Hypertension is one of the most important risk factors for the development of ischemic heart diseases, stroke, disability, vascular dementia, heart failure, renal dysfunction, retinopathy, and premature death. Despite the use of two or more blood pressure lowering medications, a considerable proportion of patients show poor control. Current antihypertensive medications show the limitation of use and effect in obese population, certain races like black population and also in renal impairment. Thus, there is an impending need to develop novel classes of antihypertensive agents acting on new targets with diversified mechanisms of action to more effectively manage raised blood pressure. With the introduction of the recent concept of overactive brain renin angiotensin system in cardiovascular disorders, attempts have been made to identify a molecule with the potential of inhibiting aminopeptidases involved in the formation of Angiotensin III. A novel aminopeptidase A inhibitor, also a prodrug Firibastat is currently undergoing development in Phase III clinical trials for hypertension as well as chronic heart failure. We hereby, provide an updated summary of evidence generated so far with Firibastat and also a glimpse into the therapeutic potential of this novel candidate extending beyond the spectrum of essential hypertension