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Mifepristone (CAS: 84371-65-3)
Mifepristone (or RU-486) is a synthetic steroid compound with both antiprogesterone and antiglucocorticoid properties. The compound is a 19-nor steroid with substitutions at positions C11 and C17 (17 beta-hydroxy-11 beta-[4-dimethylamino phenyl] 17 alpha-[1-propynyl]estra-4,9-dien-3-one), which antagonizes cortisol action competitively at the receptor level.
Mifepristone is a progesterone receptor antagonist used as an abortifacient in the first months of pregnancy, and in smaller doses as an emergency contraceptive. Mifepristone is also a powerful glucocorticoid receptor antagonist, and has occasionally been used in refractory Cushing's Syndrome (due to ectopic/neoplastic ACTH/Cortisol secretion). During early trials, it was known as RU-38486 or simply RU-486, its designation at the Roussel Uclafcompany, which designed the drug. The drug was initially made available inFrance, and other countries then followed—often amid controversy. It is marketed under tradenames Korlym and Mifeprex, according to FDA Orange Book.
Mifepristone was the first antiprogestin to be developed and it has been evaluated extensively for its use as an abortifacient. The original target for the research group, however, was the discovery and development of compounds with antiglucocorticoid properties. It is these antiglucocorticoid properties that are of great interest in the treatment of severe mood disorders and psychosis. It is on the World Health Organization's List of Essential Medicines.
According to the current RCOG abortion evidence-based clinical guideline:
• All methods of first-trimester abortion carry a small risk of failure to terminate the pregnancy. The risk for surgical abortion is around 0.23% and for medical abortion between 0.1% and 1.4% (depending on the regimen used and the experience of the centre).
• Medical abortion using mifepristone plus prostaglandin is the most effective method of abortion at gestations of less than 7 weeks.
• Conventional vacuum aspiration below 7 weeks have a higher failure rate than at later gestations. Protocols should include examination of the aspirate for the presence of the gestational sac and/or follow-up serum human chorionic gonadotrophin estimation, to ensure abortion completion.
• Early vacuum aspiration using a rigorous protocol (which includes magnification of aspirated material and indications for serum βhCG follow-up) may be used at gestations below 7 weeks, although data suggest that the failure rate is higher than for medical abortion.
• Medical abortion using mifepristone plus prostaglandin continues to be an appropriate method for women in the 7–9 week gestation band.
Mifepristone is sold outside theUnited Statesby Exelgyn Laboratories as Mifegyne, made inFrance, and is approved for:
1. Medical termination of intrauterine pregnancies of up to 49 days gestation (up to 63 days gestation inBritainandSweden)
2. Softening and dilatation of the cervix prior to mechanical cervical dilatation for pregnancy termination
3. Use in combination with gemeprost for termination of pregnancies between 13 and 24 weeks gestation
4. Labor induction in fetal death in utero.
Mifepristone is sold in theUnited Statesby Danco Laboratories as Mifeprex, made inChina, and is U.S. Food and Drug Administration-approved to terminate intrauterine pregnancies of up to 49 days gestation. Under the FDA-approved regimen, a 600 mg dose is administered by a clinician following a counseling session. Two days later, a clinician administers 400 µg of another medicine, misoprostol, to induce contractions. In European studies, this method terminated 96 to 99% of pregnancies of up to 49 days gestation, but in one large multicenter trial in the United States conducted from September 1994 to September 1995, the efficacy was lower (92%), which the authors of the study suggested may have been due to lack of experience with this method in the United States and/or the design of their study. In Europe andChina, an observation period of several hours is required after administration of misoprostol. If expulsion of fetal tissue does not occur during the observation period, surgical abortion is offered. There is no required observation period in theUnited States, but it is strongly recommended.
Mifepristone can also be used in smaller doses as an emergency contraceptive; if taken after sex but before ovulation, it can prevent ovulation and so prevent pregnancy. In this role, a 10 mg dose is not as effective as the 600 mg dose, but has fewer side-effects. Mifeprex and Mifegyne are only available in 200 mg tablets.
A review of studies in humans found that the contraceptive effects of the 10 mg dose were probably due mainly to its effects on ovulation, and not inhibition of implantation, but "the knowledge of the mechanism of action remains incomplete". Treatment with 200 mg of mifepristone changes steroid receptor expression in the fallopian tube, inhibits endometrial development, and effectively prevents implantation.
Mifepristone is approved for use in theUnited Statesand the EU for the treatment of Cushing's Syndrome via a patented preparation manufactured by Corcept Therapeutics.
Other medical applications of mifepristone that have been studied in clinical trials include regular long-term use as an oral contraceptive, and treatment of HIV infection, uterine fibroids,endometriosis, major depression with psychotic features, post-traumatic stress disorder, bipolar depression and disorders causing cognitive dysfunction, post-traumatic stress disorder, chronic multisymptom illness, glaucoma, meningiomas, breast cancer, ovarian cancer, and prostate cancer.
Mifepristone showed no detectable anti-HIV activity in clinical trials.
Mifepristone showed initial promise in psychotic major depression, a form of depression that is difficult to treat, however a Phase III clinical trial was terminated early due to lack of efficacy.
Mifepristone treatment produced clinical improvement in PTSD symptoms in a small clinical trial published in 2012.
Use as a cervical ripening agent has also been described.
Category: Endocrine Drugs API