Objective To determine the reversal effect of amlodipine combined with telmisartan (AT) or compound amiloride (ACA) on hypertensive left ventricular hypertrophy (LVH), and the effect on plasma concentrations of endothelin-1 (ET-1) and N-terminal pro-B-type natriuretic peptide (NT-proBNP) in the patients. Methods Fifty hypertensive patients with LVH who were admitted in Department of Cardiology, the First Affiliated Hospital of Xi’an Jiaotong University, during December 2007 to December 2008 were prospectively subjected in this study. There were 27 males and 23 females, at age of (61.2±7.2) years, and then randomly assigned to amlodipine (2.5mg/d) plus telmisartan (40mg/d) group (AT group, n＝25), and amlodipine (2.5mg/d) plus compound amiloride (half a tablet/d, containing amiloride 1.25mg and hydrochlorothiazide 12.5mg) group (ACA group, n＝25). The blood pressures, left ventricular mass index, plasma concentrations of ET-1 and NT-proBNP in the 2 groups were measured before and in 1 year after treatment. Another 50 healthy individuals, including, 27 males and 23 females with age of (60.4±5.4) years who received physical examination during the same period, were also enrolled as normal controls. Results The plasma concentrations of ET-1 and NT-proBNP were significantly higher in hypertensive LVH patients than in normal controls (P＜0.01). There was no significant difference in baseline indices between the AT and ACA groups before treatment. After 1 year’s antihypertensive treatment, either AT group or ACA group resulted in significant decreases in systolic blood pressure, diastolic blood pressure, left ventricular mass index (LVMI), and plasma concentrations of ET-1 and NT-proBNP (P＜0.01). AT group showed more significant effects on above indices than ACA group (P＜0.05). Conclusion The plasma concentrations of ET-1 and NT-proBNP are closely related to hypertensive LVH. The effect of AT is superior to the ACA in the reduction of plasma ET-1 concentration and reversal of LVH. The amlodipine-based combined antihypertensive therapy reverses LVH probably through reducing blood pressure and plasma concentrations of ET-1 and NT-proBNP.