platelet function. This unique feature could explain the low bleeding risk of these precision anticoagulants and makes them excellent candidates for use in long-term combination anticoagulant-antiplatelet therapy. The first development candidate is scheduled to enter clinical trials in mid-2018 and has also demonstrated very low renal clearance, a highly desirable property for patients with impaired kidney function. A second development candidate is expected to enter the clinic in 2019.
Verseon Corporation (www.verseon.com, AIM: VSN) is a technology-based pharmaceutical company that pairs a proprietary, computational drug discovery platform with a comprehensive in-house chemistry and biology workflow to develop novel therapeutics that are unlikely to be found using conventional methods. The Company is applying its platform to a growing drug pipeline and currently has four active drug programs in the areas of anticoagulation, diabetic macular edema, hereditary angioedema, and oncology. The anticoagulation program is scheduled to enter phase I clinical trials in 2018.
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