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Chemical Compound Review

Onapristona     (8S,11R,13R,14S,17R)-11-(4...

Synonyms: Onapristone, Onapristonum, AC1NSKQR, SureCN8740, IVV-1001, ...
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Disease relevance of Onapristone


High impact information on Onapristone


Chemical compound and disease context of Onapristone


Biological context of Onapristone

  • Based on our previous experiences, a dose of 2.5 or 5 mg of onapristone was administered s.c. every third day during the menstrual cycle, because these dosages impair endometrial development without upsetting the normal gonadal endocrine profiles [14].
  • Treatment with either of the two doses (2.5 or 5 mg) of onapristone caused a significant (P < 0.05) down-regulation in the expression of LIF in the peri-implantation endometria [14].
  • CONCLUSIONS: This study demonstrates that low-dose onapristone treatment throughout the menstrual cycle prevents pregnancy without disturbing the menstrual cycle and ovulation in the majority of cycles [15].
  • Onapristone inhibited apoptosis [16].
  • The intrauterine pressure recording on day 43 after coitus revealed phasic, laborlike contractions in response to oxytocin in onapristone-treated animals, in contrast to tonic reactions in controls [17].

Anatomical context of Onapristone


Associations of Onapristone with other chemical compounds


Gene context of Onapristone


Analytical, diagnostic and therapeutic context of Onapristone


  1. Onapristone, a progesterone receptor antagonist, as first-line therapy in primary breast cancer. Robertson, J.F., Willsher, P.C., Winterbottom, L., Blamey, R.W., Thorpe, S. Eur. J. Cancer (1999) [Pubmed]
  2. The effect of onapristone, a progesterone antagonist, on the growth of human gastrointestinal cancer xenografts. Jacobs, E., Watson, S.A., Ellis, I.O., Hardcastle, J.D., Robertson, J.F. Eur. J. Cancer (1997) [Pubmed]
  3. Induction of TGF-beta by an antiprogestin in the human breast cancer cell line T-47D. Dannecker, C., Possinger, K., Classen, S. Ann. Oncol. (1996) [Pubmed]
  4. Uterine activity during pregnancy and labor assessed by simultaneous recordings from the myometrium and abdominal surface in the rat. Buhimschi, C., Boyle, M.B., Saade, G.R., Garfield, R.E. Am. J. Obstet. Gynecol. (1998) [Pubmed]
  5. Effects of the progesterone antagonists onapristone (ZK 98 299) and ZK 136 799 on surgically induced endometriosis in intact rats. Stoeckemann, K., Hegele-Hartung, C., Chwalisz, K. Hum. Reprod. (1995) [Pubmed]
  6. Antiprogesterone therapy uncouples axonal loss from demyelination in a transgenic rat model of CMT1A neuropathy. Meyer Zu Horste, G., Prukop, T., Liebetanz, D., Mobius, W., Nave, K.A., Sereda, M.W. Ann. Neurol. (2007) [Pubmed]
  7. Progesterone exposure prevents matrix metalloproteinase-3 (MMP-3) stimulation by interleukin-1alpha in human endometrial stromal cells. Keller, N.R., Sierra-Rivera, E., Eisenberg, E., Osteen, K.G. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  8. Steroid regulation of prostaglandin dehydrogenase activity and expression in human term placenta and chorio-decidua in relation to labor. Patel, F.A., Clifton, V.L., Chwalisz, K., Challis, J.R. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  9. Progesterone regulation of heparin-binding epidermal growth factor-like growth factor gene expression during sensitization and decidualization in the rat uterus: effects of the antiprogestin, ZK 98.299. Zhang, Z., Funk, C., Glasser, S.R., Mulholland, J. Endocrinology (1994) [Pubmed]
  10. Luteal control of endometrial receptivity and its modification by progesterone antagonists. Hegele-Hartung, C., Mootz, U., Beier, H.M. Endocrinology (1992) [Pubmed]
  11. The tumour-inhibiting potential of the progesterone antagonist Onapristone in the human mammary carcinoma T61 in nude mice. Schneider, M.R., Michna, H., Habenicht, U.F., Nishino, Y., Grill, H.J., Pollow, K. J. Cancer Res. Clin. Oncol. (1992) [Pubmed]
  12. Preterm birth in rats produced by the synergistic action of a nitric oxide inhibitor (NG-nitro-L-arginine methyl ester) and an antiprogestin (onapristone). Yallampalli, C., Buhimschi, I., Chwalisz, K., Garfield, R.E., Dong, Y.L. Am. J. Obstet. Gynecol. (1996) [Pubmed]
  13. Effect of antiprogestins and tamoxifen on growth inhibition of MCF-7 human breast cancer cells in nude mice. El Etreby, M.F., Liang, Y. Breast Cancer Res. Treat. (1998) [Pubmed]
  14. Expression profiles of endometrial leukemia inhibitory factor, transforming growth factor beta2 (TGFbeta2), and TGFbeta2 receptor in infertile bonnet monkeys. Sachdeva, G., Patil, V., Katkam, R.R., Manjramkar, D.D., Kholkute, S.D., Puri, C.P. Biol. Reprod. (2001) [Pubmed]
  15. Onapristone (ZK 98.299): a potential antiprogestin for endometrial contraception. Katkam, R.R., Gopalkrishnan, K., Chwalisz, K., Schillinger, E., Puri, C.P. Am. J. Obstet. Gynecol. (1995) [Pubmed]
  16. Proliferation and apoptosis of fibroblasts and smooth muscle cells in rat uterine cervix throughout gestation and the effect of the antiprogesterone onapristone. Leppert, P.C. Am. J. Obstet. Gynecol. (1998) [Pubmed]
  17. The progesterone antagonist onapristone increases the effectiveness of oxytocin to produce delivery without changing the myometrial oxytocin receptor concentrations. Chwalisz, K., Fahrenholz, F., Hackenberg, M., Garfield, R., Elger, W. Am. J. Obstet. Gynecol. (1991) [Pubmed]
  18. Inhibition of the estradiol-mediated endometrial gland formation by the antigestagen onapristone in rabbits: relationship to uterine estrogen receptors. Chwalisz, K., Hegele-Hartung, C., Fritzemeier, K.H., Beier, H.M., Elger, W. Endocrinology (1991) [Pubmed]
  19. Effects of an antiprogestin onapristone on the endometrium of bonnet monkeys: morphometric and ultrastructural studies. Gopalkrishnan, K., Katkam, R.R., Sachdeva, G., Kholkute, S.D., Padwal, V., Puri, C.P. Biol. Reprod. (2003) [Pubmed]
  20. Influence of estradiol and progesterone withdrawal on the secretion of and the temporal correlation between pulses of oxytocin and prostaglandin F2(alpha) in ewes. Walker, D.L., Weston, P.G., Hixon, J.E. Biol. Reprod. (1997) [Pubmed]
  21. Decreased progesterone levels and progesterone receptor antagonists promote apoptotic cell death in bovine luteal cells. Rueda, B.R., Hendry, I.R., Hendry III, W.J., Stormshak, F., Slayden, O.D., Davis, J.S. Biol. Reprod. (2000) [Pubmed]
  22. Regulation of interleukin 8 production in the term human placenta during labor and by antigestagens. Elliott, C.L., Kelly, R.W., Critchley, H.O., Riley, S.C., Calder, A.A. Am. J. Obstet. Gynecol. (1998) [Pubmed]
  23. Synergistic role of nitric oxide and progesterone during the establishment of pregnancy in the rat. Chwalisz, K., Winterhager, E., Thienel, T., Garfield, R.E. Hum. Reprod. (1999) [Pubmed]
  24. Early and delayed effects of hydrocortisone and onapristone on intestinal brush-border enzymes and their sialylation and on thymus growth in suckling rats. Kraml, J., Kolínská, J., Kadlecová, L., Zákostelecká, M., Hirsová, D., Schreiber, V. J. Steroid Biochem. Mol. Biol. (1995) [Pubmed]
  25. Non-genomic effects of progestins--inhibition of cell growth and increased intracellular levels of cyclic nucleotides. Sager, G., Ørbo, A., Jaeger, R., Engström, C. J. Steroid Biochem. Mol. Biol. (2003) [Pubmed]
  26. Hormonal regulation of connexin-43 in baboon corpora lutea. Khan-Dawood, F.S., Yang, J., Dawood, M.Y. J. Endocrinol. (1998) [Pubmed]
  27. Expression of MAPkinases (Erk1/2) during decidualization in the rat: regulation by progesterone and nitric oxide. Thienel, T., Chwalisz, K., Winterhager, E. Mol. Hum. Reprod. (2002) [Pubmed]
  28. Cervical dilatation: induction by antigestagens via adhesion molecules. An in vitro examination in endothelial cell cultures. Kemp, B., Winkler, M., Hauptmann, S., Rath, W. Gynecol. Obstet. Invest. (1998) [Pubmed]
  29. Effects of progesterone on iNOS, COX-2, and collagen expression in the cervix. Marx, S.G., Wentz, M.J., Mackay, L.B., Schlembach, D., Maul, H., Fittkow, C., Given, R., Vedernikov, Y., Saade, G.R., Garfield, R.E. J. Histochem. Cytochem. (2006) [Pubmed]
  30. Expression of regulator of G protein signaling-2 in rat myometrium during pregnancy and parturition. Suarez, V.R., Park, E.S., Hankins, G.D., Soloff, M.S. Am. J. Obstet. Gynecol. (2003) [Pubmed]
  31. The effects of post-ovulatory administration of onapristone on the developmnent of a secretory endometrium. Cameron, S.T., Critchley, H.O., Buckley, C.H., Chard, T., Kelly, R.W., Baird, D.T. Hum. Reprod. (1996) [Pubmed]
  32. Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore. Pooley, C.L., Edwards, J.P., Goldman, M.E., Wang, M.W., Marschke, K.B., Crombie, D.L., Jones, T.K. J. Med. Chem. (1998) [Pubmed]
  33. Cervical ripening with the cytokines interleukin 8, interleukin 1 beta and tumour necrosis factor alpha in guinea-pigs. Chwalisz, K., Benson, M., Scholz, P., Daum, J., Beier, H.M., Hegele-Hartung, C. Hum. Reprod. (1994) [Pubmed]
  34. Modulation of endometrial transformation in gonadotrophin-stimulated and unstimulated pseudo-pregnant rabbits: studies with the progesterone receptor antagonist, onapristone. Krusche, C.A., Herrler, A., Classen-Linke, I., Hegele-Hartung, C., von Rango, U., Beier, H.M. Mol. Hum. Reprod. (2000) [Pubmed]
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