PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3 and MMP-13.PD-166793 ameliorates myocardial ischemia and reperfusion injury in a rat model of heart failure.PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3, and MMP-13.

MMP13:8 nM, MMP3:7 nM, MMP1:6.0 μM, MMP7:7.2 μM, MMP2:4 nM, MMP9:7.9 μM

In rat heart homogenates, PD-166793 at a concentration of 0.1 μM results in a 20% inhibition of AMP deaminase (AMPD) activity[2]. Additionally, when normal human cardiac fibroblasts are treated with PD-166793 at a concentration of 100 μM for 36 hours, there is a significant reduction in MMP‐9 activity[1].

Administered at a dosage of 1 mg/kg per day through daily gavage for a duration of 10 weeks, PD-166793 largely prevents the adverse remodeling typically observed in the aortocaval (AV) fistula model[3]. Furthermore, in rats, PD-166793 administered at a dose of 5 mg/kg via oral gavage demonstrates superior pharmacokinetics, with a half-life (t1/2) of 43.6 hours, a maximum concentration (Cmax) of 42.4 µg/mL, and an area under the curve from 0 to infinity (AUC0-∞) of 2822 µg•h/mL[2].