Apratastat

Description: Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-alpha converting enzyme (TACE) and matrix metalloproteinases (MMPs) and it also can potently inhibit the release of TNF-alpha in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively[1]. Target: MMP, TNF. Smiles: CC1(C)SCCN([C@H]1C(=O)NO)S(=O)(=O)c1ccc(OCC#CCO)cc1. References: Shu C, et al. Pharmacokinetic-pharmacodynamic modeling of apratastat: a population-based approach. J Clin Pharmacol. 2011 Apr,51(4):472-81.