This paper reviews the most recent clinical and experimental studies on diacerein, both of which are under investigation. Diacerein could be a disease-modulating agent in osteoarthritis because structural benefits have been reported in recent trials. Moreover, after an empirical use, studies return to the experimental field to understand the mechanism of action of this molecule. However, clinical trials using new sets of criteria could be conducted to estimate the structural modulating effect of diacerein; experimental studies must be performed to understand this effect.