Semagacestat

Structural formula
General
Non-proprietary name	Semagacestat
other names	(2 S ) -2-hydroxy-3-methyl- N - ((1 S ) -1-methyl-2 - {[(1 S ) -3-methyl-2-oxo-2,3,4,5- tetrahydro-1 H -3-benzazepin-1-yl] amino} -2-oxoethyl) butanamides N 2 - [2 ( S ) -Hydroxy-3-methylbutyryl] - N - [3-methyl-2-oxo-2,3,4,5-tetrahydro-1 H -3-benzazepin-1 ( S ) -yl ] - L -alaninamide
Molecular formula	C 19 H 27 N 3 O 4
External identifiers / databases
CAS number 425386-60-3 PubChem 9843750 ChemSpider 8019465 DrugBank DB12463 Wikidata Q426010
Drug information
Drug class	Alzheimer's drug
Mechanism of action	Gamma secretase inhibitor
properties
Molar mass	361.4 g · mol -1
safety instructions
GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Semagacestat is a potential drug from the group of γ-secretase inhibitors developed by Eli Lilly and Company , which is to be used in the therapy of Alzheimer's disease . After disappointing results from clinical studies on the effectiveness of Semagacestat, which showed that it was inferior to placebo and were therefore discontinued prematurely, further development of the active ingredient is suspended.

pharmacology

Mechanism of action

Semagacestat is a γ-secretase inhibitor . By inhibiting the γ-secretase - enzyme formation is β-amyloid from amyloid precursor protein suppressed, which in Alzheimer as deposit -patients in the brain occurs, and the function of the nerve cells affected. This leads to memory loss .

In animal experiments , a dose-dependent change in the β-amyloid concentration was demonstrated by Semagacestat. In the case of inefficient concentrations, increased concentrations of β-amyloid were found, while the administration of higher doses showed a concentration- dependent inhibition .

Pharmacokinetics

The substance is absorbed quickly , with maximum plasma levels being reached after 0.5 to 2 hours. Semagacestat has a plasma half-life of approximately 2.5 hours with a linear dose-response relationship .

literature

• Semagacestat. Drugs of the Future .34 (8): 613-617, 2009

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ^ Ledford H: Clinical trial disappoints . In: Nature . 466, 2010, p. 1031. doi : 10.1038 / 4661031a .