Semagacestat

Drugbox
IUPAC_name = (2S)-Hydroxy-3-methyl-N- [(1S)-1-methyl-2-oxo-2- [(1S)-2,3,4,5,-tetrahydro-3-methyl-2-oxo-1H-3-benzazepin-1-yl] amino] ethyl] -butanamide

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chemical_formula =
C=19 | H=27 | N=3 | O=4
molecular_weight = 361.434 g/mol
smiles = c12ccccc2CCN(C)C(=O)C1NC(=O)C(C)NC(=O)C(O)C(C)C
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Semagacestat is a candidate drug for a causal therapy against Alzheimer's disease. as of|2008, it is undergoing a Phase III clinical trial, the IDENTITY study, including 1500 patients from 22 countries. It is produced by Eli Lilly and Elan (USA).

Method of action

β-Amyloid is a peptide that is the main constituent of amyloid plaques in the brains of Alzheimer's disease patients. It is formed by proteolysis of APP. Research on laboratory rats suggest that the soluble form of this peptide is a causative agent in the development of Alzheimer's.

Semagacestat blocks the enzyme γ-Secretase which is responsible for APP proteolysis.

References

* cite journal
author = H. Spreitzer
date = July 21, 2008
title = Neue Wirkstoffe - Semagacestat
journal = Österreichische Apothekerzeitung
issue = 15/2008
pages = 780
language = German
* [http://www.prous.com/molecules/default.asp?ID=174 Prous Science: Molecule of the Month July 2008]