641. Anecortave Acetate

Nomenclature

CAS number: 7753-60-8
21-(Acetyloxy)-17-hydroxypregna-4,9(11)-diene-3,20-dione; Δ4,9(11)-pregnadien-17α,21-diol-3,20-dione-21-acetate; Al-3789; Retaane (Alcon ).
C23H30O5; mol wt 386.48.
C 71.48%, H 7.82%, O 20.70%.

Description and references

Angiostatic steroid. Prepn: J. Fried, E. F. Sabo, J. Am. Chem. Soc. 75, 2273 (1953); R. P. Graber et al., ibid. 4722; J. Fried, E. F. Sabo, ibid. 79, 1130 (1957). Angiostatic activity in vitro: L. G. McNatt et al., J. Ocul. Pharmacol. Ther. 15, 413 (1999); in vivo: D. BenEzra et al., Invest. Ophthalmol. Visual Sci. 38, 1954 (1997). Clinical study in age-related macular degeneration: J. S. Slakter et al., Ophthalmology 110, 2372 (2003). Review of pharmacology: A. F. Clark, Expert Opin. Invest. Drugs 6, 1867-1877 (1997); and clinical experience: S. A. Vinores, IDrugs 8, 327-334 (2005).

Chemical structure

Properties

Crystals from acetone, mp 236-237°. [α]D +117° (c = 1.0 in CHCl3). uv max (alcohol): 238 nm (ε 15500). Also reported as mp 231.5-234.5°. [α]D22 +124° (c = 1.04 in CHCl3).

Therapeutic Category

In treatment of macular degeneration.

Keywords

Macular Degeneration Treatment