| 词条 | Verubecestat |
| 释义 |
| drug_name = | INN = | type = | IUPAC_name = | image = Verubecestat.svg | alt = | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_AU = | legal_AU_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = | legal_UN = | legal_status = Investigational | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | CAS_number = 1286770-55-5 | ATCvet = | ATC_prefix = None | ATC_suffix = | ChemSpiderID = 31399364 | KEGG = D10739 | PubChem = 51352361 | DrugBank = | UNII = J1I0P6WT7T | synonyms = MK-8931 | C=17|H=17|F=2|N=5|O=3|S=1 | molecular_weight = | smiles = C[C@]1(CS(=O)(=O)N(C(=N1)N)C)c2cc(ccc2F)NC(=O)c3ccc(cn3)F | StdInChI=1S/C17H17F2N5O3S/c1-17(9-28(26,27)24(2)16(20)23-17)12-7-11(4-5-13(12)19)22-15(25)14-6-3-10(18)8-21-14/h3-8H,9H2,1-2H3,(H2,20,23)(H,22,25)/t17-/m0/s1 | StdInChIKey = YHYKUSGACIYRML-KRWDZBQOSA-N }}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|2016|12}} it was 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 were expected in February 2019. However, the trial was terminated in February 2018, after a data monitoring committee concluded it was unlikely that the drug would show a positive benefit/risk ratio.[8][9] The final conclusion was that "verubecestat did not reduce cognitive or functional decline in patients with mild-to-moderate Alzheimer’s disease and was associated with treatment-related adverse events".[10]References1. ^1 {{Cite journal | title = New Alzheimer’s drug clears milestone in human clinical trial | author = Simon Makin | date = November 2, 2016 | url = https://www.scientificamerican.com/article/new-alzheimer-s-drug-clears-milestone-in-human-clinical-trial1 | publisher = Scientific American}} {{Anti-dementia drugs}}2. ^1 {{cite journal | doi = 10.1016/j.jalz.2013.04.083| title = The novel BACE inhibitor MK-8931 dramatically lowers CSF beta-amyloid in patients with mild-to-moderate Alzheimer's disease| journal = Alzheimer's & Dementia| volume = 9| issue = 4| pages = P139| year = 2013| last1 = Forman| first1 = Mark| last2 = Kleijn| first2 = Huub-Jan| last3 = Dockendorf| first3 = Marissa| last4 = Palcza| first4 = John| last5 = Tseng| first5 = Jack| last6 = Canales| first6 = Christina| last7 = Egan| first7 = Michael| last8 = Kennedy| first8 = Matthew| last9 = Laterza| first9 = Omar| last10 = Ma| first10 = Lei| last11 = Scott| first11 = Jack| last12 = Tanen| first12 = Michael| last13 = Apter| first13 = Jeffrey| last14 = Backonja| first14 = Miroslav| last15 = Ereshefsky| first15 = Larry| last16 = Gevorkyan| first16 = Hakop| last17 = Jhee| first17 = Stanford| last18 = Rynders| first18 = Rebecca| last19 = Zari| first19 = Arian| last20 = Bryan| first20 = Ellie| last21 = Wagner| first21 = John| last22 = Troyer| first22 = Matthew| last23 = Stone| first23 = Julie | name-list-format = vanc | display-authors = 6 }} 3. ^1 {{cite journal | vauthors = Yan R, Vassar R | title = Targeting the β secretase BACE1 for Alzheimer's disease therapy | journal = The Lancet. Neurology | volume = 13 | issue = 3 | pages = 319–29 | date = March 2014 | pmid = 24556009 | pmc = 4086426 | doi = 10.1016/S1474-4422(13)70276-X }} 4. ^{{cite news |url=http://www.merck.com/newsroom/news-release-archive/research-and-development/2012_0427.html |title=Merck presents results of a phase I clinical trial evaluating investigational BACE inhibitor MK-8931 at American Academy of Neurology |date=April 2012 |access-date=2012-07-16 |archive-url=https://web.archive.org/web/20120728084446/http://www.merck.com/newsroom/news-release-archive/research-and-development/2012_0427.html |archive-date=2012-07-28 |dead-url=yes |df= }} 5. ^{{cite web |url=https://clinicaltrials.gov/ct2/show/NCT01953601 |title=Efficacy and safety trial of verubecestat (MK-8931) in participants with prodromal Alzheimer's disease (MK-8931-019) (APECS)|access-date=16 February 2017 |publisher=Merck Sharp & Dohme Corp. }} 6. ^1 {{cite web|url=https://clinicaltrials.gov/ct2/show/NCT01739348 |title=An efficacy and safety trial of verubecestat (MK-8931) in mild to moderate Alzheimer's disease (P07738) (EPOCH) |publisher=Merck Sharp & Dohme Corp. |date=October 2016 |access-date=16 February 2017}} 7. ^{{cite press release |url=http://www.mercknewsroom.com/news-release/research-and-development-news/merck-announces-epoch-study-verubecestat-treatment-people |title=Merck announces EPOCH study of verubecestat for the treatment of people with mild to moderate Alzheimer’s disease to stop for lack of efficacy |publisher=Merck |date=14 February 2017}} 8. ^ Barber, J. (2018). Merck & Co. terminates Phase III study of verubecestat in prodromal Alzheimer's disease. Retrieved from https://www.firstwordpharma.com/node/1542930 9. ^{{ClinicalTrialsGov|NCT01953601|Efficacy and Safety Trial of Verubecestat (MK-8931) in Participants With Prodromal Alzheimer's Disease (MK-8931-019)}} 10. ^{{cite journal | doi = 10.1056/NEJMoa1706441| pmid = 29719179| title = Randomized Trial of Verubecestat for Mild-to-Moderate Alzheimer's Disease| journal = New England Journal of Medicine| volume = 378| issue = 18| pages = 1691| year = 2018| last1 = Egan| first1 = Michael F| last2 = Kost| first2 = James| last3 = Tariot| first3 = Pierre N| last4 = Aisen| first4 = Paul S| last5 = Cummings| first5 = Jeffrey L| last6 = Vellas| first6 = Bruno| last7 = Sur| first7 = Cyrille| last8 = Mukai| first8 = Yuki| last9 = Voss| first9 = Tiffini| last10 = Furtek| first10 = Christine| last11 = Mahoney| first11 = Erin| last12 = Harper Mozley| first12 = Lyn| last13 = Vandenberghe| first13 = Rik| last14 = Mo| first14 = Yi| last15 = Michelson| first15 = David}} 4 : Fluoroarenes|Carboxamides|Enzyme inhibitors|Alzheimer's disease research |
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