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Alzheimer's disease (AD)

b-Site APP-cleaving enzyme 1 (BACE1); b-amyloid 40

Rodent studies suggest fused bicyclic iminopyrimidinone-based BACE1 inhibitors could help treat neurodegenerative diseases such as AD. In vitro, a lead member of the series inhibited BACE1 with a Ki of 4 nM. In a rat model of AD, oral treatment with the lead inhibitor decreased plasma, cerebrospinal fluid and brain levels of b-amyloid 40 compared with vehicle treatment. Next steps include studies to move a lead analog from the series toward clinical development.
MK-8931, a BACE1 inhibitor from Merck & Co. Inc., is in Phase I testing to treat AD.
At least six other companies have BACE1 inhibitors in Phase I development or earlier to treat AD.

SciBX 5(40); doi:10.1038/scibx.2012.1057
Published online Oct. 11, 2012

Patented; unavailable for licensing

Mandal, M. et al. J. Med. Chem.; published online Sept. 18, 2012;
Contact: Mihirbaran Mandal,
Merck Research Laboratories, Kenilworth, N.J.