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

GABA_A receptor potentiators

• EVT-201 – GABA_A receptor positive allosteric modulator
• Lorediplon (GF-015535-00) – GABA_A receptor positive allosteric modulator
• Remimazolam (HR-7056) – GABA_A receptor positive allosteric modulator
• Zuranolone (SAGE-217) – GABA_A receptor positive allosteric modulator

Orexin receptor antagonists

• Daridorexant (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-HT_1A and 5-HT_1D receptor agonist

Others/undefined

• IMB-115 (V-117957) – novel mechanism of action (ORL-1 agonist)

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)
• (r)-phenylpiracetam - dopamine reuptake inhibitor
• AXS-12 (Reboxetine) - norepinephrine reuptake inhibitor (NRI) for cataplexy

GHB receptor agonists

• FT-218 (sodium oxybate controlled release) – GHB and GABA_B receptor agonist
• JZP-258 (oxybate mixed salt solution) – GHB and GABA_B receptor agonist
• JZP-386 (C-10323; deuterated sodium oxybate) – GHB and GABA_B receptor agonist
• JZP-507 (oxybate mixed salt solution) – GHB and GABA_B receptor agonist

H₃ receptor inverse agonists

• LGD-3437 – H₃ receptor antagonist

GABA_A receptor inhibitors

• Golexanolone – GABA_A receptor negative allosteric modulator
• Pentylenetetrazole (BTD-001) – GABA_A receptor negative allosteric modulator
• GR3027 - an antagonist at GABAA receptors (GABAARs)

Others/undefined

• TS-091 (TS-0911) – undefined mechanism of action

See also

• List of investigational drugs

References

1. "Takeda". www.ox2rsparkleprogram.com. Retrieved 2019-11-15.