PF-4693627

PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 ( m PGES-1 ) inhibitor ( IC 50 =3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) In Vitro PF-4693627 also inhibits mPGES-1 with IC 50 s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively. PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC 50 =109 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model . PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t 1/2 =3.7 h) in Sprague-Dawley rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Guinea pig with carrageenan stimulated air pouch inflammation model Dosage: 10 mg/kg Administration: Administered orally Result: 63% PGE2 inhibition. Animal Model: Sprague-Dawley rats . Dosage: 1.0 mg/kg (Pharmacokinetic Analysis) Administration: Administered i.v. Result: Clearance (CL), volume of distribution (Vd ss ), t 1/2 , mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively. Form:Solid IC50& Target:IC50: 3 nM (mPGES-1)

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