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Archives
BACE
Quantification and Pharmacokinetic Property of Verubecestat an BACE1 Inhibitor in Rat Plasma
57 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
117 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
105 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
112 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
345 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
416 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
1352 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]
