Carbohydrates play a critical role in many biological processes and disease states including cancer, inflammation and infection. The development of carbohydrates as therapeutics continues to gain interest, as the biological roles of these biopolymers are further elucidated and understood. However, many carbohydrates display poor affinity, stability and bioavailability characteristics, which has led to a widely held view that this class of molecules make poor drugs. As there are already a significant number of carbohydrate-based drugs presently being employed by physicians, it is clear that some carbohydrates do make effective drugs. Recent advances in (a) the understanding of carbohydrate specific transport mechanisms, and (b) the development of novel carbohydrate based bioactives which may overcome many of the previous limitations of stability and bioavailability, suggest that carbohydrate-based compounds may provide a rich source of new drug candidates for a variety of diseases.