HISTORY AND PERSPECTIVES OF ANTIPROGESTINS FROM THE CHEMISTS POINT-OF-VIEW

Citation
G. Teutsch et D. Philibert, HISTORY AND PERSPECTIVES OF ANTIPROGESTINS FROM THE CHEMISTS POINT-OF-VIEW, Human reproduction, 9, 1994, pp. 12-31
Citations number
88
Categorie Soggetti
Reproductive Biology
Journal title
ISSN journal
02681161
Volume
9
Year of publication
1994
Supplement
1
Pages
12 - 31
Database
ISI
SICI code
0268-1161(1994)9:<12:HAPOAF>2.0.ZU;2-R
Abstract
The discovery of RU486 and its potent activity as an antiglucocorticoi d and antiprogestin brought the long story on steroid hormones and ant ihormones to its logical conclusion. Even though scattered improvement s are still possible, the armamentarium of the steroid endocrinologist is by now complete. Like any successful drug, RU486 has become the pr ototype of a number of analogues which are claimed to be either more a ctive or more dissociated. The literature (mainly patents) has been se arched for available data on abortive activities, and some as yet unpu blished results on RU compounds have been included. It appears that a number of compounds are both more active than RU486 on a dose basis in animal studies and more dissociated in relation to a possible antiglu cocorticoid activity. In addition, hydrosoluble compounds suitable for i.v. injection are available for possible development. In a longer te rm perspective, it cannot be excluded that potential non-steroidal ant iprogestins could present additional advantages over steroidal compoun ds, in particular improved receptor specificity and/or reduced suscept ibility to receptor mutation.