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Tanaproget is a novel agonist of progesterone receptor with IC50 of 1.7 nM [1].

Progesterone receptor (PR) is a member of the nuclear receptor superfamily and binding of progesterone causes PR conformational changes, which then changing gene expression. Progesterone plays an important role in female reproduction [1].

In T47D cells, tanaproget caused alkaline phosphatase activity with EC50 value of 0.1 nM. In a mammalian two-hybrid assay, tanaproget showed  50-fold more potent than progesterone. In stromal cells isolated from endometrial, tanaproget (1 nM) significantly suppressed pro-MMP-3 secretion. Also, Tanaproget effectively prevented pro-MMP-3 secretion through IL-1α-mediated stimulation [2].

In endometriosis mice model with human lesions growing on the parietal peritoneum of mice, tanaproget completely regressed human lesions in 58% treated animals. Also, the lesions were smaller and fewer compared with the lesions in placebo-treated mice at the end of therapy [2]. In healthy women, the elimination half-life (t(1/2)) of tanaproget ranged from 12 to 30 h. Tanaproget reduced cervical mucus scores, which suggesting poor production and quality of cervical mucus [3].

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