Heparin has long been known to possess biological effects that are unrelated to its anticoagulant activity. In particular, much emphasis has been placed upon heparin, or novel agents based upon the heparin template, as potential anti-inflammatory agents. Moreover, heparin has been reported to possess clinical benefit in humans, including in chronic inflammatory diseases and cancer, that are over and above the expected effects on blood coagulation and which in many cases are entirely separable from this role. This chapter aims to provide an overview of the non-anticoagulant effects that have been ascribed to heparin, from those involving the binding and inhibition of specific mediators involved in the inflammatory process to effects in whole system models of disease, with reference to the effects of heparin that have been reported to date in human diseases.