Lilopristone

Lilopristone (IUPAC name: 11β-[4-(Dimethylamino)phenyl]-17α-hydroxy-17β-(3-hydroxypropyl)-13α-[[1-methyl-2-(3,4,5-trimethoxyphenyl)ethylidene]-7,8-didehydro-4,5-epoxymorphinan-6-one) is a synthetic, steroidal antiprogestogen with additional antiglucocorticoid activity that was developed by Schering AG and described in the literature in 1984 but was never marketed.

Pharmacology

Lilopristone acts as a selective progesterone receptor antagonist (or blocker), with a high affinity for the progesterone receptor and no significant affinity for other steroid hormone receptors. It has been found to inhibit the endometrial effects of progesterone in animal studies. In addition to its antiprogestogenic activity, lilopristone has been found to possess antiglucocorticoid activity, and has been used in scientific research to study the role of glucocorticoids in various biological processes.

Chemistry

Lilopristone, also known as 11β-[4-(Dimethylamino)phenyl]-17α-hydroxy-17β-(3-hydroxypropyl)-13α-[[1-methyl-2-(3,4,5-trimethoxyphenyl)ethylidene]-7,8-didehydro-4,5-epoxymorphinan-6-one, is a synthetic steroidal compound of the 19-norprogesterone and 17α-hydroxyprogesterone groups. It is structurally related to other antiprogestogens such as mifepristone and onapristone.

History

Lilopristone was developed by the German pharmaceutical company Schering AG and was first described in the scientific literature in 1984. Despite its promising pharmacological profile, it was never marketed for medical use.

See also

• List of investigational sex-hormonal agents
• List of steroidal antiandrogens

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  Lilopristone