Calcitriol, the hormonally active form of vitamin D, is well known for its diverse pharmacological activities, including modulation of cell growth, neuromuscular and immune function and reduction of inflammation. Calcitriol and its analogs exert potent effects on cellular differentiation and proliferation, regulate apoptosis and produce immunomodulatory effects. The purpose of this review is to provide information on various physiological and pharmacological activities of calcitriol and its newly discovered analogs. Special emphasis is given to skin diseases, cancer, diabetes and multiple sclerosis. A discussion is raised on the mechanisms of action of calcitriol and its analogs in various diseases, as well as on possible methods of delivery and targeting.