The initiation of studies starting the train of development of the hormonal contraceptives occurred over 100 years ago with animal studies which demonstrated that ovarian transplants and ovarian extracts were able to inhibit ovulation. Subsequent studies defi ned the endocrinology of the ovarian cycle and factors involved in ovulation. This was followed by a dramatic era of pharmaceutical chemistry during which the orally active estrogens and progestins were discovered. Early studies demonstrated that a combination of the steroids could produce an effective inhibition of ovulation and would serve as an acceptable contraceptive for women. Over the years dramatic changes have been made to these products such that the levels of both the estrogen and progestin components have been greatly lowered and a variety of new steroidal compounds (progestins) have been produced along the way to reduce adverse effects, probably imparting some pharmaceutical patent protection for the manufacturers. Most recently, the utilization of these same products formulated for nonoral administration has turned out to be a fine-tuning of the use of estrogen–progestin contraception for better utility and compliance. Hormonal contraceptives have been an important sociological discovery having a great impact on the sexual liberation of women, allowing reasonable family planning and initiating controversies along the way in politics, religion and clinical medicine. They have been the most thoroughly studied pharmaceutical agents in history and have brought tremendous benefi ts to mankind in their effective and, by all standards, relatively safe usage in many different clinical situations. They are currently used by millions of women around the world as the major form of contraception. Perhaps the most surprising aspect of such pharmaceutical agents to inhibit ovulation is that we now recognize a broad spectrum of noncontraceptive benefits which have extended the utility of these agents into many areas of women's health. This chapter briefl y discusses the development, utility and relationship of estrogen–progestin contraception to women's health.