The lignans derived from flaxseed possess a number of pharmacological properties, both in vitro and in vivo. The ability of these lignans to reduce oxidative stress likely contributes to many of these biological properties. However, it is likely that flaxseed-derived lignans also provide pharmacological activity as a result of their interactions with specific receptors and enzymes within these biological systems. In order to better understand the therapeutic role that flaxseed and flaxseed lignans may play, further studies into the mechanisms of action is warranted. A better understanding of the pharmacology of flaxseed lignans will ultimately lead to appropriate recommendations for their therapeutic use, either as stand-alone therapies or as adjuvants with other pharmaceutical or natural products.