Drug intelligence / Profile preview

PG-116800

Development stage
Phase 2
Lead developer
Procter & Gamble
Modality
Small Molecules
Administration
Oral
01

Overview

**PG-116800** is an orally active, small molecule inhibitor of matrix metalloproteinases (MMPs), specifically designed to target MMP subtypes implicated in tissue remodeling and degradation. It belongs to the hydroxyproline-based hydroxamic acid class of MMP inhibitors and exhibits high affinity for MMP-2, -3, -8, -9, -13, and -14. The drug was developed by Procter & Gamble Pharmaceuticals primarily for the treatment of osteoarthritis (OA) and also investigated for its potential to reduce left ventricular remodeling after myocardial infarction (MI). Despite promising preclinical antiremodeling effects in animal models of MI and ischemic heart failure, clinical trials failed to demonstrate efficacy in patients with knee OA or post-MI cardiac remodeling. Notably, higher doses were associated with musculoskeletal adverse effects such as arthralgia and joint stiffness[2][3][5][6][7][8].

Other names
291533-11-4UNII-F94T42GL80UNII-F-94T42GL80UNII-F 94T42GL80
02

Targets

MMP9 (Matrix metalloproteinase-9)MMP8 (Neutrophil collagenase)MMP2 (Matrix metalloproteinase-2)MMP14 (Matrix metalloproteinase 14)MMP3 (Matrix metalloproteinase-3)MMP1 (Matrix metalloproteinase-1)MMP7 (Matrix metallopeptidase 7)MMP13 (Matrix metalloproteinase-13)

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