The Antiprogestin Steroid RU 486 and Human Fertility Control

Book excerpt: Advances in basic biological research have proceeded rapidly in recent years. The fields of molecular genetics and immunology have experienced dramatic breakthroughs, capturing the imagination of both the scientific community and the general public. With less public notice, receptor biology has brought a cascade of new discoveries and insights. The entire science of pharmacology has been virtually rewritten in terms of receptor phenomenology. In particular, the discovery of specific receptors for steroid and protein hormones has been of seminal importance. With this new information, we have advanced our understanding of the mechanism and specifity of hormone action. We can now explain how hormones interact selectively with specific target cells and how hormones alter biochemical events within the target cells. These facts have already impacted on applied problems of clinical medicine, particularly in diagnosis and treatment of cancer and some metabolic diseases. Now, a new and important application of basic receptor biology and chemistry looms ahead. Within a few short years since the discovery of the progesterone receptor, chemists have synthesized molecules with a greater affinity for the receptor than progesterone itself and which, while occupying the receptor, fail to trigger the events which transform a target cell from the unstimulated to the stimulated state. This is the basis of the competitive inhibitory action of the anti-progestational agent, synthesized by the chemists at Roussel Uc1af, Paris, and designated RU 486.