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Drug candidates in clinical trials for Alzheimer's disease.
Hung SY, Fu WM. Hung SY, et al. J Biomed Sci. 2017 Jul 19;24(1):47. doi: 10.1186/s12929-017-0355-7. J Biomed Sci. 2017. PMID: 28720101 Free PMC article. Review.
Ongoing Phase III clinical trials via passive immunotherapy against Aβ peptides (crenezumab, gantenerumab, and aducanumab) seem to be promising. Using small molecules blocking 5-HT(6) serotonin receptor (intepirdine), inhibiting BACE activity (E2609, AZD3293, …
Ongoing Phase III clinical trials via passive immunotherapy against Aβ peptides (crenezumab, gantenerumab, and aducanumab) seem to be …
BACE1 Dynamics Upon Inhibition with a BACE Inhibitor and Correlation to Downstream Alzheimer's Disease Markers in Elderly Healthy Participants.
Timmers M, Barão S, Van Broeck B, Tesseur I, Slemmon J, De Waepenaert K, Bogert J, Shaw LM, Engelborghs S, Moechars D, Mercken M, Van Nueten L, Tritsmans L, de Strooper B, Streffer JR. Timmers M, et al. J Alzheimers Dis. 2017;56(4):1437-1449. doi: 10.3233/JAD-160829. J Alzheimers Dis. 2017. PMID: 28157093 Free PMC article. Clinical Trial.
We analyzed BACE1 levels in CSF of elderly healthy participants before and after chronic treatment with a BACE inhibitor (BACEi) and evaluated the correlation between BACE1 levels and downstream AD markers. ...Generally, chronic BACE inhibition did not influe …
We analyzed BACE1 levels in CSF of elderly healthy participants before and after chronic treatment with a BACE inhibitor (BACEi) and …
Further analyses of the safety of verubecestat in the phase 3 EPOCH trial of mild-to-moderate Alzheimer's disease.
Egan MF, Mukai Y, Voss T, Kost J, Stone J, Furtek C, Mahoney E, Cummings JL, Tariot PN, Aisen PS, Vellas B, Lines C, Michelson D. Egan MF, et al. Alzheimers Res Ther. 2019 Aug 7;11(1):68. doi: 10.1186/s13195-019-0520-1. Alzheimers Res Ther. 2019. PMID: 31387606 Free PMC article.
While the mechanisms underlying the increased adverse events are unclear, they may be due to BACE inhibition and should be considered in future clinical development programs of BACE1 inhibitors. TRIAL REGISTRATION: ClinicalTrials.gov NCT01739348 , regi …
While the mechanisms underlying the increased adverse events are unclear, they may be due to BACE inhibition and should be con …
Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer's disease: randomized, double-blind, placebo-controlled study.
Timmers M, Streffer JR, Russu A, Tominaga Y, Shimizu H, Shiraishi A, Tatikola K, Smekens P, Börjesson-Hanson A, Andreasen N, Matias-Guiu J, Baquero M, Boada M, Tesseur I, Tritsmans L, Van Nueten L, Engelborghs S. Timmers M, et al. Alzheimers Res Ther. 2018 Aug 23;10(1):85. doi: 10.1186/s13195-018-0415-6. Alzheimers Res Ther. 2018. PMID: 30134967 Free PMC article. Clinical Trial.
BACKGROUND: β-Secretase enzyme (BACE) inhibition has been proposed as a priority treatment mechanism for Alzheimer's disease (AD), but treatment initiation may need to be very early. ...TRIAL REGISTRATION: ALZ1005: ClinicalTrials.gov, NCT01978548. Registered …
BACKGROUND: β-Secretase enzyme (BACE) inhibition has been proposed as a priority treatment mechanism for Alzheimer's disease ( …
What Have We Learned from Expedition III and EPOCH Trials? Perspective of the CTAD Task Force.
Aisen PS, Siemers E, Michelson D, Salloway S, Sampaio C, Carrillo MC, Sperling R, Doody R, Scheltens P, Bateman R, Weiner M, Vellas B. Aisen PS, et al. J Prev Alzheimers Dis. 2018;5(3):171-174. doi: 10.14283/jpad.2018.23. J Prev Alzheimers Dis. 2018. PMID: 29972209
Although the results were disappointing from two recent clinical trials of amyloid-targeting drugs in mild-to-moderate AD, the trials provided information that will be important for future studies, according to the EU-US CTAD Task Force, which met in November 2017 to discu …
Although the results were disappointing from two recent clinical trials of amyloid-targeting drugs in mild-to-moderate AD, the trials …
Icaritin, an inhibitor of beta-site amyloid cleaving enzyme-1, inhibits secretion of amyloid precursor protein in APP-PS1-HEK293 cells by impeding the amyloidogenic pathway.
Feng F, Li Y, Huang N, Luo Y. Feng F, et al. PeerJ. 2019 Dec 10;7:e8219. doi: 10.7717/peerj.8219. eCollection 2019. PeerJ. 2019. PMID: 31844591 Free PMC article.
METHODS: We exposed APP-PS1-HEK293 cells to ICT to investigate its effect on beta-site amyloid cleaving enzyme (BACE)1. Cell viability was evaluated by MTT and lactate dehydrogenase (LDH) assays. ...CONCLUSIONS: Icaritin, as a BACE1 inhibitor, inhibits APP secretion …
METHODS: We exposed APP-PS1-HEK293 cells to ICT to investigate its effect on beta-site amyloid cleaving enzyme (BACE)1. Cell viabilit …
Characterization of plasma β-secretase (BACE1) activity and soluble amyloid precursor proteins as potential biomarkers for Alzheimer's disease.
Wu G, Sankaranarayanan S, Wong J, Tugusheva K, Michener MS, Shi X, Cook JJ, Simon AJ, Savage MJ. Wu G, et al. J Neurosci Res. 2012 Dec;90(12):2247-58. doi: 10.1002/jnr.23122. Epub 2012 Sep 18. J Neurosci Res. 2012. PMID: 22987781 Clinical Trial.
Plasma BACE activity assay was sensitive and specific, with signal being immunodepleted with a specific BACE1 antibody and inhibited with a BACE1-specific inhibitor. ...In conclusion, plasma BACE activity and sAPP endpoints provide novel investigative biomark …
Plasma BACE activity assay was sensitive and specific, with signal being immunodepleted with a specific BACE1 antibody and inhibit
Molecular investigations of protriptyline as a multi-target directed ligand in Alzheimer's disease.
Bansode SB, Jana AK, Batkulwar KB, Warkad SD, Joshi RS, Sengupta N, Kulkarni MJ. Bansode SB, et al. PLoS One. 2014 Aug 20;9(8):e105196. doi: 10.1371/journal.pone.0105196. eCollection 2014. PLoS One. 2014. PMID: 25141174 Free PMC article.
The repositioning of existing non-toxic drugs could dramatically reduce the time and costs involved in developmental and clinical trial stages. ...The molecular basis of inhibition was supported with comprehensive molecular dynamics simulations. Further, the …
The repositioning of existing non-toxic drugs could dramatically reduce the time and costs involved in developmental and clinical
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