Drug intelligence / Profile preview

calcitriol

Development stage
Approved
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Topical
01

Overview

Calcitriol is the hormonally active form of vitamin D3 and is classified as a vitamin D analog. It is primarily used to treat and prevent low levels of calcium (hypocalcemia) and bone disease in patients with chronic kidney disease or parathyroid disorders. Calcitriol acts by binding to the vitamin D receptor (VDR), a nuclear receptor that regulates gene transcription. This interaction increases intestinal absorption of calcium and phosphate, enhances renal tubular reabsorption of calcium, stimulates release of calcium from bone via osteoblast-mediated activation of osteoclasts (through RANKL), and suppresses parathyroid hormone (PTH) synthesis by direct genomic effects in parathyroid cells[1][5][6]. Calcitriol also has immunomodulatory and anti-proliferative properties[3]. It is indicated for secondary hyperparathyroidism in chronic kidney disease patients not on dialysis or on dialysis; hypoparathyroidism; metabolic bone diseases associated with renal failure; and other conditions involving abnormal calcium metabolism[1][4][7].

Brand names
RocaltrolCalcijexVectical
Other names
1,25-dihydroxyvitamin D31,25(OH)2D3active vitamin D3
02

Targets

VDR (Vitamin D receptor)

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