Vicagrel

Vicagrel is a new antiplatelet drug jointly developed by Jiangsu VcarePharmatech Co., Ltd. and China Pharmaceutical University. The IP right of Vicagrel is wholly owned by Jiangsu Vcare Pharmatech Co., Ltd. The NCE and process patent of Vicagrel has been authorized in China, US, Japan, EU and Canada. Moreover, the related PCT application has entered the national phase in more than 30 countries. A related research paper was published in the Journal of Medicinal Chemistry (2012, 55, 3342–3352) and was highlighted in SciBX under the Nature publishing group.

Vicagrel is a prodrug, which is activated through two-step metabolism in vivo to generate an active metabolite that is identical to that of the commercially available drug Clopidogrel (Plavix). Vicagrel, as a P₂Y₁₂ receptor antagonist, can inhibit ADP-mediated activation of glycoprotein GP IIb/IIIa complex, and thus inhibit the platelet aggregation. Additionally, Vicagrel can block the platelet aggregation resulting from ADP release by other agonists. Similar to Clopidogrel, Vicagrel has an irreversible antagonistic effect on platelet P₂Y₁₂ receptor. Accordingly, Vicagrel has an impact on the whole life span of platelets exposed thereto, and the rate of recovery of normal platelet functions is identical to the rate of renewal of platelets.

The commercially available drug Clopidogrel is also a prodrug, which has no activities itself, and can exert a therapeutic effect only through metabolic conversion into Clopidogrelthiolactone by the hepatic drug-metabolizing enzyme CYP2C19 and then into an active metabolite of Clopidogrel. The main disadvantage of Clopidogrel in clinical application is the “Clopidogrel Resistance” in patients suffering from poor CYP2C19 metabolism. The new drug design concept of Vicagrel is to utilize the widely present esterase-mediated metabolic pathways in place of the hepatic CYP2C19-mediated metabolic pathway, thereby overcoming Clopidogrel Resistance.

CFDA approved IND application of Vicagrel in March of 2015. Pre-clinical and phase I clinical trials of Vicagrel have been finished. Currently, phase II clinical trials are ongoing. Now, we are seeking collaboration for international new drug application of Vicagrel.