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Bi-Lian Chen,1,* Yin-Zhuang Zhang,1,* Jian-Quan Luo,2,3 Wei Zhang2,3 1Department of Geriatrics, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of China; 2Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of China; 3Institute of Clinical Pharmacology, Central South University, Changsha, Hunan, People’s Republic of China *These authors contributed equally to this work Background: Hypertension is the most common chronic disease and the calcium channel antagonist is the most popularly used antihypertensive drug in Chinese patients. Azelnidipine is a third generation and long-acting dihydropyridine calcium channel antagonist. A series of research has demonstrated that azelnidipine produced an effective antihypertensive effect in patients with essential hypertension. Now it is need to summarize clinical use of azelnidipine in the treatment of hypertension in Chinese patients. Methods: Relevant literature was identified by performing searches in PubMed and CNKI (China National Knowledge Infrastructure), covering the period from January 2003 (the year azelnidipine was launched) to July 2014. We included studies that described pharmacology ofazelnidipine, especially the pharmacokinetics, clinical efficacy, and safety and tolerability of azelnidipine in a Chinese population. The full text of each article was strictly reviewed, and data interpretation was performed. Results: In Chinese healthy volunteers, a single-dose oral administration of azelnidipine 8–16 mg had a peak plasma concentration of 1.66–23.06 ng/mL and time to peak plasma concentration was 2.6–4.0 hours and the area under the plasma concentration versus time curve from time 0 hour to 96 hours was 17.9–429 ng/mL·h and elimination half-life was 16.0–28.0 hours. Anumber of clinical trials have demonstrated that azelnidipine produced a significant reduction in blood pressure in Chinese patients with mild-to-moderate hypertension, which was similar to that of other effective antihypertensive drugs such as amlodipine, zofenopril, and nifedipine. In addition to its antihypertensive effect, azelnidipine had other cardiovascular protective effects as well, like anti-oxidative action, decreasing heart rate, and improving systolic and diastolic function. Azelnidipine was generally well tolerated in Chinese patients and no severe adverse events were observed. Conclusion: Azelnidipine is effective and safe in the treatment of hypertension in Chinese patients. Keywords: azelnidipine, hypertension, Chinese, pharmacology, pharmacokinetics, efficacy