Novel HDACi CS014
The investigational drug candidate CS014 belongs to Cereno’s HDAC inhibitor program capitalizing on the principle of epigenetic modulation. In March 2019, CS014 was acquired from Emeriti Bio and is being developed in a collaboration between Cereno, Emeriti Bio and University of Michigan. The drug candidate CS014 is being developed as a treatment to effectively prevent arterial and venous thrombosis without increasing the risk of bleeding. An ongoing phase I, first in human, trial is evaluating the safety and tolerability of CS014 in healthy volunteers.
The innovative drug candidate represents a novel approach to antithrombotic treatment without the associated increased risk of bleeding. CS014 is a new chemical entity with a multi-fold mechanism of action as an epigenetic modulator – regulating platelet activity, local fibrinolysis, and clot stability for the prevention of thrombosis without increased risk of bleeding, as documented in preclinical studies. Given the potential for the additional disease-modifying properties seen with HDAC inhibition, additional cardiovascular benefits of CS014 may be expected, including amelioration of inflammation, fibrosis, vascular changes and elevated blood pressure. HDAC inhibition as thrombosis prevention could fundamentally change the thrombosis prevention landscape and meet a major unmet medical need.
Preclinical data suggests that CS014 is an effective HDAC inhibitor that inhibits platelet activity, fibrin accumulation and small and large vessel thrombosis while maintaining hemostasis in a dose-dependent manner. Also, when combined with rivaroxaban, CS014 inhibited the formation of platelet and fibrin-rich thrombosis without adding to the bleeding risk. These cumulated data show that CS014 has the potential to enrich the toolbox of antithrombotic therapies in both venous and arterial thrombosis. With clinical use of the HDAC inhibitor CS014, through epigenetic modulation, it could be possible to prevent thrombosis without an increased risk of bleeding, a much-desired unmet medical need. Additional preclinical and clinical studies will be conducted to determine the first indication where CS014 has the greatest potential as a treatment to prevent thrombosis.