Objective To provide the China Essential Drugs List with evidence-based data for selecting the antihypertensive drugs in ARBs category. Methods With following search terms such as losartan, atenolol and clinical trial, the relevant clinical trials on losartan and atenolol for treating hypertension in both Chinese and English languages were collected from the EMbase, PubMed, The Cochrane Library, website of clinicaltrials.gov, CNKI, VIP and CBM. Results A total of 52 studies were pooled in this systematic review, of which most focused on the losartan intervention for endpoint reduction in hypertension (LIFE) study. The main results were that: a) With the same effects in lowering blood pressure, losartan was superior to atenolol in toleration and reducing left ventricular hypertrophy; b) Losartan was more effective than atenolol in preventing cardiovascular and cerebrovascular events, especially better in preventing new-onset stroke; c) Losartan was superior to atenolol in the patients complicated with or without diabetes mellitus, with or without atrial fibrillation, and with low hemoglobin or high blood uric acid, as well as in the patients co-treated by aspirin or hydrochlorothiazide; d) No matter either losartan or atenolol used in the aggressive antihypertensive therapy, the risk of sudden cardiac death got increased in hypertensive patients with prolonged QRS duration; e) Losartan was superior to atenolol in treating patients with smoking and drinking habits; and f) There were no significant differences between losartan and atenolol in hypertensive patients of black people, different genders, as well as the patients with mutant angiotensin-converting enzyme (ACE) gene. Conclusion Losartan has the same antihypertensive effects as atenolol dose, but it is more effective in reducing left ventricular hypertrophy, and has more benefits to hypertensive patients beyond lowering blood pressure, such as, reducing urine protein and uric acid rather than high density lipoprotein.