Azilsartan medoxomil (AZL-M) is a prodrug quickly hydrolyzing to the active moiety azilsartan, a potent and highly selective ARB with estimated bioavailability of 60% and half-life of 12 hours. Azilsartan is possibly a promising molecule for control of hypertension especially in setting of cardio-diabetes because of its multiplicity of actions. AZL-M was found to be more effective in terms of reducing indices of blood pressure over alternative ARBs or angiotensin-converting enzyme (ACE) inhibitors with minimal side effects. Preclinical studies have established pleiotropic effects for AZL-M beyond its primary antihypertensive role through differential gene expression, up regulation of membrane receptors and favorable effect on selective intracellular biochemical and pro-atherosclerotic pathways.