ACS chemical neuroscience molecule spotlight on semagacestat (LY450139)

ACS Chem Neurosci. 2010 Aug 18;1(8):533-4. doi: 10.1021/cn1000606.

Abstract

Semagacestat (LY450139) is a novel γ-secretase inhibitor currently in late-stage development by Eli Lilly and Company as a potential treatment for Alzheimer's disease (AD). Semagacestat is currently being studied in two phase III clinical trials.

Keywords: AD; Alzheimer’s disease; Gamma-secretase; LY450139; neurodegeneration; semagacestat.

MeSH terms

  • Alanine / adverse effects
  • Alanine / analogs & derivatives*
  • Alanine / chemistry
  • Alanine / pharmacology
  • Alanine / therapeutic use
  • Alzheimer Disease / drug therapy
  • Alzheimer Disease / metabolism
  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Amyloid Precursor Protein Secretases / physiology
  • Amyloid beta-Peptides / blood
  • Amyloid beta-Peptides / cerebrospinal fluid
  • Amyloid beta-Protein Precursor / metabolism
  • Azepines* / adverse effects
  • Azepines* / chemistry
  • Azepines* / pharmacology
  • Azepines* / therapeutic use
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Humans
  • Molecular Structure
  • Multicenter Studies as Topic
  • Neuroprotective Agents* / adverse effects
  • Neuroprotective Agents* / chemistry
  • Neuroprotective Agents* / pharmacology
  • Neuroprotective Agents* / therapeutic use
  • Peptide Fragments / blood
  • Peptide Fragments / cerebrospinal fluid
  • Protein Processing, Post-Translational
  • Receptors, Notch / antagonists & inhibitors
  • Receptors, Notch / physiology
  • Signal Transduction / drug effects

Substances

  • Amyloid beta-Peptides
  • Amyloid beta-Protein Precursor
  • Azepines
  • 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
  • Neuroprotective Agents
  • Peptide Fragments
  • Receptors, Notch
  • amyloid beta-protein (1-40)
  • Amyloid Precursor Protein Secretases
  • Alanine