Patients with cancer are frequently exposed to risk of renal injuries associated with disease-related or iatrogenic causes. Nephrotoxicity is a potential adverse effect of anti-cancer agents and may result in a variety of functional abnormalities, including glomerular or tubular dysfunction, hypertension and disturbance of the renal endocrine function. In this review article, we comprehensively discuss the incidence, clinical presentation, prevention and management of anti-cancer agent-induced renal dysfunction. We focus on both relatively new anti-cancer agents (bevacizumab, gefitinib, gemcitabine, imatinib, rituximab and trastuzumab) and traditional agents (cisplatin, methotrexate, ifosfamide and taxanes) to cover a selection of the most frequently used anti-cancer agents. Increased understanding of the mechanism of renal injury by these agents is considered to be important for developing novel anti-cancer agents that have far fewer adverse effects on kidneys.