Newer, nonsteroidal, orally active, tissue-selective progestins are being d
eveloped through a molecular approach to compound selection with human prog
esterone receptor (hPR) serving as the molecular target. The co-transfectio
n and binding assays are used to test receptor selectivity and cross reacti
vity with a panel of receptors. Transcriptional products are used to furthe
r profile new progestin compounds. Desirable new progestins will suppress e
strogen-induced endometrial stimulation, show no or minimal proliferative a
ctivity, maintain pregnancy, inhibit ovulation, contain no androgenic, mine
ralocorticoid or glucocorticoid activity, and possess minimal adverse physi
ologic effects. Newer progestins that possess many of these desirable prope
rties are in development. (J Soc Gynecol Investig 2000;7:S53-4) Copyright (
C) 2000 by the Society for Gynecologic Investigation.