Profile of estetrol, a promising native estrogen for oral contraception and the relief of climacteric symptoms of menopause
Published in Expert Review of Clinical Pharmacology, 2022
Céline Gérard, Jean-François Arnal, Maud Jost, Jonathan Douxfils, Françoise Lenfant, Coralie Fontaine, René Houtman, David F. Archer, Robert L. Reid, Rogerio A. Lobo, Ulysse Gaspard, Herjan J.T. Coelingh Bennink, Mitchell D. Creinin, Jean-Michel Foidart
Estrogens were first synthesized in the laboratory almost 100 years ago with purification of E1 in 1929 and the discovery of E2 in 1931 and E3 in 1933. Within 5 years of their discovery, E1, E2, and E3 were introduced as potential therapeutic agents. Ethinyl estradiol (EE) was the first synthetic estrogen, produced in 1938, and marketed in 1943 for the treatment of dysmenorrhea [6]. Conjugated equine estrogens (CEEs), a mixture of estrogen conjugates found in the urine of mares, were introduced in 1941 for the relief of hot flushes in postmenopausal women. Since then, no new natural estrogens have been characterized and evaluated for the benefit of women’s health for over 80 years.