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RO5508887
- Development stage
- Phase 1
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral (based On Typical Administration For Similar Small Molecules; Specific Route Not Explicitly Stated But Inferred From Clinical Trial Design)
01
Overview
RO5508887 is a potent small molecule inhibitor of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), also known as beta-secretase. It is an aminooxazoline derivative that inhibits BACE1 with an IC50 of approximately 30 nM and is similarly potent against BACE2. The compound was developed by Roche for the treatment of Alzheimer's disease and entered clinical trials in 2011. However, development was discontinued in October 2013 without public explanation. Preclinical studies demonstrated its efficacy in reducing amyloid-beta production, and it was also studied in combination with anti-Aβ antibody gantenerumab[1][2][3][4][5][7].
- Other names
- 1310347-50-2
02
Targets
BACE2 (Beta-site amyloid precursor protein cleaving enzyme 2)BACE1 (Beta-site APP-cleaving enzyme 1)
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