Estradiol prodrugs (EP) for efficient oral estrogen treatment and abolished effects on estrogen modulated liver functions

详细信息    查看全文

• 作者：W. Elger^a ; R. Wyrwa^d ; G. Ahmed^a ; F. Meece^a ; H.B. Nair^a ; B. Santhamma^a ; Z. Killeen^e ; B. Schneider^a ; R. Meister^c ; H. Schubert^b ; K. Nickisch^a ; ^{knickisch@evestra.com} ; ^{klausnickisch@aol.com}
• 关键词：AUC ; area under the curve ; BW ; body weight ; C0 ; extrapolated concentration time zero (i. v.) ; Cmax ; maximum concentration ; CA-II ; carbonic anhydrase II ; CBG ; cortisol binding globulin ; COC ; combined oral contraceptive ; EDTA ; ethylene diamine tetra acetic acid ; EE ; ethinyl estradiol ; EMATE ; estrone sulfamate ; EP ; estradiol prodrug ; ER ; estrogen receptor ; ERT ; estrogen replacement therapy ; ES ; estradiol sulfamate ; E2 ; estradiol ; FSH ; follicle stimulating hormone ; GH-/IGF1 ; growth hormone / insulin
• 刊名：The Journal of Steroid Biochemistry and Molecular Biology
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：165
• 期：part_PB
• 页码：305-311
• 全文大小：920 K
• 卷排序：165

文摘

Sulfonamide esters of estradiol may technically improve oral estrogen therapy. CA-II-mediated binding by erythrocytes avoids metabolism during hepatic clearance. Systemic hydrolysis improves the bioavailability of estradiol. E2 prodrug-based COC may reduce thromboembolic events.