More than 30 years since their discovery, angiotensin-converting enzyme (ACE) inhibitors still represent one of the most commonly prescribed medications for treating hypertension and one of the favored first-line agents, particularly in the presence of high-risk conditions, such as diabetes. Even if the primary importance of blood pressure lowering in reducing cardiovascular and renal outcomes is unquestionable, ACE inhibitors remain a cornerstone among the different classes of antihypertensive drugs, as available evidence from several randomized controlled trials and meta-analyses highlights their beneficial effects in controlling blood pressure, treating heart failure, improving survival after heart attacks and preventing renal damage. ACE inhibitors are still unsurpassed in terms of efficacy in reducing clinical events, safety and costs. Given clinicians’ favorable experience with ACE inhibitors, the increasing prevalence of Type 2 diabetes worldwide and the fact that most hypertensive patients need two or more drugs for blood pressure control and concomitant reduction of the risk of cardiovascular (CV) and renal outcomes, it is very likely that ACE inhibitors will maintain an important role in the treatment of hypertension and other CV disorders in the future.