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Gestodene is a progestin.1 It selectively binds to the progesterone receptor over the estrogen receptor.2 Gestodene induces transcriptional activity mediated by the progesterone receptor, and, weakly, the androgen receptor in reporter assays.3 It increases the growth of MCF-7 cells when used at concentrations ranging from 0.1 to 1 µM.4 In contrast, gestodene (0.1 mg/kg) reduces tumor growth in an estrogen-dependent model of rat mammary tumors induced by DMBA (Item No. 30383). Formulations containing gestodene, in combination with ethynyl estradiol have been used as oral contraceptives.
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