Neurology · 2006 · 294 citations · 5 references
MedicinePharmacologyPharmacotherapyClinical PharmacologyDementiaNeuropharmacologyAlzheimer DiseaseDementia PharmacotherapyDementia TreatmentEnzyme InhibitionNeurodegenerative Disease PharmacotherapyNeurodegenerative DiseasesAlzheimer's Disease PharmacokineticsGamma Secretase InhibitionPharmacological Treatment Of Dementia
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.
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Alzheimer-type neuropathology in transgenic mice overexpressing V717F β-amyloid precursor protein
Dora Games, David S. Adams, Ree Alessandrini et al. · Nature · 1995 · 2.5K citations
Gwendolyn T. Wong, Denise Manfra, Frederique M. Poulet et al. · Journal of Biological Chemistry · 2004 · 716 citations · Full text