Dilevalol combines blockade of β-receptors with vasodilation that is mainly due to a β2-agonist activity. This prospective, randomized, double-blind, multicenter trial was carried out in patients with supine diastolic blood pressure (SuDBP) of 95-115 mm Hg. After a 4-week placebo washout phase, 309 patients were randomized to dilevalol and 136 to metoprolol. On a 2- to 8-week titration phase, dilevalol was increased from 200 to 1600 mg once daily or metoprolol from 100 to 400 mg once daily to achieve a SuDBP < 90 mm Hg and ≥ 10 mm Hg decrease from baseline. Responders were followed over a 1 year maintenance phase. The mean patient age was 51 years, 72% were men, and 54% white. The reductions in blood pressure (BP) and heart rte (HR) are shown. The two drugs were similar with regard to percentage of normotensives (60%). Significantly (p = 0.03) more patients discontinued metoprolol due to side effects than dilevalol, specifically for depression and impotence. Nervousness, depression, bradycardia, fatigue, and pruritus were significantly (p < 0.04) more frequent with metoprolol than with dilevalol, as were cold extremities (2% versus <1%). Transaminase levels were elevated from a normal baseline in 2% of patients on dilevalol and in 1% on metoprolol (N.S.) Dilevalol elevated HDL cholesterol by 8.5% with no change in cholesterol or LDL. Triglycerides increased 21 mg/dl with dilevalol and 42 mg/dl with metoprolol. We conclude that both dilevalol and metoprolol are equally effective in lowering BP. Dilevalol appears to have a more favorable safety profile than metoprolol.