Beta-blockers (BBs) are a multiform group of drugs with multiple applications in the treatment of patients with cardiovascular disease. They are used in a variety of cardiac diseases (arterial hypertension, coronary artery disease, HF, cardiomyopathies, and arrhythmias) and it is worth emphasizing that their use has improved the survival of the patients with cardiovascular diseases. Bisoprolol is β-1 selective BB with no ISA and membrane-stabilizing effects. Bisoprolol also has minimal effects on glucose tolerance and plasma lipid profiles. Efficacy of bisoprolol is proved in various clinical trials for indications such as HF, hypertension, and coronary artery disease. Overall, bisoprolol is very well tolerated without significant serious AEs and may be considered as a preferred BB in patients having cardiovascular disease with diabetes mellitus.