Toripristone Explained

Toripristone (INN; developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.^{[1] [2]} It is reported as a potent and highly selective antagonist of the glucocorticoid receptor (GR) (K_i = 2.4 nM),^{[3] [4]} though it also acts as an antagonist of the progesterone receptor (PR).^{[5] [6]} The pharmacological profile of toripristone is said to be very similar to that of mifepristone, except that toripristone does not bind to orosomucoid (α1-acid glycoprotein). The drug has been used to study the hypothalamic-pituitary-adrenal axis and has been used as a radiotracer for the GR. Its INN was given in 1990.

See also

• Aglepristone
• Lilopristone
• Onapristone
• Telapristone

Notes and References

1. Book: Hill RA, Makin HL, Kirk DN, Murphy GM . Toripristone . Dictionary of Steroids . https://books.google.com/books?id=AI7EnUyeEtUC&pg=PA101 . 23 May 1991 . CRC Press . 978-0-412-27060-4 . 101–.
2. International Nonproprietary Names for Pharmaceutical Substances . WHO Drug Information . 3 . 2 . 18 . 1989. https://web.archive.org/web/20160304035111/https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf . 4 March 2016.
3. Steiniger B, Kniess T, Bergmann R, Pietzsch J, Wuest FR . Radiolabeled glucocorticoids as molecular probes for imaging brain glucocorticoid receptors by means of positron emission tomography (PET) . Mini Reviews in Medicinal Chemistry . 8 . 7 . 728–739 . June 2008 . 18537728 . 10.2174/138955708784567403 .
4. Bachmann CG, Linthorst AC, Holsboer F, Reul JM . Effect of chronic administration of selective glucocorticoid receptor antagonists on the rat hypothalamic-pituitary-adrenocortical axis . Neuropsychopharmacology . 28 . 6 . 1056–1067 . June 2003 . 12700716 . 10.1038/sj.npp.1300158 . free .
5. Book: Philibert D, Costerousse G, Gaillard-Moguilewsky M, Nedelec L, Nique F, Tournemine C, Teutsch G . Antihormones in Health and Disease. From RU 38486 towards Dissociated Antiglucocorticoid and Antiprogesterone. Frontiers of Hormone Research. 19. 1991. 1–17. 0301-3073. 10.1159/000419634. 978-3-8055-5297-4.
6. Fu J, Hu L, Huang W, Zhu H, Wang Q, He F, Xie L, Gan, Huang W . Huang W . Cochrane Database of Systematic Reviews. Progesterone receptor antagonists and progesterone receptor modulators for endometriosis . 10.1002/14651858.CD009881 . 2012 . 5 . CD009881 .