Merck Inc. announces publication in Science Translational Medicine of development of verubecestat as a potential treatment for Alzheimer�s disease.

Merck Inc. announced the publication of research conducted by Merck scientists on the discovery and development of verubecestat, an investigational small molecule inhibitor of the enzyme beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), for the potential treatment of Alzheimer�s disease (AD). The research was published online in the latest edition of the peer-reviewed journal Science Translational Medicine and includes results from the Phase 1 clinical trials in healthy volunteers and people with AD.

The efficacy and safety of verubecestat is currently being evaluated in two pivotal Phase III clinical trials, EPOCH and APECS, for the treatment of mild-to-moderate AD and prodromal AD, respectively. BACE1 is an important enzyme in the initiation of the toxic A beta peptide production in the brain. Researchers believe that sustained, selective inhibition of BACE1 leading to a significant decrease in the toxic A beta peptide production is a promising means for therapeutic intervention. This hypothesis has not yet been demonstrated in clinical studies. evaluation of once-daily doses of verubecestat in Phase 1 studies of healthy volunteers and in people with AD for a duration of one week demonstrated significant decreases in the levels of A beta peptide production, a key marker of BACE1 activity, in the cerebral spinal fluid (CSF) of up to 80 percent.

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"The BACE1 inhibitor verubecestat (MK-8931) reduces CNS ?-amyloid in animal models and in Alzheimer�s disease patients"- Matthew E. Kennedy, Andrew W. Stamford, Xia Chen, Kathleen Cox, Jared N. Cumming, Marissa F. Dockendorf, Michael Egan, Larry Ereshefsky, Robert A. Hodgson, Lynn A. Hyde, Stanford Jhee, Huub J. Kleijn, Reshma Kuvelkar, Wei Li, Britta A. Mattson, Hong Mei, John Palcza, Jack D. Scott, Michael Tanen, Matthew D. Troyer, Jack L. Tseng, Julie A. Stone, Eric M. Parker and Mark S. Forman- Science Translational Medicine 02 Nov 2016: Vol. 8, Issue 363, pp. 363ra150 DOI: 10.1126/scitranslmed.aad9704.