Nov 15, 2017
FREMONT, Calif.—Verseon, a technology-based pharmaceutical company employing a computer-driven platform to develop a diverse drug pipeline, presented a second development candidate for clinical trials from its anticoagulation program at the American Heart Association’s (AHA) Scientific Sessions 2017, yesterday. VE-2851 shows excellent efficacy paired with low bleeding risk in preclinical testing and is expected to enter clinical trials in 2018.
The candidate potently inhibits thrombin and is highly selective against a panel of related serine proteases. VE-2851 also shows pharmacokinetics suitable for oral dosing and was well tolerated in a 14-day dose-range finding study. In preclinical efficacy models such as the arteriovenous shunt thrombosis model, the compound displayed comparable efficacy to marketed anticoagulants. Similar to Verseon’s first development candidate VE-1902, which is expected to enter phase I trials in early 2018, VE-2851 likewise potently inhibits thrombosis, but does not disrupt platelet function. It shows 30–40 fold weaker inhibition of thrombin-mediated platelet activation in vitro and allows up to 5-fold higher maximum platelet activation in vivo compared to current NOACs. This distinguishing feature of Verseon’s anticoagulants provides a biological rationale for their improved hemostatic control and the resulting lower bleeding risk observed in preclinical bleeding time tests.
“We are excited to have two drug candidates heading to the clinic in 2018,” said Dr. Anirban Datta, Verseon’s Director of Discovery Biology, who presented the results at the AHA conference. “Both development candidates act as potent anticoagulants without disrupting platelet function. This may allow them to become the first anticoagulants suitable for long-term combination therapy with antiplatelet drugs, achieving a significantly reduced risk of both major adverse cardiovascular events and bleeding.”
The full AHA abstract is available on the conference website and will be published in Circulation. Dr. Datta’s presentation will also be featured in Thrombosis.TV, a leading destination for venous and arterial thrombosis education, news, and expert opinion.
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.
Verseon Corporation (www.verseon.com, AIM: VSN) is a technology-based pharmaceutical company that combines 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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