Verubecestat
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| Synonyms | MK-8931 |
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| Formula | C17H17F2N5O3S |
| Molar mass | 409.41 g·mol−1 |
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Verubecestat (MK-8931) is an experimental drug for the treatment of Alzheimer's disease.[1] It is an inhibitor of beta-secretase 1 (BACE1).[2][3]
In April 2012 phase I clinical results were announced.[4] Phase 1b results have also been reported.[3][2]
As of December 2016 it ws in two phase 2/3 clinical trials that have progressed to phase 3.[1][5][6] EPOCH, was to complete data collection for the primary outcome measure by June 2017.[6] However, in February 2017 Merck halted its late-stage trial of verubecestat for mild to moderate Alzheimer's disease after it was reported as having "virtually no chance of finding a positive clinical effect" according to an independent panel of experts.[7] The results of Merck's trial of verubecestat on patients with prodromal (early stage) Alzheimer's are still expected in February 2019.
References
- 1 2 Simon Makin (November 2, 2016). "New Alzheimer’s drug clears milestone in human clinical trial". Scientific American.
- 1 2 Forman, Mark; Kleijn, Huub-Jan; Dockendorf, Marissa; Palcza, John; Tseng, Jack; Canales, Christina; Egan, Michael; Kennedy, Matthew; Laterza, Omar; Ma, Lei; Scott, Jack; Tanen, Michael; Apter, Jeffrey; Backonja, Miroslav; Ereshefsky, Larry; Gevorkyan, Hakop; Jhee, Stanford; Rynders, Rebecca; Zari, Arian; Bryan, Ellie; Wagner, John; Troyer, Matthew; Stone, Julie (2013). "The novel BACE inhibitor MK-8931 dramatically lowers CSF beta-amyloid in patients with mild-to-moderate Alzheimer's disease". Alzheimer's & Dementia. 9 (4): P139. doi:10.1016/j.jalz.2013.04.083.
- 1 2 Yan, Riqiang; Vassar, Robert (2014). "Targeting the β secretase BACE1 for Alzheimer's disease therapy". The Lancet Neurology. 13 (3): 319–329. PMC 4086426
. PMID 24556009. doi:10.1016/S1474-4422(13)70276-X. - ↑ "Merck presents results of a phase I clinical trial evaluating investigational BACE inhibitor MK-8931 at American Academy of Neurology". April 2012.
- ↑ "Efficacy and safety trial of verubecestat (MK-8931) in participants with prodromal Alzheimer's disease (MK-8931-019) (APECS)". Merck Sharp & Dohme Corp. Retrieved 16 February 2017.
- 1 2 "An efficacy and safety trial of verubecestat (MK-8931) in mild to moderate Alzheimer's disease (P07738) (EPOCH)". Merck Sharp & Dohme Corp. October 2016. Retrieved 16 February 2017.
- ↑ "Merck announces EPOCH study of verubecestat for the treatment of people with mild to moderate Alzheimer’s disease to stop for lack of efficacy" (Press release). Merck. 14 February 2017.