The control of human fertility is not a modern quest, since it has been sought for millennia. In contrast to this, the search for hormonally induced temporary infertility started only in the early part of the twentieth century. In all probability, the pioneers who opened the road for this search were two scientists: W. Rübsamen from Germany and L. Haberlandt from Austria. By necessity, both could only use ovarian extracts. Further progress came with the isolation and subsequent characterization in the 1930s of reproductive steroid hormones. Since the natural hormones, estradiol and progesterone, are not active if given orally, the next step involved the synthesis of orally active steroids. In the 1950s, thanks to these compounds, G. Pincus and his group launched a series of animal and clinical trials giving birth to the hormonal pill. Initial tests were conducted with a progestin alone, until, thanks to a fortunate error, it was determined that both estrogen and the progestin were necessary. Today, thanks to major efforts by the pharmaceutical Industry, combined contraception benefits from a large number of products that can be administered orally, transdermally, vaginally, and as a monthly injectable. Hormonal contraceptives are designed for use by young, mostly healthy, women. For this reason, adverse effects have been closely scrutinized and a number of improvements, including lowering the dosage and introducing new molecules, have been made over time and will continue to be made in the foreseeable future.