Drug intelligence / Profile preview

calcifediol

Development stage
Approved
Lead developer
OPKO Health
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Calcifediol is a synthetic vitamin D3 analog and the major circulating metabolite of cholecalciferol (vitamin D3). It is used primarily to treat secondary hyperparathyroidism in adults with stage 3 or 4 chronic kidney disease who have low serum total 25-hydroxyvitamin D levels. Calcifediol works by increasing intestinal absorption of calcium and phosphate and by regulating parathyroid hormone (PTH) synthesis and secretion. It acts as an agonist at the vitamin D receptor, which modulates gene expression involved in calcium homeostasis. After oral administration, calcifediol is further hydroxylated in the kidneys to form calcitriol (1,25-dihydroxycholecalciferol), the biologically active form of vitamin D[1][2][5][9].

Brand names
RayaldeeCalderol
Other names
25-hydroxyvitamin D325-hydroxycholecalciferolcalcidiol
02

Targets

VDR (Vitamin D receptor)

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