Background: Cardiovascular disease is the leading cause of morbidity and mortality worldwide in developed countries, and its social and economic burden is expected to increase dramatically over the next decades. Despite significative improvement in the pharmacological treatment, and the huge advances in prevention, the quest for new molecular targets and for novel, more efficient and personalized therapies is still a priority for this group of pathologies.Objective: The paramount complexity of the metabolic networks responsible for the onset and progression of cardiovascular disease is highlighted by the wide and diverse array of new molecular targets recently described in literature. In this brief review, we focused our interest on a subset of promising molecular targets for the development of new pharmacological treatments specific for cardiac diseases such as coronary artery disease, heart failure and myocardial infarction. Conclusion: The global quest for new molecular targets for the treatment of cardiac diseases is leading to an impressive amount of records in the more recent literature. Although several promising molecular pathways have been identified so far, great caution should be used in considering all these targets effective in promoting the production of new drugs. The identification of suitable therapeutic targets is in fact an ongoing challenge that often lacks enough pre-clinical and clinical studies, which hinders the effective utilization of several new drugs due to a lack of efficacy or induction of safety liabilities.