Ulipristal acetate is a selective modulator ofprogesterone receptor and can be used to treat uterine myoma.
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Progesterone is a sex hormone that plays an important role in the pathogenesis of uterine leiomyomas. Ulipristal acetate is an orally active, selective progesterone receptor modulator that can stimulate autophagic response and upregulate Atg7 protein expression in leiomyoma cells at a concentration of 5µM (96 hours)[3]. The EC50 values of ulipristal acetate for recombinant human progesterone receptor-B, recombinant human progesterone receptor-A, rabbit uterine progesterone receptor, and rabbit thymic glucocorticoid receptor were 7.7±0.5, 8.5±0.6, 13.6±0.6, and 15.4±1.3nM, respectively[4]. In Sprague-Dawley rats, treatment with ulipristal acetate (1, 3, or 10mg/kg/day) decreased incidences of fibroadenomas and adenocarcinomas in the mammary gland[5].
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