List of investigational sleep drugs
This is a list of investigational sleep drugs, or drugs for the treatment of sleep disorders that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.
Insomnia
GABAA receptor potentiators
- EVT-201 – GABAA receptor positive allosteric modulator
- Lorediplon (GF-015535-00) – GABAA receptor positive allosteric modulator
- Remimazolam (HR-7056) – GABAA receptor positive allosteric modulator
- Zuranolone (SAGE-217) – GABAA receptor positive allosteric modulator
Orexin receptor antagonists
- Filorexant (MK-6096) – orexin receptor antagonist
- Lemborexant (E-2006, LEM-10, LEM-5) – orexin receptor antagonist
- Nemorexant (ACT-541468) – orexin receptor antagonist
- Seltorexant (MIN-202, JNJ,42847922, JNJ-922) – selective OX2 receptor antagonist
Melatonin receptor agonists
- Piromelatine (Neu-P11) – melatonin receptor agonist and 5-HT1A and 5-HT1D receptor agonist
Others/undefined
- Brexpiprazole (Lu AF41156, OPC-34712; Rexulti) – atypical antipsychotic / complex mechanism of action
- Lumateperone (ITI-007, ITI-722) – atypical antipsychotic / complex mechanism of action
- S-117957 (V-117957) – undefined mechanism of action
Hypersomnia/narcolepsy
Orexin receptor agonists
- TAK-925 – OX2 receptor-selective agonist via IV infusion [1]
- TAK-994 – OX2 receptor agonist pill (orally available) [1]
Monoaminergics
- Flecainide/modafinil (THN-102) – modafinil (dopamine reuptake inhibitor) and flecainide (antiarrhythmic) combination
- JZP-507 – dopamine receptor agonist
- Mazindol controlled release (NLS-1001, NLS-1) – norepinephrine-predominant serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI)
- Phacetoperane (NLS-3) – norepinephrine–dopamine reuptake inhibitor (NDRI)
GHB receptor agonists
- FT-218 (sodium oxybate controlled release) – GHB and GABAB receptor agonist
- JZP-258 (oxybate mixed salt solution) – GHB and GABAB receptor agonist
- JZP-386 (C-10323; deuterated sodium oxybate) – GHB and GABAB receptor agonist
- JZP-507 (oxybate mixed salt solution) – GHB and GABAB receptor agonist
GABAA receptor inhibitors
- Golexanolone – GABAA receptor negative allosteric modulator
- Pentylenetetrazole (BTD-001) – GABAA receptor negative allosteric modulator
See also
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