•Development of highly bioavailable curcumin (Theracurmin).•Effect of curcumin on cancer.•Effect of curcumin on cardiovascular disease.•Effect of curcumin supplementation and aerobic exercise training on arterial compliance.•Effect of curcumin supplementation on exercise-induced oxidative stress, inflammation, and muscle damage. Curcumin is a polyphenol with antioxidant and anti-inflammatory properties. It is highly lipophilic and sparingly soluble in water and very little is absorbed when it is ingested; therefore, improving its absorbability is a major priority. We developed a highly bioavailable curcumin called Theracurmin using submicron particle formation and surface controlled technology. In human study, the area under the blood concentration–time curve (AUC) after oral administration of Theracurmin was 27-fold higher than that of commercially available curcumin. Preclinical safety tests were conducted and no adverse effects were confirmed. The effects of Theracurmin on cancer (lung, pancreatic, and prostate), cardiovascular disease (heart disease), vascular function (arterial stiffness and central blood pressure), and bone and cartilage (knee osteoarthritis) were evaluated by collaborating with universities and medical institutions. In this paper, we present the development of Theracurmin and its effects in an animal model as well as in human clinical studies.