Drug intelligence / Profile preview

ilomastat

Development stage
Unknown
Lead developer
Ligand Pharmaceuticals
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Ilomastat is a synthetic small molecule and a broad-spectrum inhibitor of matrix metalloproteinases (MMPs), including MMP-1 (interstitial collagenase), MMP-2, MMP-3, and MMP-9[1][2][3][5]. It belongs to the hydroxamic acid class of reversible metallopeptidase inhibitors. Ilomastat acts by binding the catalytic zinc ion in the active site of MMPs in a bidentate manner, thereby blocking substrate access and inhibiting enzymatic activity[3][5]. This mechanism underlies its anti-scarring effects observed in preclinical models for ophthalmic surgery (such as glaucoma filtration surgery) and other tissue remodeling conditions[4][7]. Ilomastat has also demonstrated anti-tumor and anti-angiogenic properties in experimental settings[4][5], as well as potential applications for trauma healing and corneal repair. It remains an experimental compound without regulatory approval for any indication.

Brand names
Galardin
Other names
GM6001GM-6001GM 6001galardinilomastat
02

Targets

MMP1 (Matrix metalloproteinase-1)MMP12 (Macrophage Metalloelastase)MMP14 (Matrix metalloproteinase 14)MMP2 (Matrix metalloproteinase-2)MMP3 (Matrix metalloproteinase-3)MMP7 (Matrix metallopeptidase 7)MMP8 (Neutrophil collagenase)MMP9 (Matrix metalloproteinase-9)

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