Galectin-3 (gal-3), a member of the galectin family, is a glycoprotein with high affinity for β-galactoside. Gal-3 is a cytoplasmically synthesized protein that can shuttle between the cytoplasm and nucleus and can even be transported to the membrane and secreted into the extracellular environment. Cardio/cerebrovascular diseases generally refer to ischemic or hemorrhagic diseases occurring in the heart, brain and systemic tissues, which are characterized by high morbidity, high disability rates and high mortality rates. To date, considerable research has demonstrated that gal-3 expression is aberrantly increased and plays important roles in cardio/cerebrovascular diseases, such as acute ischemic stroke (AIS), myocardial fibrosis, acute coronary syndrome (ACS), and heart failure (HF). Hence, understanding the biological roles of gal-3 in these diseases may be essential for cardio/cerebrovascular disease treatment and diagnosis to improve patient quality of life. In this review, we summarize current research on the roles of gal-3 in human cardiovascular diseases and potential inhibitors of gal-3, which may provide new strategies for disease therapies.