Neutrophil gelatinase-associated lipocalin (NGAL), also known as Lcn2 (lipocalin 2), or oncogene 24p3, is a gelatinase complex stored in mature neutrophil-specific particles. Glycoproteins are also produced by other cell types, including cardiomyocytes. NGAL is an early biomarker of acute kidney injury. Recently, NGAL has been found to be an independent predictor of major adverse cardiovascular events and mortality, but the relationship between NGAL and cardiovascular disease (CVD) has not been agreed. This article reviews the relationship between NGAL and coronary heart disease, hypertension and heart failure, and the targeted therapy of NGAL and CVD.