List of investigational sleep drugs

This is a dynamic list and may never be able to satisfy particular standards for completeness. You can help by adding missing items with reliable sources.

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.

This list was last comprehensively updated sometime between June 2017 and August 2021. It is likely to become outdated with time.

Insomnia

GABA_A receptor potentiators

• EVT-201 – GABA_A receptor positive allosteric modulator[1]
• Lorediplon (GF-015535-00) – GABA_A receptor positive allosteric modulator [2]
• Zuranolone (SAGE-217) – GABA_A receptor positive allosteric modulator [3]

Orexin receptor antagonists

• Seltorexant (MIN-202, JNJ,42847922, JNJ-922) – selective OX₂ receptor antagonist [4]
• Vornorexant (ORN-0829, TS-142) – dual OX₁ and OX₂ receptor antagonist [5]

Melatonin receptor agonists

• Piromelatine (Neu-P11) – melatonin receptor agonist and 5-HT_1A and 5-HT_1D receptor agonist [6]

Nociceptin receptor agonists

• Sunobinop (IMB-115, IT-1315, S-117957, V-117957) – nociceptin receptor agonist [7][8]

Hypersomnia/narcolepsy

Orexin receptor agonists

• ALKS-2680 – selective OX₂ receptor agonist[1]
• Danavorexton (TAK-925) – selective OX₂ receptor agonist via IV infusion[2][9]
• E-2086 – selective OX₂ receptor agonist[3]
• Firazorexton (TAK-994) – OX₂ receptor agonist pill (orally available)[10][2]
• Suntinorexton (TAK-861) – selective OX₂ receptor agonist (orally available) [11][4]

Monoaminergics

• Flecainide/modafinil (THN-102) – modafinil (dopamine reuptake inhibitor) and flecainide (antiarrhythmic) combination [12]
• Mazindol controlled release (NLS-1001, NLS-1) – norepinephrine-predominant serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI)[13]
• Reboxetine (AXS-12) – norepinephrine reuptake inhibitor (NRI) [14]

GHB receptor agonists

H₃ receptor inverse agonists

• Samelisant (SUVN-G3031) – H₃ receptor antagonist [15]

GABA_A receptor inhibitors

• Pentylenetetrazole (BTD-001) – GABA_A receptor negative allosteric modulator [16]

See also

• List of investigational drugs

References

1. "ALKS 2680". AdisInsight. 7 June 2024. Retrieved 31 July 2024.
2. "Takeda". www.ox2rsparkleprogram.com. Retrieved 2019-11-15.
3. "E-2086". AdisInsight. 15 July 2024. Retrieved 31 July 2024.
4. Konofal, Eric (2024). "From past to future: 50 years of pharmacological interventions to treat narcolepsy". Pharmacology Biochemistry and Behavior. 241: 173804. doi:10.1016/j.pbb.2024.173804.