As a new humanized monoclonal antibody against the interleukin-6 receptor, tocilizumab is currently used for the treatment of rheumatoid arthritis (RA) patients. Tocilizumab was reported to provoke drug-related liver toxicity, although there have been no reports on significant liver toxicity from tocilizumab in Korean patients with RA to date. Here, we describe the first case of tocilizumab-related liver toxicity in a patient with complicated RA, accompanied with macrophage activation syndrome, who had received tacrolimus and prednisolone and in whom both conventional disease modifying anti-rheumatic drugs, including methotrexate, leflunomide and sulfasalazine or tumor necrotizing factor-α blockades, were contraindicated due to drug eruption and a history of lung cancer.