Antithrombotic drug (project company Proton, LLC)
(code name – GRS, trade name – Granik®)
GRS (Granik®) is a new generation antithrombotic drug (small molecule), combining antithrombotic and antihypertensive effects and the ability to treat endothelial dysfunction – an important part of cardiovascular disease pathogenesis.
New mechanism of action: GRS is a soluble guanylate cyclase (sGC) stimulator; it activates the NO-sGC-cGMP signal pathway which regulates different cardiovascular functions, such as smooth muscle relaxation, endothelium permeability, platelet aggregation and antiplatelet function of the vascular wall.
Patent profile: patented in Russia, USA, EU.
Indications for use:
– prevention of atherothrombotic complications in combination with aspirin in patients with CAD (ACS, stable angina) after PCI and CABG;
Other promising indications;
– cerebrovascular diseases (prevention of secondary transitory ischemic attach and atherothrombotic complications);
– pulmonary hypertensions, including PAH and CTEPH;
– peripheral artery disease;
– chronic heart failure;
– prevention of venous thrombosis and pulmonary artery thromboembolism.
Main advantages:
– thrombosis prevention at 3 levels simultaneously:
– alleviates endothelial dysfunction;
– reversibly inhibits platelet aggregation;
– normalizes arterial blood pressure (prevents artery spasm);
– organ-protective properties (towards the heart, lungs, brain, kidneys and liver);
– wide therapeutic range (over 10 times better than competitors);
– independence of liver metabolism – low risk of drug interaction and activity fluctuation (inherent in competitors);
– low risk of bleeding (due to another mechanism of index);
– safety in long-term use.
Current status: Substance and dosage form are developed. Pilot batches for preclinical and clinical studies are produced. Phase Ia and Ib clinical trials (in healthy volunteers) are completed. Phase II clinical trial in patients with CAD (stable angina of I-III functional class) after endovascular revascularization was completed in March 2023. Phase III clinical trials are being prepared. Substance and drug production technology transfer to a production facility (JSC “Organica”) is ongoing.