The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders.
ChemMedChem
; 15(23): 2286-2305, 2020 12 03.
Article
em En
| MEDLINE
| ID: mdl-32937014
ABSTRACT
Since its discovery in 1998, the orexin system has been of interest to the research community as a potential therapeutic target for the treatment of sleep/wake disorders, stress and anxiety disorders, addiction or eating disorders. It consists of two G protein-coupled receptors, the orexin 1 and orexin 2 receptors, and two neuropeptides with agonistic effects, the orexin A and orexin B peptides. Herein we describe our efforts leading to the identification of a promising set of dual orexin receptor antagonists (DORAs) which subsequently went through physiology-based pharmacokinetic and pharmacodynamic modelling>[1] and finally led to the selection of daridorexant, currently in phase 3 clinical trials for the treatment of insomnia disorders.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Receptores de Orexina
/
Antagonistas dos Receptores de Orexina
/
Imidazóis
/
Distúrbios do Início e da Manutenção do Sono
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article