Lemborexant is a dual orexin antagonist indicated for the treatment of sleep-onset and/or sleep maintenance insomnia. Recent research in the field of sleep disorders has revealed that insomnia is likely driven not by the inability of the brain to "switch on" sleep-related circuits, but rather an inability to "switch-off" wake-promoting circuits.
- Mechanism
- Curator reviewed · 3 references
The orexin neuropeptide signaling system is involved in many physiologic functions, including sleep/wake control. Orexin-A and orexin-B activate post-synaptic G-protein coupled orexin-1 receptors (OX1R) and orexin-2 receptors (OX2R), which are found on neurons in the hypothalamus that project to numerous wake-controlling nuclei. Each receptor carries slightly different activity - activation of OX1R appears to suppress the onset of rapid eye movement (REM) sleep, whereas activation of OX2R appears to suppress non-REM sleep.
Lemborexant is an competitive antagonist of OX1R and OX2R. By blocking the binding of wake-promoting orexin-A and -B at these receptors, lemborexant suppresses the wake-drive, thereby promoting sleep.
- Primary indication
- Lemborexant is indicated for the treatment of adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance.Curator reviewed · 1 structured indication
- Formula / weight
- C22H20F2N4O2 · 410.425 g/mol (avg)
- First approval
- Canada, 2020 · United States, 2020
- Code names
- E-2006
- Brand names
Resolves to
MUGXRYIUWFITCP-PGRDOPGGSA-NSMILESCC1=NC=C(OC[C@]2(C[C@H]2C(=O)NC2=NC=C(F)C=C2)C2=CC=CC(F)=C2)C(C)=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Lemborexant, and which of those have an active Phase 3 trial?
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