2010 年 68 巻 9 号 p. 904-910
In vitamin D research, there have been three milestones from the perspective of pharmaceutical studies. The first was the early stages of vitamin D research and involved the discovery of vitamin D and its physiological significance as an anti-rickets factor. The second was the elucidation of the vitamin D activation pathway in the body and the discovery of biologically active metabolites. The third has been characterized by the discovery of the differentiation-inducing properties of active vitamin D. This indicated the diversity of the physiological actions of active vitamin D, which initially had been thought only to contribute to bone and calcium metabolism. Because these physiological actions were clinically useful, the third discovery revealed opportunities for the development of drugs appropriate to specific purposes by synthesizing derivatives to separate biological effects. Six active vitamin D derivatives (maxacalcitol, calcipotriol, tacalcitol, paricalcitol, doxercalciferol, and falecalcitriol) based on the findings during the third milestone are now commercially available and contributing to current clinical practice. This article discusses the various milestones outlining vitamin D and derivatives in terms of pharmaceutical studies and practical syntheses of the six derivatives developed during the third milestone.