DBPR807, a safehighly specific CXCR4-targeting antagonist, has completed the concept validation of treating acute myocardial infarction (AMI) through both ratmini-pig animal disease models induced by occluding the left anterior descending artery (LAD). When DBPR807 (5 mg/kg, SC) was given in the rat model, a significant heart-protective effect was observed with reducing cardiac infarctionfibrosis by 4341, respectively. In the mini-pig model, DBPR807 (3 mg/kg, IV) treatment was allowed to improve 3-month LVEF up to 52 falling in a standard range between 50~70.