Abstract: The heat shock protein 90 (HSP90) molecular chaperone protects cellular proteins through the ubiquitin-proteasome pathway. HSP90 is overexpressed in cancer cells to maintain the potential of survival, proliferation, anti-apoptosis and metastasis. This review focuses on the small molecule HSP90 inhibitor-ganetespib, which has been widely used in the clinical trials of cancer treatment. Single-agent HSP90 inhibitor therapy is efficacious. Besides, this inhibitor can potentiate the effects of other molecularly targeted therapy and standard chemotherapy while overcoming drug resistance in some type of tumors. The efficacy of ganetespib in treatment of human solid tumor is reviewed in this article.