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PMID: 16505324 Published · ppublish English Comparative Study Journal Article Randomized Controlled Trial Research Support, Non-U.S. Gov't

Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease.

Neurology ·Vol. 66 ·No. 4 ·2006-02-28 ·Pages 602-4

Siemers ER, Quinn JF, Kaye J, Farlow MR, Porsteinsson A, Tariot P, Zoulnouni P, Galvin JE, Holtzman DM, Knopman DS, Satterwhite J, Gonzales C, Dean RA, May PC

Abstract

LY450139 dihydrate, a gamma-secretase inhibitor, was studied in a randomized, controlled trial of 70 patients with Alzheimer disease. Subjects were given 30 mg for 1 week followed by 40 mg for 5 weeks. Treatment was well tolerated. Abeta(1-40) in plasma decreased by 38.2%; in CSF, Abeta(1-40) decreased by 4.42 +/- 9.55% (p = not significant). Higher drug doses may result in additional decreases in plasma Abeta concentrations and a measurable decrease in CSF Abeta.

MeSH Terms
Alanine/analogs & derivatives,pharmacokinetics,therapeutic use Alzheimer Disease/drug therapy Amyloid Precursor Protein Secretases Aspartic Acid Endopeptidases Azepines/pharmacokinetics,therapeutic use Endopeptidases/metabolism Enzyme Inhibitors/pharmacokinetics,therapeutic use Humans Placebos
Chemicals
Azepines Enzyme Inhibitors 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 Placebos Amyloid Precursor Protein Secretases Endopeptidases Aspartic Acid Endopeptidases BACE1 protein, human Alanine
Authors & Affiliations
14 authors, click to expand affiliations / ORCID
Siemers E R
Eli Lilly and Company, Indianapolis, IN 46085, USA. [email protected]
Quinn J F
Kaye J
Farlow M R
Porsteinsson A
Tariot P
Zoulnouni P
Galvin J E
Holtzman D M
Knopman D S
Satterwhite J
Gonzales C
Dean R A
May P C
Article Info
Journal
Neurology
Abbr.
Neurology
ISSN
1526-632X
DOI
10.1212/01.WNL.0000198762.41312.E1
Email
[email protected]
Published
2006-02-28
Pages
602-4
Language
English
Region
United States
NLM ID
0401060
Subset
IM
External Links
PubMed source DOI: 10.1212/01.WNL.0000198762.41312.E1 View journal details
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