Although remarkable advancement in computed tomography (CT) has been achieved, heart rate control is important to maintain an optimal image quality in coronary CT angiography. Oral or intravenous β-blockers are used as premedication for this purpose. Landiolol was developed as a β-blocker with very high cardioselectivity (β1/β2 =255) and short half-life (4 minutes). In this review, we report the pharmacological features and usage of landiolol and also its effects on heart rate and image quality in coronary CT angiography. In addition, we discuss the safety of landiolol.