Semagacestat

• (2S)-2-hydroxy-3-methyl-N-((1S)-1-methyl-2-{[(1S)-3-methyl-2-oxo-2,3,4,5-tetrahydro-1H-3-benzazepin-1-yl]amino}-2-oxoethyl)butanamide
• N2-[2(S)-Hydroxy-3-methylbutyryl]-N-[3-methyl-2-oxo-2,3,4,5-tetrahydro-1H-3-benzazepin-1(S)-yl]-L-alaninamid

Alzheimer's drug

Gamma -secretase inhibitor

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Semagacestat is developed by Eli Lilly and Company potential drug is selected from the group of γ -secretase inhibitors, which is to be used in the treatment of Alzheimer's disease. After disappointing results from clinical studies on the effectiveness of Semagacestat which showed inferiority to placebo and were therefore terminated prematurely, rests the further development of the drug.

Pharmacology

Mechanism of Action

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

In animal studies, a dose- dependent change in the β - amyloid levels by Semagacestat was detected. In subeffizienten concentrations showed elevated levels of β -amyloid, whereas higher doses a concentration-dependent inhibition was observed.

Pharmacokinetics

The substance is rapidly absorbed (Tmax = 0.5-2 h) and has a plasma half -life of about 2.5 hours with a linear relationship to the dose -response curve.