BI-4394

BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor ( IC 50 =1 nM ) for the potential treatment of osteoarthritis . BI-4394 is >1000 selective over other MMPs In Vitro BI-4394 (Compound 15) is potent in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC 50 of 31 nM. BI-4394 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC 50 s of 18, 8.9, 16 and 8.3 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo When dosed orally at 10 mg/kg or i.v. 1 mg/kg, BI-4394 (Compound 15) reaches micromolar plasma levels (AUC=1109±64 nM h/mL), displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The V ss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 has short terminal elimination half-life (t 1/2 =0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Srapgue Dally Rats Dosage: 10 mg/kg (oral gavage); 1 mg/kg (i.v.) Administration: Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis) Result: T 1/2 =0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively. Form:Solid IC50& Target:MMP-13 1 nM (IC 50 ) MMP-14 8.3 μM (IC 50 ) MMP-9 8.9 μM (IC 50 ) MMP-10 16 μM (IC 50 ) MMP-2 18 μM (IC 50 )

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