PF-02413873 (PF-2413873) is a potent, selective, fully competitive, and orally active progesterone receptor (PR) antagonist with Ki of 9.7 nM.
PF-02413873 displays >30-fold selectivity over other homologous nuclear hormone receptors, GR, AR, and MR.
PF-02413873 blocks the follicular phase increase in endometrial thickness, the midcycle lutenizing hormone surge, and elevation in estradiol in a dose-dependent fashion compared with placebo in clinical trials.
