Orally active progestins like nomegestrol acetate reproduce progesterone action on its target organs. This 19-norprogesterone derivative possesses a high anti-estrogenic action which is mediated by progesterone receptors (PgR). The interaction of nomegestrol acetate with PgR has been studied in rat uterus as well as in human endometrium and mammary gland. Results show high relative binding affinities for nomegestrol acetate especially for the PgR in mammary tissue and pointed out a species-related specificity as well as some organ-related differences in progesterone binding sites.