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Doxercalciferol, the active ingredient in Hectorol (doxercalciferol injection) , is a synthetic vitamin D₂ analog that undergoes metabolic activation in vivo to form 1α,25-dihydroxyvitamin D₂ (1α,25-(0H)₂D₂), a naturally occurring, biologically active form of vitamin D₂. Hectorol (doxercalciferol injection) is available as a sterile, clear, colorless aqueous solution for intravenous injection. Mectorol Injection is supplied as either 4 mcg/2mL or 2 mcg/mL each in a stoppered, single use 2 mL amber glass vial, with an aluminum seal and yellow (4 mcg/2mL) or green (2 mcg/mL) flip-off cap. Each milliliter (mL) of solution contains doxercalciferol, 2 meg; ethanol, 100%, 0.05 mL; Polysorbate 20,10 mg; sodium chloride, 1.5 mg; butylated hydroxytoluene, 0.02 mg; sodium phosphate dibasic, heptahydrate, 14.4 mg; sodium phosphate monobasic, monohydrate, 1.8 mg; and disodium edetate, 1.1 mg.

Doxercalciferol is a colorless crystalline compound with a calculated molecular weight of 412.66 and a molecular formula of C28H44O2. It is soluble in oils and organic solvents, but is relatively insoluble in water. Chemically, doxercalciferol is (1α,3β,5Z,7E,22E)-9,10-secoergosta-5,7,10(19),22-tetraene-1,3-diol and has the structural formula presented in Figure 1.

Figure 1: Chemical Structure of Doxercalciferol

Other names frequently used for doxercalciferol are 1a-hydroxyvitamin D₂,1a-0H-D₂, and 1a-hydroxy-ergocalciferol.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.