Mifepristone (RU486): a review.
OBJECTIVE
To review the literature concerning the mechanism of action and pharmacodynamics of mifepristone (RU486), potential new uses of RU486, and its current use not only as an abortifacient but also as therapy for endometriosis, leiomyoma, breast cancer, and meningioma.


METHODS
Studies that relate to RU486 were identified through a MEDLINE search.


CONCLUSIONS
RU486 is an 11 beta-dimethyl-amino-phenyl derivative of norethindrone with a high affinity for P and glucocorticoid receptors. The receptor binding is not followed by transcription of P-dependent genes. Mifepristone effectively blocks P receptors in the placenta, resulting in the termination of pregnancy. In addition, it has been used in the treatment of leiomyomata, endometriosis, advanced breast cancer, and meningioma. It is a powerful tool to study the molecular action of P and in the future may be used as an estrogen-free contraceptive.
Mahajan
D K
DK
Department of Obstetrics and Gynecology, Louisiana State University School of Medicine, Shreveport 71130, USA. DMAHAJ@LSUMC.EDU
London
S N
SN
D000021:Abortifacient Agents, Steroidal / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D000028:Abortion, Induced / Q000379:methods*; D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D003280:Contraceptives, Oral, Synthetic / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D003283:Contraceptives, Postcoital, Synthetic / Q000493:pharmacokinetics / Q000494:pharmacology; D004715:Endometriosis / Q000188:drug therapy; D005260:Female; D006801:Humans; D007889:Leiomyoma / Q000188:drug therapy; D015735:Mifepristone / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D011247:Pregnancy; D014594:Uterine Neoplasms / Q000188:drug therapy
D000021:Abortifacient Agents, Steroidal; D003280:Contraceptives, Oral, Synthetic; D003283:Contraceptives, Postcoital, Synthetic; D015735:Mifepristone