Seltorexant is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist under development for the treatment of major depressive disorder (MDD) and insomnia.
In clinical trials, seltorexant has demonstrated significant improvements in depression scores on the Hamilton Depression Rating Scale (HDRS 17) in patients with MDD, particularly in those with higher baseline insomnia severity. It has also shown efficacy in improving sleep onset, total sleep time, and sleep efficiency in individuals with MDD and/or insomnia. The drug’s antidepressant effects are more pronounced in patients with moderate to severe insomnia symptoms, and it has been found to normalize the cortisol waking response, which is often elevated in MDD patients.
Currently, seltorexant is in Phase 3 clinical trials for MDD and Phase 2 trials for insomnia. Janssen Research & Development and Minerva Neurosciences are collaborating on its development. The drug’s unique mechanism of action, targeting the orexin-2 receptor, distinguishes it from other orexin receptor antagonists like suvorexant, lemborexant, and daridorexant, which are dual orexin receptor antagonists (DORAs). Seltorexant’s potential to address both depressive symptoms and sleep disturbances makes it a promising therapeutic option for patients with MDD.
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| Other Names | JNJ-42847922 |
|---|---|
| IUPAC Name | [2-(4, 6-dimethylpyrimidin-2-yl)-1, 3, 3a, 4, 6, 6a-hexahydropyrrolo[3, 4-c]pyrrol-5-yl]-[2-fluoro-6-(triazol-2-yl)phenyl]methanone |
| CAS | 1293281-49-8 |
| Molecular Weight | 407.4 |
| Molecular Formula | C21H22FN7O |
| SMILES | CC1=CC(=NC(=N1)N2CC3CN(CC3C2)C(=O)C4=C(C=CC=C4F)N5N=CC=N5)C |