PF-02413873

PF-02413873 is a potent, selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist. It blocks progesterone binding and PR nuclear translocation with high affinity (Ki of 2.6 nM), and inhibits endometrial growth in vivo. The drug was developed for the treatment of endometriosis and demonstrated efficacy in preclinical models by reducing endometrial thickness and proliferation rates comparable to steroidal PR antagonists like RU-486 (mifepristone), though its pharmacological mode of action differs from steroidal antagonists. In clinical studies, it blocked the follicular phase increase in endometrial thickness as well as hormonal surges associated with ovulation. PF-02413873 was evaluated in phase I clinical trials but development for endometriosis was discontinued[1][2][4][6].

Other names

4-[3-cyclopropyl-1-(methylsulfonylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2,6-dimethylbenzonitrile