Diacerein (4,5-bis(acetyloxy)-9,10-dioxo-2-anthracene carboxylic acid) is an oral agent that has been developed specifically for the treatment of osteoarthritis. It has a novel mode of action that differentiates it from non-steroidal anti-inflammatory drugs (NSAIDs) and other conventional forms of drug therapy.Clinical trials have shown tha diacerein is highly effective in relieving the symptoms of osteoarthritis. Moreover, results from studies conducted in vitro, in animals and in humans indicate that it may be able to modify the course of the disease. Diacerein has a unique mode of action, namely the inhibition of IL-1, which distinguishes it from other drugs indicated for the treatment of osteoarthritis.
In many in vitro models, therapeutic levels of diacerein and rhein, its active metabolite, have been shown to inhibit the synthesis and activity of IL-1, as well as to stimulate anabolic processes.