Coronary artery disease is the leading cause of morbidity and mortality worldwide, needing innovative strategies for cardiac protection and repair. This thesis explores the fundamental principles of cardio-protection, distinguishing between acute and chronic mechanisms, and explains in detail the process of ischaemia/reperfusion (I/R) injury process as a target of therapeutic interventions. The molecular process of I/R injury is discussed, which consists of key processes like oxidative stress, mitochondrial dysfunction and calcium overload. Classical and emerging cardio-protective strategies which include ischaemic preconditioning, post-conditioning and remote conditioning, as well as targeted pharmaceutical therapies which are critically examined, include molecular targets like hypoxia-inducible factor-1, microRNAs and sodium-glucose cotransporter (SGLT-2) inhibitors. In addition, the role of existing drugs and their role as cardioprotective agents, like metformin, colchicine and cyclosporine A. Moreover, the innovation of antibody-based therapies, cell-based angiogenesis for cardiac repair with the application of biomarkers specific for cardiac repair monitoring. This paper highlights the interplay between molecular biology, pharmacology and the clinical application of targeted therapy aimed at reducing myocardial injury and promoting cardiac regeneration.