6847. Onapristone

Nomenclature

CAS number: 96346-61-1
(11β,13α,17α)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(3-hydroxypropyl)estra-4,9-dien-3-one; 11β-(4-dimethylaminophenyl)-17α-hydroxy-17β-(3-hydroxypropyl)-13α-methyl-4,9-gonadien-3-one; ZK-98299.
C29H39NO3; mol wt 449.62.
C 77.47%, H 8.74%, N 3.12%, O 10.68%.

Description and references

Progesterone receptor antagonist. Prepn: G. Neef et al., EP 129499; eidem, US 4780461 (1984, 1988 both to Schering AG); idem et al., Steroids 44, 349 (1984). HPLC determn in plasma and serum: C. Zurth, F. Kagels, J. Chromatogr. 532, 115 (1990). In vitro effect on breast cancer cells: S. Classen et al., J. Steroid Biochem. Mol. Biol. 45, 315 (1993). Mechanism of action study: D. P. Edwards et al., ibid. 53, 449 (1995). Clinical antifolliculotrophic effect: H. B. Croxatto et al., Hum. Reprod. 9, 1442 (1994).

Chemical structure

Properties

Amorphous glass. [α]D25 +446.2° (c = 0.51 in chloroform).

Therapeutic Category

Antiprogestin; antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); Antiprogestins; Antiprogestin