Metoprolol (MTP), a hypertension depressor, has been increasingly detected even after conventional water treatment processes. In this study, the removal of MTP was compared using chlorination (Cl-2), UV-C photolysis, and UV/chlorination (Cl-2/UV) reactions. The results showed that the UV/chlorination reaction was most effective for MTP removal. MTP removal during UV/chlorination reaction was optimized under various conditions of UV intensity (1.1-4.4 mW/cm(2)), chlorine dose (1-5 mg/L as Cl-2), pH (2-9), and dissolved organic matter (DOM, 1-4 mg C/L) using a two-level factorial design with 16 experimental combinations of the four factors. Among the factors examined, DOM scavenging by OH radicals was the most dominant in terms of MTP removal during UV/chlorination reaction. The established model fit well with the experimental results using to various water samples including surface waters, filtered and tap water samples. The optimized conditions (UV intensity = 4.4mW/cm(2), [Cl-2] = 5 mg/L, pH 7, and [DOM] = 0.8-1.1 mg C/L) of the model removed more than 78.9% of MTP for filtered water samples during UV/chlorination reaction. Using LC-MS/MS, five byproducts of MTP (molecular weight: 171, 211,309, 313, and 341, respectively) were identified during UV/chlorination reaction. Based on this information, the MTP transformation mechanism during UV/chlorination was suggested. Our results imply that applying UV/chlorination process after filtration stage in the water treatment plant (WTP) would be the most appropriate for effective removal of MTP. (C) 2014 Elsevier B.V. All rights reserved.