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Dimethisterone is a **synthetic progestin (progestogen)**, formerly used orally as a component of birth control pills and for the treatment of gynecological disorders[1][4][3][5]. It acts as an **agonist of the progesterone receptor** (PR), with well-marked progestational properties and negligible androgenic or estrogenic activity, and some minor antimineralocorticoid activity[1][4][3]. Dimethisterone was introduced in the 1950s by British Drug Houses and became marketed primarily under the brand names Lutagan and Secrosteron, as well as in combination products with ethinylestradiol (for contraception). Despite increased potency compared to ethisterone, dimethisterone was one of the weakest oral progestogens known and was eventually discontinued, primarily due to a failure to adequately mitigate estrogen-induced endometrial cancer risk in combination formulations[1][4]. Mechanistically, it does not demonstrate important activity at other hormone receptors[1][4][3][5].
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