In the past decade, accumulating evidence highlighted the role of monoamine oxidases (MAOs) in cardiovascular disease (CVD). MAOs are flavoenzymes located in the outer mitochondrial membrane, responsible for the degradation of neurotransmitters and biogenic amines. During this process they generate hydrogen peroxide, aldehydes and ammonia, species that can target mitochondria and induce mitochondrial dysfunction and cardiomyocyte death. Indeed, MAO inhibition affords cardioprotection in several models of CVD, such as ischemia/reperfusion, heart failure and diabetes. Importantly, a few studies provided encouraging results suggesting that MAO inhibition might be beneficial also in patients with CVD. Thus, selective and reversible MAO inhibitors, currently used as therapy for depression and neurodegenerative disorders, might be considered as candidate drugs for the treatment of CVD.