Histone deacetylases are a class of enzymes that play important roles in post translational modifications of histones by deacetylating the lysine residues as well as interacting with various non-histone proteins. This type of enzymes is closely related to oncogenesis and has been proved to be attractive targets for designing novel anti-cancer agents. Over the last 10 years, a large number of HDACs have entered pre-clinical and/or clinical trials. Among these drug candidates, the pan-HDAC inhibitor, panobinostat demonstrated high therapeutic potential as monotherapy and combined therapy in both preclinical models and clinical cancer patients. In this review, we have mainly focused on the recent progress of the clinical studies about panobinostat, and discussed its anti-cancer effects and molecular rationale for the treatment strategies.