The study was evaluated to investigate the efficacy of selenocystine (CysSeSeCys), a well-known organoselenium compound, on the prevention of carbon tetrachloride (CCl(4))-induced acute hepatic injury in Wistar rats. Forty healthy male Wistar rats were utilized in this study. Acute hepatotoxicity was induced by CCl(4) intoxication in rats. Serum biological analysis, oxidative stress, immune parameters, and gene expression of COX-2 and CYP2E1 were carried out. Pretreatment of CysSeSeCys prior to CCl(4) administration significantly prevented an increase in serum hepatic enzymatic activities. In addition, pretreatment of CysSeSeCys significantly prevented the formation of ROS, MDA, depletion of glutathione, and alteration of antioxidant enzyme activities in the liver of CCl(4)-intoxicated rats. This study also revealed that pretreatment with CysSeSeCys normalized the levels of interleukin 6 and10, IgG, and CD4 cell count. Pretreatment of CysSeSeCys significantly reversed COX-2 inflammatory response and the upregulation of CYP2E1 expression as well. Histopathological changes induced by CCl(4) were also significantly attenuated by CysSeSeCys pretreatment. CysSeSeCys has a potent hepatoprotective effect on CCl(4)-induced liver injury in rats through its antioxidative, immunomodulatory and anti-inflammatory activity.