- Verseon’s anti coagulants are as effective as NOACS at preventing arterial and venous thromboembolism and thrombin-induced pulmonary embolism.
- Lead candidate has low renal clearance compared to NOACS – highly desirable for patients with impaired renal function.
Preclinical research to be presented at the American Society of Hematology (ASH) Annual Meeting shows that Verseon’s new class of direct thrombin inhibitors (VE-DTIs) are able to preserve platelet function. This indicates a reason why the VE-DTIs have a significantly reduced bleeding risk when compared to current NOACs.
The key finding of this study is that Verseon’s potent, highly selective direct thrombin inhibitors do not disrupt platelet function, while they still block fibrinogen cleavage. NOACs are associated with a bleeding risk and are known to strongly inhibit thrombin–mediated platelet activation which effects platelet function. Compared to the NOACs, Verseon’s drug candidates inhibit thrombin-mediated platelet activation from 19 to 900 fold less strongly.
Preclinical studies have already demonstrated that these drug candidates successfully prevent arterial and venous thromboembolism, as well as thrombin-induced pulmonary embolism, with efficacy comparable to existing anticoagulants.
“Preserving platelet function while preventing thrombosis could be a key to reducing bleeding risk. This discovery may lead to a new generation of safer blood thinners,” said Dr. John Deanfield, Professor of Cardiology at University College, London, who recently chaired a cardiology advisory board for Verseon.
Earlier this month, Verseon presented a poster at the American Heart Association (AHA) Scientific Sessions which demonstrated that one of their lead drug candidates shows favorable safety, toxicity and pharmacokinetics including very low renal clearance of less than 10 percent.
Low renal clearance would be highly desirable for patients with impaired renal function many of whom require anti-coagulants. Reported renal clearances for NOACS – apixaban, rivaroxaban, edoxaban and dabigatran range from 27 percent to 80 percent. The poster also featured a single oral dose tolerability study for this compound, which established a high maximum tolerated dose in vivo. Moreover, a seven-day repeat dose-range finding study, with oral dosing once a day, indicated that the compound is well tolerated.
Verseon CEO Adityo Prakash, speaking about drug discovery and development at the Financial Times Global Pharmaceutical and Biotechnology Conference in London earlier this month, explained that this new class of anticoagulants has been developed using Verseon’s proprietary, computationally driven drug discovery platform. “Our platform can provide better drugs through the generation of genuinely novel chemical matter,” said Prakash. “The results presented at AHA and ASH continue to validate our drug discovery process, which is producing a series of new drug candidates on an ongoing basis. In addition to our anticoagulant program, we currently also have programs on diabetic macular edema and oncology in preclinical testing, all with multiple novel drug candidates.”
Verseon’s abstract is available on the conference website and will be published in Blood, on December 1, 2016. Details of the ASH poster presentation are as follows:
Abstract title: “Novel Class of Direct Thrombin Inhibitors Prevent Thrombosis by Inhibiting Fibrinogen Cleavage While Preserving Platelet Function”
Abstract Number: #3834
Session Name: 332. Antithrombotic Therapy: Poster III
Date and Time: December 5, 2016, 6:00–8:00 p.m.
Location: San Diego Convention Center, Hall GH