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Calcitriol was identified as the active form of vitamin D in 1971 and the drug was approved for medical use in the United States in 1978. [7] It is available as a generic medication. [12] In 2022, it was the 254th most commonly prescribed medication in the United States, with more than 1 million prescriptions.
Calcitriol plays a key role in regulating vitamin D levels through a negative feedback mechanism. [203] It strongly upregulates the expression of the enzyme CYP24A1 , which inactivates vitamin D. This activation happens through binding of the activated vitamin D receptor (VDR) to two vitamin D response elements (VDREs) in the in the CYP24A1 gene.
1α-Hydroxyvitamin D 5 is a chemical derivative of vitamin D 5.The motive to study 1α-hydroxyvitamin D 5 as a potential pharmaceutical drug stemmed from the tendency of calcitriol, a natural metabolite produced in the kidney, to cause toxic hypercalcemia in patients when dosed at concentrations needed to interrupt prostate cancer cells' cycle and stimulate apoptosis.
The natural, active form of vitamin D is calcitriol (1,25-dihydroxycholecalciferol). This molecule and other naturally occurring forms of vitamin D, including its precursors and metabolites, have been modified to synthesize pharmaceuticals with potentially greater, or selective, therapeutic actions. [1] [2] [3] [4]
The level of serum 1,25(OH)D (calcitriol) is not usually used to determine vitamin D status because it often is regulated by other hormones in the body such as parathyroid hormone. [53] The levels of 1,25(OH)D can remain normal even when a person may be vitamin D deficient. [53]
Calcipotriol, also known as calcipotriene, is a synthetic derivative of calcitriol, a form of vitamin D. It is used in the treatment of psoriasis. [1] It is safe for long-term application in psoriatic skin conditions. [medical citation needed] It was patented in 1985 and approved for medical use in 1991. [2]
The vitamin D receptor (VDR also known as the calcitriol receptor) is a member of the nuclear receptor family of transcription factors. [5] Calcitriol (the active form of vitamin D , 1,25-(OH) 2 vitamin D 3 ) binds to VDR, which then forms a heterodimer with the retinoid-X receptor .
Eldecalcitol is an analog of calcitriol, the active form of vitamin D. [1]Commonly used in Japan for the treatment of osteoporosis. [2] Osteoporosis is a common bone disease among the older generation, with an estimated prevalence of over 200 million people. [2]
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