Importance of the field: Since ethinyl estradiol is a potent activator of hepatic enzymes, the use of natural estradiol (E2) has been studied; but, until recently, bleeding control has hampered development of an E2 pill.
Areas covered in this review: A historical review of oral contraceptive development leading to the successful design of an estradiol pill. Pharmacology, mechanism of action and clinical trials of contraceptive efficacy and bleeding profile of the estradiol valerate/dienogest (E2V/DNG) pill are reviewed. Details of two placebo-controlled treatment trials of the E2V/DNG pill in women with heavy menstrual bleeding are discussed. All available literature was searched using pubMed and additional data were obtained from published abstracts.
What the reader will gain: Information on the novel features and indications for the E2V/DNG pill.
Take home message: The dynamic-dosing E2V/DNG oral contraceptive pill provides a highly effective contraceptive option with an adjusted Pearl Index (method failure) of 0.51 (upper limit of 95% CI 0.97) and unadjusted Pearl Index (user failure) of 1.01 (1.59) for women aged 18-35 years. In addition, two large randomized controlled trials have demonstrated that E2V/DNG provides effective treatment for women with heavy menstrual bleeding.