The preclinical data, presented by Verseon’s Director of Discovery Biology Dr. Anirban Datta, shows that VE-2851 potently inhibits thrombin and is highly selective against a panel of related serine proteases. It has pharmacokinetics suitable for oral administration and was well tolerated in a 14-day dose-range finding study. In preclinical tests, the candidate also displays efficacy comparable to marketed anticoagulants, but with a significantly lower bleeding risk.
Similar to Verseon’s first development candidate VE-1902, which is scheduled to enter phase I trials in early 2018, VE-2851 likewise does not disrupt platelet function, a critical component in wound healing, healthy tissue growth, and hemostasis (stopping of bleeding). This feature distinguishes Verseon’s class of anticoagulants from current NOACs and provides a biological rationale for the low bleeding risk.
“The pharmacological profile of our anticoagulants puts us in the unique position to address the unmet need for long-term combination therapy with anti-platelets,” commented Verseon’s CEO Adityo Prakash. “This has the potential to have a major impact on the anticoagulation market.”
“We are excited to have two drug candidates heading to the clinic in 2018,” said Dr. Datta. “Both development candidates act as potent anticoagulants without disrupting platelet function. This may significantly reduce the risk of major adverse cardiovascular events and bleeding when used in conjunction with antiplatelet drugs.”
Today’s anticoagulant market is dominated by the NOACs, oral anticoagulants with less need for constant monitoring and reduced drug and food interactions compared to their predecessors. However, the bleeding risk associated with the NOACs remains high, which is particularly problematic when they are co-dosed with antiplatelet drugs. Such life-long combination therapy is desired for the many patients suffering from both atrial fibrillation and coronary artery disease, but current treatment guidelines limit it to at most one year due to safety concerns.
Dr. Datta’s presentation will be featured in Thrombosis.TV, a leading destination for venous and arterial thrombosis education, news, and expert opinion.
Verseon uses a computer-driven drug discovery platform embedded in a comprehensive chemistry and biology workflow to design new drug candidates for a wide range of diseases. In addition to the anticoagulation program, the company currently has drug programs in diabetic macular edema, hereditary angioedema, and oncology.
About Verseon’s anticoagulation program
Verseon’s potent, highly selective oral direct thrombin inhibitors 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. Two development candidates are expected to enter clinical trials in 2018, one of which has also demonstrated very low renal clearance, a highly desirable property for patients with impaired kidney function.