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

Siemers, E R; 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.

Neurology ; 66(4): 602-4, 2006 Feb 28.

Article in English | MEDLINE | ID: mdl-16505324

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.

Subject(s)

Alanine/analogs & derivatives , Alzheimer Disease/drug therapy , Azepines/therapeutic use , Endopeptidases/metabolism , Alanine/pharmacokinetics , Alanine/therapeutic use , Amyloid Precursor Protein Secretases , Aspartic Acid Endopeptidases , Azepines/pharmacokinetics , Enzyme Inhibitors/pharmacokinetics , Enzyme Inhibitors/therapeutic use , Humans , Placebos

ABSTRACT

Subject(s)

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