2008/01/01 by Herjan J.T. Coelingh Bennink, Christian F. Holinka, E. Diczfalusy · 5 citations
Biochemistry, Genetics and Molecular Biology · Medicine · #Estrogen and related hormone effects #Pregnancy and Medication Impact #Inflammatory mediators and NSAID effects
paper · doi:10.1080/13697130802073425
openalex publication_date 2008/01/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/15
In this review paper, the existing information on the human fetal steroid estetrol (E4) has been summarized. In the past, E4 was considered as a weak estrogen and interest disappeared. However, recent new research has demonstrated that E4 is a potent, orally bioavailable, natural human fetal selective estrogen receptor modulator, since it acts in the rat as an estrogen on all tissues investigated except breast tumor tissue, where it has estrogen antagonistic properties in the presence of estradiol. Based on its safety data, its pharmacokinetic properties, its pharmacological profile and the results of first human studies, E4 may be suitable as a potential drug for human use in applications such as hormone replacement therapy (vaginal atrophy, hot flushes), contraception and osteoporosis. Additional areas worth exploring are the treatment of breast and prostate cancer, hypoactive sexual desire disorder and topical use (wrinkles) in women, auto-immune diseases, migraine, cardiovascular applications and the treatment of selected obstetric disorders.