Doxercalciferol is a synthetic vitamin D2 analog introduced in the US as
Hectorol for the treatment of secondary hyperparathyroidism (SHPT) in patients
with end-stage renal failure. It is actually 1-alpha-hydroxyvitamin D2 (one-alpha-
D2) and can be synthesized by direct hydroxylation of vitamin D2 tosylate or in
5 steps from ergosterol. Doxercalciferol itself is inactive until metabolized by the
liver into active 1,24-dihydroxyvitamin D2, showing a pharmacokinetic profile
similar to calcitriol. During placebo-controlled clinical trials, patients with
moderate to severe SHPT were treated with 1-alpha-D2 (10 μg doses) for 16 to
24 weeks; in 9 patients out of 10, blood levels of parathyroid hormone were
considerably reduced, so maintaining a good control of the parathyroid
hyperplasia. Moreover, only a moderate tendency to raise calcium and
phosphate was observed. Doxercalciferol is orally-active and less toxic than
other vitamin D analogs like alfacalcidol; it shows differentially controlled effects
and has an improved safety profile compared to calcitriol.
화학적 성질
Doxercalciferol is Crystalline Solid
용도
Synthetic vitamin D prohormone. A new active Vitamin D analog which inhibits growth of human neuroblastoma.
Antihyperparathyroid
생물학적 활성
Vitamin D 2 analog that acts as a vitamin D receptor activator (VDRA).
