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Calcitriol is the most active form of Vitamin D that exists as a small lipophilic molecule with superior cellular penetration. Calcitriol binds to intracellular vitamin D receptor (VDR) in most cells in the body by functioning both as a paracrine and an autocrine agent. Calcitriol plays an important role in mineral homeostasis and bone growth by promoting the export of calcium from bone, absorption of calcium from the gastrointestinal tract and the stimulation of the absorption of phosphate and magnesium ions to support mineralization. Calcitriol has potent effects on factors involved in growth and differentiation of many types of cancer cells, as well as cell adhesion and apoptosis. This could be largely due to its role in regulating the cell cycle and number of genes that are implicated in cancer initiation. Calcitriol has been shown to exhibit anti-proliferative, pro-differentiating, pro-apoptotic and anti-inflammatory actions in a variety of cancer cells in vitro including prostate cancer cells. 

Calcitriol is used for preclinical studies and research. Many preclinical studies have demonstrated that  exposure to high calcitriol concentrations can result in inhibition of prostate cancer cell growth in vitro and retardation or slow-down tumor growth in animal models of prostate cancer. Recent studies have suggested that calcitriol-induced increased absorption of phosphate from the intestine might also be involved in the increase of fibroblast growth factor-23 (FGF23).

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