Clinical applications for estetrol.
In this paper the potential clinical applications for the human fetal estrogen estetrol (E(4)) are presented based on recently obtained data in preclinical and clinical studies. In the past E(4) has been classified as a weak estrogen due to its rather low estrogen receptor affinity. However, recent research has demonstrated that due to its favorable pharmacokinetic properties, especially the slow elimination and long half-life, E(4) is an effective orally bioavailable estrogen agonist with estrogen antagonistic effects on the breast in the presence of estradiol. Based on the pharmacokinetic properties, the pharmacological profile and the safety and efficacy results in human studies, E(4) seems potentially suitable as a drug for human use in applications such as hormone replacement therapy (vaginal atrophy and vasomotor symptoms), contraception, osteoporosis and breast cancer.
Visser
Monique
M
Pantarhei Bioscience, PO Box 464, 3700 AL Zeist, The Netherlands. mv@pantarheibio.com
Coelingh Bennink
Herjan J T
HJ
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D002986:Clinical Trials as Topic; D003271:Contraceptive Agents, Female; D004953:Estetrol / Q000627:therapeutic use; D005260:Female; D005333:Fetus / Q000378:metabolism; D020249:Hormone Replacement Therapy; D006801:Humans; D008593:Menopause / Q000502:physiology; D010024:Osteoporosis / Q000188:drug therapy; D011247:Pregnancy; D011960:Receptors, Estrogen / Q000378:metabolism; D014621:Vagina / Q000473:pathology
D003271:Contraceptive Agents, Female; D011960:Receptors, Estrogen; D004953:Estetrol