Drug intelligence / Profile preview

ly2886721

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY2886721 is an oral small molecule inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1), developed for the treatment of Alzheimer's disease. By inhibiting BACE1, it reduces the synthesis of β‑amyloid peptides implicated in Alzheimer’s pathology. The compound demonstrated high selectivity for BACE1 over other aspartyl proteases such as cathepsin D and pepsin and showed robust amyloid-lowering effects in preclinical animal models and healthy human subjects. In clinical studies, LY2886721 lowered cerebrospinal fluid (CSF) Aβ40 and Aβ42 levels by up to 72% after two weeks of daily dosing. It was the first BACE inhibitor to reach Phase 2 clinical trials but development was terminated due to liver toxicity observed in a subset of patients during these trials[3][5][6].

Other names
1262036-50-9UNII-2CQ62IWB67UNII2CQ62IWB67UNII 2CQ62IWB67N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide
02

Targets

BACE1 (Beta-site APP-cleaving enzyme 1)BACE2 (Beta-site amyloid precursor protein cleaving enzyme 2)

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