Cardiovascular disease or hypertension is caused by genetic abnormalities and/or environment factors. Molecular biological and biochemical analyses have demonstrated the cardiovascular disease or hypertension is related to increased gene products such as vasoactive peptide, activated signal transduction pathways, and cell surface antigen, etc. Molecular target drugs have been designed to suppress these molecules via receptor, signal transduction pathways, or mRNA. Differing from conventional drug, molecular target drugs show higher specificity for pathophysiology in cardiovascular disease or hypertension. Although term of 'molecular target drug' is not used frequently in the field of cardiovascular or hypertension, I describe in this review, angiotensin receptor blocker, endothelin receptor blocker and statin, because these three drugs are indispensable to treat these diseases in the present clinical setting.