Ly411575
| Title | Journal |
|---|---|
| A phase 3 trial of semagacestat for treatment of Alzheimer's disease. | The New England journal of medicine 20130725 |
| Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design. | Proceedings of the National Academy of Sciences of the United States of America 20121226 |
| The effects on metabolic clearance when administering a potent CYP3A autoinducer with the prototypic CYP3A inhibitor, ketoconazole. | Drug metabolism and disposition: the biological fate of chemicals 20121001 |
| Semagacestat pharmacokinetics are not significantly affected by formulation, food, or time of dosing in healthy participants. | Journal of clinical pharmacology 20120601 |
| miR-9 controls the timing of neurogenesis through the direct inhibition of antagonistic factors. | Developmental cell 20120515 |
| A brain aggregate model gives new insights into the pathobiology and treatment of prion diseases. | Journal of neuropathology and experimental neurology 20120501 |
| First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms. | The Journal of biological chemistry 20120406 |
| Γ-secretase modulators do not induce Aβ-rebound and accumulation of β-C-terminal fragment. | Journal of neurochemistry 20120401 |
| QT effect of semagacestat at therapeutic and supratherapeutic doses. | International journal of clinical pharmacology and therapeutics 20120401 |
| Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20120208 |
| A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators. | Journal of Alzheimer's disease : JAD 20120101 |
| Evaluation of the performance of novel Aβ isoforms as theragnostic markers in Alzheimer's disease: from the cell to the patient. | Neuro-degenerative diseases 20120101 |
| Translatability scoring in drug development: eight case studies. | Journal of translational medicine 20120101 |
| Advances in the identification of γ-secretase inhibitors for the treatment of Alzheimer's disease. | Expert opinion on drug discovery 20120101 |
| Modulation of γ-secretase activity by multiple enzyme-substrate interactions: implications in pathogenesis of Alzheimer's disease. | PloS one 20120101 |
| Amyloid-β(1-15/16) as a marker for γ-secretase inhibition in Alzheimer's disease. | Journal of Alzheimer's disease : JAD 20120101 |
| γ-Secretase modulator in Alzheimer's disease: shifting the end. | Journal of Alzheimer's disease : JAD 20120101 |
| pPKCα-mediated effect on in vitro Aβ production in response to gamma secretase inhibitor LY411575 in rat CTXTNA2 astrocytes. | Journal of biological regulators and homeostatic agents 20120101 |
| Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors. | The Journal of pharmacology and experimental therapeutics 20111201 |
| [Gamma-secretase inhibitors and modulators]. | Nihon rinsho. Japanese journal of clinical medicine 20111201 |
| Drugs: a tangled web of targets. | Nature 20110713 |
| Prevalence of asymptomatic vasogenic edema in pretreatment Alzheimer's disease study cohorts from phase 3 trials of semagacestat and solanezumab. | Alzheimer's & dementia : the journal of the Alzheimer's Association 20110701 |
| What the halted phase III γ-secretase inhibitor trial may (or may not) be telling us. | Annals of neurology 20110201 |
| New pathway links γ-secretase to inflammation and memory while sparing notch. | Annals of neurology 20110101 |
| Validation of ELISA methods for quantification of total tau and phosporylated-tau181 in human cerebrospinal fluid with measurement in specimens from two Alzheimer's disease studies. | Journal of Alzheimer's disease : JAD 20110101 |
| BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells. | Journal of biomedical science 20110101 |
| Interacting with γ-secretase for treating Alzheimer's disease: from inhibition to modulation. | Current medicinal chemistry 20110101 |
| Genetics. Gamma-secretase and human disease. | Science (New York, N.Y.) 20101119 |
| What can be inferred from the interruption of the semagacestat trial for treatment of Alzheimer's disease? | Biological psychiatry 20101115 |
| Alzheimer's failure raises questions about disease-modifying strategies. | Nature reviews. Drug discovery 20101001 |
| NerveCenter: Phase III Alzheimer trial halted: Search for therapeutic biomarkers continues. | Annals of neurology 20101001 |
| ACS chemical neuroscience molecule spotlight on semagacestat (LY450139). | ACS chemical neuroscience 20100818 |
| [Progress in the development of anti-amyloid drugs for treatment of Alzheimer's disease.]. | Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20100701 |
| Disposition and metabolism of semagacestat, a {gamma}-secretase inhibitor, in humans. | Drug metabolism and disposition: the biological fate of chemicals 20100401 |
| In response to 'a gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system'. | Annals of neurology 20100101 |
| Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs. | Journal of Alzheimer's disease : JAD 20100101 |
| Use of theragnostic markers to select drugs for phase II/III trials for Alzheimer disease. | Alzheimer's research & therapy 20100101 |
| Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease. | Alzheimer's research & therapy 20100101 |
| Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. | Journal of medicinal chemistry 20091022 |
| Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo. | Journal of neurochemistry 20090901 |
| A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system. | Annals of neurology 20090701 |
| Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease. | Expert opinion on pharmacotherapy 20090701 |
| Semagacestat, a gamma-secretase inhibitor for the potential treatment of Alzheimer's disease. | Current opinion in investigational drugs (London, England : 2000) 20090701 |
| gamma-Secretase inhibitor reduces diet-induced atherosclerosis in apolipoprotein E-deficient mice. | Biochemical and biophysical research communications 20090529 |
| Committed neuronal precursors confer astrocytic potential on residual neural precursor cells. | Developmental cell 20090201 |
| Requirement of Notch activation during regeneration of the intestinal epithelia. | American journal of physiology. Gastrointestinal and liver physiology 20090101 |
| A small molecule inhibitor of signal peptide peptidase inhibits Plasmodium development in the liver and decreases malaria severity. | PloS one 20090101 |
| Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575. | Molecular neurodegeneration 20090101 |
| Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition. | The Journal of pharmacology and experimental therapeutics 20081101 |
| Notch1 and TGFbeta1 cooperatively regulate Foxp3 expression and the maintenance of peripheral regulatory T cells. | Blood 20080901 |
| Molecule of the month. Semagacestat. | Drug news & perspectives 20080901 |
| Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease. | Archives of neurology 20080801 |
| A multigram chemical synthesis of the gamma-secretase inhibitor LY411575 and its diastereoisomers. | Bioorganic & medicinal chemistry letters 20071115 |
| Epidermal growth factor receptor and notch pathways participate in the tumor suppressor function of gamma-secretase. | The Journal of biological chemistry 20071102 |
| Novel orally active, dibenzazepinone-based gamma-secretase inhibitors. | Bioorganic & medicinal chemistry letters 20071101 |
| Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations. | The Journal of biological chemistry 20070824 |
| Dominance of amyloid precursor protein sequence over host cell secretases in determining beta-amyloid profiles studies of interspecies variation and drug action by internally standardized immunoprecipitation/mass spectrometry. | The Journal of pharmacology and experimental therapeutics 20070301 |
| Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase. | Clinical neuropharmacology 20070101 |
| Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse. | The Journal of pharmacology and experimental therapeutics 20061201 |
| Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139. | The Journal of pharmacology and experimental therapeutics 20061101 |
| [The molecular mechanism of Notch-induced transformation and the therapeutic potential of its inhibitor]. | [Rinsho ketsueki] The Japanese journal of clinical hematology 20060701 |
| Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease. | Neurology 20060227 |
| Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide]. | The Journal of pharmacology and experimental therapeutics 20050501 |
| Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers. | Clinical neuropharmacology 20050101 |
| Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY-411575). | The Journal of pharmacology and experimental therapeutics 20040401 |