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Drugs of the Future
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Drugs Fut 2009, 34(1): 5
ISSN 0377-8282
Copyright 2009 Clarivate Analytics
CCC: 0377-8282
DOI: 10.1358/dof.2009.034.01.1324392
 
 
Almorexant
Owen, R.T., Castaner, R., Bolos, J., Estivill, C.
 
 
Almorexant is a novel, selective, orally active dual orexin OX1 and OX2 receptor antagonist. It is rapidly absorbed and distributed and shows no tendency to accumulate with repeated dosing. Preclinical studies in rats and dogs have demonstrated a sleep-promoting effect which resembles physiological sleep; this could be quickly reversed upon sensorimotor stimulation and yet allow resumption of sleep upon its cessation. Almorexant's sleep-promoting effects were confirmed in volunteers and patients with primary insomnia. It dose-dependently increased sleep efficiency and decreased sleep latency and wake time after sleep onset. The compound was well tolerated, with no significant effects on next-day motor performance, memory or reaction time.


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