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Gestodene, also known as 17α-ethynyl-18-methyl-19-nor-δ 15 -testosterone , as well as 17α-ethynyl-18-methylestra-4,15-dien-17β-ol-3-one or 13β-ethyl-18,19-dinor-17α-pregna-4,15-dien-20-yn-17β-ol-3-one , is a synthetic estrane steroid and a derivative of testosterone . [2] [22] It is more specifically a derivative of norethisterone (17α-ethynyl-19-nortestosterone) and is a member of the gonane (18-methylestrane) subgroup of the 19-nortestosterone family of progestins. [23] Gestodene is almost identical to levonorgestrel in terms of chemical structure , differing only in having an additional double bond between the C15 and C16 positions, and for this reason is also known as δ 15 -norgestrel or as 15-dehydronorgestrel . [24] [25]

Tibolone has tissue -selective estrogenic effects, with desirable effects in bone , the brain , and the vagina , and lack of undesirable action in the endometrium and breasts . [14] Its tissue selectivity is the result of metabolism , enzyme modulation (., of estrogen sulfatase and estrogen sulfotransferase ), and receptor modulation that vary in different target tissues, and differs mechanistically from that of selective estrogen receptor modulators (SERMs) such as tamoxifen , which produce their tissue selectivity via means of modulation of the ER. [13] [14] As such, to distinguish it from SERMs, tibolone has been described as a "selective tissue estrogenic activity regulator" (STEAR), [14] and also as a "selective estrogen enzyme modulator" (SEEM). [15]

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