PF-02413873

PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a K i of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo In Vitro PF-02413873 shows potent PR antagonist activity with a derived K i of 9.7 nM in the T47D native functional assay. PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques . PF-02413873 (3 mg/kg; a single p.o.) exhibits t 1/2 (4.2 h), C max (162 ng/mL) and CL/F (41 mL/min/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Cynomolgus macaques (3.7-5.7 kg; 5-6 years) Dosage: 2.5, 10 mg/kg Administration: P.o. twice daily for 10 days Result: Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively. Animal Model: Cynomolgus macaques (3.7-5.7 kg; 5-6 years) Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: A single p.o. Result: t 1/2 =4.2 h, C max =162 ng/mL, CL/F=41 mL/min/kg. IC50& Target:Ki: 2.6 nM (progesterone receptor)

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