3436. Doxercalciferol

Nomenclature

CAS number: 54573-75-0
(1α,3β,5Z,7E,22E)-9,10-Secoergosta-5,7,10(19),22-tetraene-1,3-diol; 1α-hydroxyvitamin D2; 1-hydroxyergocalciferol; Hectorol (Bone Care).
C28H44O2; mol wt 412.65.
C 81.50%, H 10.75%, O 7.75%.

Description and references

Synthetic vitamin D prohormone. Prepn: H.-Y. P. Lam et al., Science 186, 1038 (1974); eidem, Steroids 30, 671 (1977); H. E. Paaren et al., J. Org. Chem. 45, 3253 (1980). Comparative activity and toxicity: G. Sj"oden et al., Proc. Soc. Exp. Biol. Med. 178, 432 (1985). Metabolism to bioactive form: J. C. Knutson et al., Endocrinology 136, 4749 (1995). Pharmacology: J. W. Coburn et al., Nephrol. Dial. Transplant. 11, Suppl. 3, 153 (1996). Clinical trial for suppression of secondary hyperparathyroidism in hemodialysis: J. M. Frazao et al., ibid. 13, Suppl. 3, 68 (1998).

Chemical structure

Properties

Crystals, mp 138-140°. uv max (ethanol): 265 nm (ε 18300). LD50 orally in rats: 3.5-6.5 mg/kg (Sj"oden).

Therapeutic Category

Antihyperparathyroid.

Keywords

Antihyperparathyroid