Abstract: Renal cell carcinoma (RCC) is currently one of treatment-resistant malignancies and is not sensitive to con-ventional radiotherapy or chemotherapy. The effective rate of high dose of recombinant human interleukin- 2 (IL- 2) and re -combinant human interferon-α (IFN-α) was only 10%-15% . Advances in the understanding of cancer at molecular level have led to more progress in the development of anti-cancer agents. Recently, mutation of Von Hippel-Lindau (VHL), Ras, PTEN genes have been observed in RCC and the mutation can result in different expression levels of RTK. Among the newly invented medications for targeted cancer therapy, protein kinase inhibitors target intracellular molecules crucial in sig-naling pathways of cancer cell survival and proliferation. Compared with conventional chemotherapy and immune therapy, targeted therapy is effective, with fewer adverse effects. According to 2009 NCCN Clinical Practice Guidelines in oncolo -gy, this article reviewed the clinical application of sunitinib, sorafenib, temsirolimus, and bevacizumab in the targeted thera-py for renal cell carcinoma.