This database contains 20 studies, archived under the term: "antagonists inhibitors"
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Amyloid-β(1-15/16) as a marker for γ-secretase inhibition in Alzheimer’s disease
Portelius, Erik,
Zetterberg, Henrik,
Dean, Robert A.,
Marcil, Alexandre,
Bourgeois, Philippe,
Nutu, Magdalena,
Andreasson, Ulf,
Siemers, Eric,
Mawuenyega, Kwasi G.,
Sigurdson, Wendy C.,
May, Patrick C.,
Paul, Steven M.,
Holtzman, David M.,
Blennow, Kaj,
Bateman, Randall J.
Amyloid-β (Aβ) producing enzymes are key targets for disease-modifying Alzheimer’s disease (AD) therapies since Aβ trafficking is at the core of AD pathogenesis. Development of such drugs might benefit from the identification of markers indicating in vivo drug effects in the central nervous system. We have previously shown that Aβ(1-15) is produced by concerted β-and […]
A placebo-controlled, multiple ascending dose study to evaluate the safety, pharmacokinetics and pharmacodynamics of avagacestat (BMS-708163) in healthy young and elderly subjects
Dockens, Randy,
Wang, Jun-Sheng,
Castaneda, Lorna,
Sverdlov, Oleksandr,
Huang, Shu-Pang,
Slemmon, Randy,
Gu, Huidong,
Wong, Oi,
Li, Hewei,
Berman, Robert M.,
Smith, Christina,
Albright, Charles F.,
Tong, Gary
Background and Objectives: Avagacestat is an orally active γ-secretase inhibitor that selectively inhibits amyloid β (Aβ) synthesis in cell culture and animal models. The objective of the current study was to assess the pharmacokinetics, pharmacodynamics, safety and tolerability of multiple doses of avagacestat over 28 days in healthy young men and elderly men and women […]
Donepezil and memantine for moderate-to-severe Alzheimer’s disease
Howard, Robert,
McShane, Rupert,
Lindesay, James,
Ritchie, Craig,
Baldwin, Ashley,
Barber, Robert,
Burns, Alistair,
Dening, Tom,
Findlay, David,
Holmes, Clive,
Hughes, Alan,
Jacoby, Robin,
Jones, Rob,
Jones, Roy,
McKeith, Ian,
Macharouthu, Ajay,
O'Brien, John,
Passmore, Peter,
Sheehan, Bart,
Juszczak, Edmund,
Katona, Cornelius,
Hills, Robert,
Knapp, Martin,
Ballard, Clive,
Brown, Richard,
Banerjee, Sube,
Onions, Caroline,
Griffin, Mary,
Adams, Jessica,
Gray, Richard,
Johnson, Tony,
Bentham, Peter,
Phillips, Patrick
Background: Clinical trials have shown the benefits of cholinesterase inhibitors for the treatment of mild-to-moderate Alzheimer’s disease. It is not known whether treatment benefits continue after the progression to moderate-to-severe disease.; Methods: We assigned 295 community-dwelling patients who had been treated with donepezil for at least 3 months and who had moderate or severe Alzheimer’s […]
Memantine for dementia in adults older than 40 years with Down’s syndrome (MEADOWS): a randomised, double-blind, placebo-controlled trial
Hanney, Marisa,
Prasher, Vee,
Williams, Nicola,
Jones, Emma L.,
Aarsland, Dag,
Corbett, Anne,
Lawrence, Dale,
Yu, Ly-Mee,
Tyrer, Stephen,
Francis, Paul T.,
Johnson, Tony,
Bullock, Roger,
Ballard, Clive
Background: Prevalence of Alzheimer’s disease in people with Down’s syndrome is very high, and many such individuals who are older than 40 years have pathological changes characteristic of Alzheimer’s disease. Evidence to support treatment with Alzheimer’s drugs is inadequate, although memantine is beneficial in transgenic mice. We aimed to assess safety and efficacy of memantine […]
Effect of B vitamins and lowering homocysteine on cognitive impairment in patients with previous stroke or transient ischemic attack: a prespecified secondary analysis of a randomized, placebo-controlled trial and meta-analysis
Hankey, Graeme J.,
Ford, Andrew H.,
Yi, Qilong,
Eikelboom, John W.,
Lees, Kennedy R.,
Chen, Christopher,
Xavier, Denis,
Navarro, Jose C.,
Ranawaka, Udaya K.,
Uddin, Wasim,
Ricci, Stefano,
Gommans, John,
Schmidt, Reinhold,
Almeida, Osvaldo P.,
van Bockxmeer, Frank M.
Background and Purpose: High plasma total homocysteine (tHcy) has been associated with cognitive impairment but lowering tHcy with B-vitamins has produced equivocal results. We aimed to determine whether B-vitamin supplementation would reduce tHcy and the incidence of new cognitive impairment among individuals with stroke or transient ischemic attack≥6 months previously.; Methods: A total of 8164 […]
Comparative cardiovascular safety of dementia medications: a cross-national study
Fosbøl, Emil L.,
Peterson, Eric D.,
Holm, Ellen,
Gislason, Gunnar H.,
Zhang, Yinghong,
Curtis, Lesley H.,
Køber, Lars,
Iwata, Isao,
Torp-Pedersen, Christian,
Setoguchi, Soko
Objectives: To compare the cardiovascular safety of currently marketed dementia medications in new users in the United States and Denmark.; Design: Retrospective cohort study.; Setting: Nationally representative sample of Medicare beneficiaries from 2006 through 2009 and nationwide Danish administrative registries from 1997 through 2007.; Participants: Individuals treated with a dementia medication aged 65 and older.; […]
Akatinol memantine in patients with vascular cognitive disorders
Treatment of cognitive disorders developed in cerebrovascular pathology is an actual medical problem. Of great importance is the timed diagnosis of these changes in the earlier phases of the development of cognitive deficit as well as adequate therapy that can delay and prevent the development of such complication as dementia. Pathogenetic mechanisms of cognitive disorders […]
Effect of tarenflurbil on cognitive decline and activities of daily living in patients with mild Alzheimer disease: a randomized controlled trial
Green, Robert C.,
Schneider, Lon S.,
Amato, David A.,
Beelen, Andrew P.,
Wilcock, Gordon,
Swabb, Edward A.,
Zavitz, Kenton H.
Context: Amyloid-beta peptide (Abeta(42)) has been implicated in the pathogenesis of Alzheimer disease (AD). Tarenflurbil, a selective Abeta(42)-lowering agent, demonstrated encouraging results on cognitive and functional outcomes among mildly affected patients in an earlier phase 2 trial.; Objective: To determine the efficacy, safety, and tolerability of tarenflurbil.; Design, Setting, and Patients: A multicenter, randomized, double-blind, […]
Lithium trial in Alzheimer’s disease: a randomized, single-blind, placebo-controlled, multicenter 10-week study
Hampel, Harald,
Ewers, Michael,
Bürger, Katharina,
Annas, Peter,
Mörtberg, Anette,
Bogstedt, Anna,
Frölich, Lutz,
Schröder, Johannes,
Schönknecht, Peter,
Riepe, Matthias W.,
Kraft, Inga,
Gasser, Thomas,
Leyhe, Thomas,
Möller, Hans-Jürgen,
Kurz, Alexander,
Basun, Hans
Objective: Lithium, a first-line drug for the treatment of bipolar depression, has recently been shown to regulate glycogen synthase kinase-3 (GSK-3), a kinase that is involved in the phosphorylation of the tau protein. Since hyperphosphorylation of tau is a core pathological feature in Alzheimer’s disease, lithium-induced inhibition of GSK-3 activity may have therapeutic effects in […]