Hypertension is a common disease, and hypertensive patients are at increased risk of cardiovascular events. The prevalence and socioeconomic burden of hypertension in the Asia-Pacific region are predicted to increase in the coming decades. Effective blood pressure lowering reduces overall cardiovascular morbidity and mortality in patients, yet doubt has been raised regarding the use of (mainly older generation) β-blockers as initial therapy in hypertension. Consequently, several international treatment guidelines do not recommend β-blockers for the treatment of hypertension. However, in contrast to first-generation and second-generation β-blockers, the third-generation, vasodilating β-blocker nebivolol has a considerably better metabolic, haemodynamic and side effect profile. In addition to providing effective blood pressure control similar to other β-blockers and drugs from other antihypertensive classes, nebivolol exerts a dual mechanism for increasing the bioavailability of the naturally occurring vasodilator nitric oxide. The clinical benefits and significance of enhancing nitric oxide levels in hypertensive patients have been shown in direct comparisons of nebivolol with other β-blockers. While β-blockers generally provide comparable blood pressure reductions, only nebivolol demonstrated enhanced vasodilation and blood flow by increasing the expression of endothelial nitric oxide synthase and therefore increasing nitric oxide release from the endothelium. In contrast to other β-blockers, therefore, it has been suggested that nebivolol has beneficial effects in several hypertensive subgroups due to its vasodilating properties. Considering the existing data, it may be timely for treatment guidelines to recommend third-generation vasodilating β-blockers as a first-line option for the pharmacotherapy of hypertension.