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  1. www.alzforum.org › therapeutics › verubecestatVerubecestat - ALZFORUM

    2021年1月21日 · MK-8931 is a small-molecule inhibitor of BACE1 and BACE2. BACE1 is the β-secretase enzyme that cleaves the APP protein to release the C99 fragment of APP, which gives rise to various species of Aβ peptide during its subsequent cleavage by γ-secretase.

  2. 2014年11月28日 · In press in Biological Psychiatry, the full study now reports that BACE inhibitors quash synaptic plasticity and cause memory loss in normal adult mice. The findings suggest that such inhibitors could pose a threat to neurons if used at high enough doses, but also offer reassurance that low doses could block Aβ production without affecting memory.

  3. If MK-8931 causes overproduction and accumulation of Aβ 17-40/42 in vivo, pathological consequences might emerge after some years of treatment in people. I suggest that the authors examine the effect of MK-8931 on our single NL-F App knock-in mice ( Saito et al., 2014 ), which show extensive pathology at six months without overexpressing APP.

  4. 13 Nov 2021. Letdown though it was, BACE inhibitors’ fall from grace as the up-and-coming Alzheimer’s disease treatment may not have been in vain. According to a study published November 8 in Nature Cancer, verubecestat, the first of a class of BACE inhibitors to fail big in AD trials, may yet hold promise as a treatment for glioblastoma.

  5. Amyloid-Related 2000 2001 2002 2003 2004 2005 2006 2007 2008 2009 2010 2011 2012 2013 2014 2015 2016 2017 2018 2019 2020 2021 2022 ...

  6. www.alzforum.org › therapeutics › elenbecestatElenbecestat - ALZFORUM

    Elenbecestat is a small-molecule inhibitor of BACE, aka the β-secretase enzyme. It was developed with the rationale of interfering with the amyloid cascade upstream of Aβ peptide generation. BACE inhibition is sometimes envisioned as long-term maintenance therapy to limit Aβ production after an initial round of immunotherapy to remove ...

  7. www.alzforum.org › therapeutics › atabecestatAtabecestat - ALZFORUM

    At the 2018 CTAD conference, Janssen reported that EARLY participants who took 25 mg atabecestat scored four points worse than the placebo group on the RBANS at three months, and one point worse on the PACC at six and 12 months. Treatment groups reported more depression, anxiety, and sleep problems than controls (Nov 2018 conference news).

  8. www.alzforum.org › therapeutics › azd3293Lanabecestat - ALZFORUM

    Likewise, DAYBREAK revealed no treatment benefit on any endpoint, with similar side effects. Biomarker data demonstrated target engagement. Lanabecestat reduced blood Aβ40 and Aβ42 levels by 70 to 80 percent in both trials. CSF Aβ, measured in AMARANTH, dropped by 50 and 73 percent at the low and high doses, respectively.

  9. Alzheimer's Disease (Discontinued) Denali Therapeutics Inc., Takeda Pharmaceutical Company. Amyloid-Related, Inflammation. Immunotherapy (passive) Docosahexaenoic acid (DHA) Omega-3 fatty acid. Alzheimer's Disease (Phase 4) Martek Biosciences Corporation, NeuroBioPharm, Inc.

  10. 12 Dec 2017. The enormous challenges of recruitment loomed large at the 10th annual Clinical Trials on Amyloid Disease conference, held November 1–4 in Boston. Researchers are seeking new ways of identifying legions of eligible volunteers to enroll in clinical trials for Alzheimer’s disease.

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