Hepatitis poses a significant health issue worldwide as it may progress to cirrhosis and hepatocellular carcinoma. The crucial role of liver in different metabolic and synthetic functions of the body stimulates researchers to continually explore and develop different hepatoprotective drugs. The present study was designed to assess the potential hepatoprotective effect of deferasirox (DFX) in a rat model of acute liver injury induced by concanavalin A (Con A) at a dose of 20 mg/kg intravenously dissolved in normal saline solution. The hepatoprotective effect of DFX was screened at the doses (25, 50, and 100 mg/kg) via assessing the hepatotoxicity indices and histopathological examination. DFX at a dose of 100 mg/kg was the most effective in preventing the rise in activities of hepatotoxicity serum markers; alanine aminotransferase (ALT), and aspartate aminotransferase (AST) enzymes and histopathologic changes induced by con A.