Drug intelligence / Profile preview

GRL-8234

Development stage
Unknown
Lead developer
CoMentis
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal, Subcutaneous, Intranasal, Oral
01

Overview

GRL-8234 is a potent and selective small-molecule inhibitor of Beta-secretase 1 (BACE1), also known as β-secretase. Developed by CoMentis, the compound was designed to treat Alzheimer's disease by blocking the initial step in the proteolytic processing of amyloid precursor protein (APP) into amyloid-β (Aβ) peptides, specifically Aβ42. Preclinical studies in transgenic mouse models demonstrated that GRL-8234 effectively crosses the blood-brain barrier, reduces cerebral Aβ levels, and reverses memory impairments. Although it was positioned as a clinical candidate, the development status is currently unclear following the apparent cessation of operations by CoMentis.

Other names
3-N-[(2S,3R)-3-hydroxy-4-[(3-methoxyphenyl)methylamino]-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-1-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
02

Targets

CTSD (Cathepsin D)BACE1 (Beta-site APP-cleaving enzyme 1)

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