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Archives
BACE
Selective Secretase Targeting for Alzheimer's Disease Therapy
9 views | May 05 2021
Alvaro Miranda et al. summarized structures and the activities of the latest compounds designed for AD treatment, with remarkable in vitro, in vivo, and clinical phase activities. [Read the Full Post]
Further analyses of the safety of verubecestat in the phase 3 EPOCH trial of mild-to-moderate Alzheimer's disease
24 views | Nov 27 2020
Michael F Egan et al. thought that verubecestat was associated with increased risk for several types of adverse events. [Read the Full Post]
Quantification and Pharmacokinetic Property of Verubecestat an BACE1 Inhibitor in Rat Plasma
90 views | Jun 29 2020
Qiong Wang et al. designed an ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) approach to measure the rat plasma levels of verubecestat with diazepam as the internal standard. [Read the Full Post]
BACE1 Inhibitor MK-8931 Alters Formation but Not Stability of Dendritic Spines
0 views | Apr 05 2020
Blume T et al. suggested that carefully dosed inhibitors might be therapeutically effective without affecting the structural integrity of excitatory synapses if given at an early disease stage. [Read the Full Post]
Randomized Trial of Verubecestat for Prodromal Alzheimer's Disease
142 views | Feb 23 2020
Michael F Egan et al. indicated that verubecestat did not improve clinical ratings of dementia among patients with prodromal Alzheimer's disease, and some measures suggested that cognition and daily function were worse among patients who received verubecestat than among those who received placebo. [Read the Full Post]
Adavosertib (AZD1775) in Combination With Gemcitabine and Radiation for Patients With Locally Advanced Pancreatic Cancer
133 views | Feb 20 2020
Kyle C Cuneo et al. indicated that AZD1775 in combination with gemcitabine and radiation therapy was well tolerated at a dose that produced target engagement in a surrogate tissue. The overall survival is substantially higher than prior results combining gemcitabine with radiation therapy and warrants additional investigation. [Read the Full Post]
BACE1 Inhibitor MK-8931 Alters Formation but Not Stability of Dendritic Spines
140 views | Feb 20 2020
Tanja Blume et al. suggested that carefully dosed inhibitors might be therapeutically effective without affecting the structural integrity of excitatory synapses if given at an early disease stage. [Read the Full Post]
The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients
378 views | Aug 27 2019
Kennedy ME indicated the human data were fit to an amyloid pathway model that provided insight into the Aβ pools affected by BACE1 inhibition and guided the choice of doses for subsequent clinical trials. [Read the Full Post]
Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage
450 views | Jul 02 2019
Villarreal S et al. showed the absence of elevated ARIA events in verubecestat-treated mice was associated with a significant reduction in the level of accumulated CNS amyloid pathology and brain Aβ peptides; effects consistent with the desired therapeutic mechanism of verubecestat in AD patients. These data will be compared with longitudinal MRI profiles from ongoing clinical trials. [Read the Full Post]
Cyclic cis-Locked Phospho-Dipeptides Reduce Entry of AβPP into Amyloidogenic Processing Pathway
1385 views | Sep 24 2018
Fisher CL et al. suggested a model in which pCDP-diBzl and pCDP-diPOM act at a common point to inhibit entry of AβPP into the amyloidogenic AβPP processing pathway but through different targets, and provide important insights for the development of novel AD therapeutics. [Read the Full Post]
