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Advances in Steroid Biochemistry and Pharmacology. 1979; 7:1-8.Due to the numerous adverse side effects of steroidal contraceptives which continuously arise and result in potential decreases in the benefit-to-risk ratio, new chemical and biologic strategies need to be designed and implemented to assure continued success in the contraceptive area. Novel contraceptive stragegies include both new chemical classes and their receptive biologic targets. 4 basic pharmacologic approaches subserve female contraception: inhibition of ovulation; inhibition of fertilization; inhibition of implantation; and interruption of established implantation. Many diverse compounds have been evaluated in regard to a male contraceptive, but problems of toxicity and loss of libido have made the search difficult. The problem is further complicated by the task of trying to eliminate the hundreds of millions of sperm that are constantly being produced and which are in different stages of the spermatogenic cycle. This task calls for chronic dosing and the accompanying problem of eventual liver involvement and hypertrophy of the secondary accessory sex organs. An interesting area supported by the World Health Organization is the identification of plants and the isolation of their active principles for fertility regulating purposes. The United States National Institute of Health supports 3 major and separate programs related to contraception: 1) synthesis and testing of anti-ovulatory agents; 2) synthesis and testing of male contraceptive agents; and 3) peptide antagonists of LH-RH (luteinizing hormone-releasing hormone) as ovulation inhibitors. The following categories represent areas of research that might prove fruitful: LH-RH agonists; LH-RH antagonists; non-natural synthetic products; inhibin; and plant extracts. These categories are reviewed.