Literature DB >> 9418681

Mifepristone (RU486): a review.

D K Mahajan1, S N London.   

Abstract

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. DATA IDENTIFICATION AND SELECTION: Studies that relate to RU486 were identified through a MEDLINE search. CONCLUSION(S): 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.

Entities:  

Keywords:  Abortion, Drug Induced; Abortion, Induced; Biology; Breast Cancer; Cancer; Contraception; Contraceptive Agents; Contraceptive Agents, Female; Contraceptive Agents, Postcoital; Diseases; Endocrine System; Endometrium; Family Planning; Fertility Control, Postconception; Fibroids; Genitalia; Genitalia, Female; Hormone Antagonists; Hormones; Literature Review; Neoplasms; Neoplasms, Benign; Physiology; Ru-486; Treatment; Urogenital System; Uterus

Mesh:

Substances:

Year:  1997        PMID: 9418681     DOI: 10.1016/s0015-0282(97)00189-1

Source DB:  PubMed          Journal:  Fertil Steril        ISSN: 0015-0282            Impact factor:   7.329


  24 in total

1.  Glucocorticoid receptor antagonist sensitizes TRAIL-induced apoptosis in renal carcinoma cells through up-regulation of DR5 and down-regulation of c-FLIP(L) and Bcl-2.

Authors:  Kyoung-Jin Min; Ji Hoon Jang; Jung Tae Lee; Kyeong Sook Choi; Taeg Kyu Kwon
Journal:  J Mol Med (Berl)       Date:  2011-10-19       Impact factor: 4.599

Review 2.  How were new medicines discovered?

Authors:  David C Swinney; Jason Anthony
Journal:  Nat Rev Drug Discov       Date:  2011-06-24       Impact factor: 84.694

3.  Mechanism of glucocorticoid regulation of the intestinal tight junction barrier.

Authors:  Michel A Boivin; Dongmei Ye; John C Kennedy; Rana Al-Sadi; Chris Shepela; Thomas Y Ma
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2006-10-26       Impact factor: 4.052

4.  Mifepristone (RU486), a pure antiprogesterone drug, in combination with vinblastine for the treatment of progesterone receptor-positive desmoid tumor.

Authors:  A Halevy; I Samuk; Z Halpern; L Copel; J Sandbank; Y Ziv
Journal:  Tech Coloproctol       Date:  2010-06-29       Impact factor: 3.781

5.  Mifepristone in the central nucleus of the amygdala reduces yohimbine stress-induced reinstatement of ethanol-seeking.

Authors:  Jeffrey A Simms; Carolina L Haass-Koffler; Jade Bito-Onon; Rui Li; Selena E Bartlett
Journal:  Neuropsychopharmacology       Date:  2011-11-02       Impact factor: 7.853

6.  The steroid RU486 induces UCP1 expression in brown adipocytes.

Authors:  Ana M Rodríguez; Andreu Palou
Journal:  Pflugers Arch       Date:  2004-08-27       Impact factor: 3.657

7.  TNF-α signals through PKCζ/NF-κB to alter the tight junction complex and increase retinal endothelial cell permeability.

Authors:  Célia A Aveleira; Cheng-Mao Lin; Steven F Abcouwer; António F Ambrósio; David A Antonetti
Journal:  Diabetes       Date:  2010-08-06       Impact factor: 9.461

8.  Inhibition of NF-κB activity by HIV-1 Vpr is dependent on Vpr binding protein.

Authors:  Michael Kogan; Satish Deshmane; Bassel E Sawaya; Edward J Gracely; Kamel Khalili; Jay Rappaport
Journal:  J Cell Physiol       Date:  2013-04       Impact factor: 6.384

9.  Glucocorticoids induce transactivation of tight junction genes occludin and claudin-5 in retinal endothelial cells via a novel cis-element.

Authors:  Edward A Felinski; Amy E Cox; Brett E Phillips; David A Antonetti
Journal:  Exp Eye Res       Date:  2008-01-12       Impact factor: 3.467

10.  Effects of mifepristone on invasive and metastatic potential of human gastric adenocarcinoma cell line MKN-45 in vitro and in vivo.

Authors:  Da-Qiang Li; Zhi-Biao Wang; Jin Bai; Jie Zhao; Yuan Wang; Kai Hu; Yong-Hong Du
Journal:  World J Gastroenterol       Date:  2004-06-15       Impact factor: 5.742

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