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apratastat

Development stage: Phase 2
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

Apratastat is an orally active, small molecule inhibitor that targets both tumor necrosis factor-alpha converting enzyme (TACE, also known as ADAM17) and matrix metalloproteinases (MMPs), particularly MMP13. It acts as a reversible dual inhibitor, blocking the release of TNF-alpha by inhibiting its conversion from membrane-bound to soluble form. Apratastat was developed for the treatment of inflammatory diseases such as rheumatoid arthritis and was investigated in phase II clinical trials. Despite demonstrating potent inhibition of TNF-alpha release in vitro, ex vivo, and in vivo studies, clinical development was terminated due to lack of efficacy in rheumatoid arthritis[1][4][6][7].

Other names: apratastat

Targets

MMP13 (Matrix metalloproteinase-13)ADAM17 (A disintegrin and metalloprotease 17)

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