PD166793

PD166793 is a small molecule, carboxylate-based matrix metalloproteinase (MMP) inhibitor originally developed by Parke-Davis (later acquired by Warner-Lambert and Pfizer) for the treatment of cardiovascular diseases, specifically systolic heart failure and post-ischemic myocardial remodeling. It exhibits potent, nanomolar inhibitory activity against MMP-2, MMP-3, and MMP-13, while sparing MMP-1, MMP-7, and MMP-9 to avoid the musculoskeletal syndrome associated with broad-spectrum MMP inhibitors. Additionally, PD166793 acts as a weak inhibitor of AMP deaminase. More recently, PD166793 has been investigated as a repurposed therapeutic agent for Alzheimer's disease, where it directly binds to amyloid-beta 42 (Aβ42) and selectively blocks its oligomerization, thereby mitigating neurotoxicity, reducing neuroinflammation, and improving cognitive function in preclinical models.

Other names

(S)-2-(4'-Bromo-biphenyl-4-sulfonylamino)-3-methyl-butyric acidMMP-2/MMP-3 Inhibitor IIIN-[(4'-Bromo[1,1'-biphenyl]-4-yl)sulfonyl]-L-valine