List of investigational sleep drugs explained

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 It is likely to become outdated with time.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 modulatorhttp://adisinsight.springer.com/drugs/800023883
• Lorediplon (GF-015535-00) GABA_A receptor positive allosteric modulator http://adisinsight.springer.com/drugs/800029512

• Zuranolone (SAGE-217) GABA_A receptor positive allosteric modulator http://adisinsight.springer.com/drugs/800043382

Orexin receptor antagonists

• Seltorexant (MIN-202, JNJ,42847922, JNJ-922) selective OX₂ receptor antagonist http://adisinsight.springer.com/drugs/800040115
• Vornorexant (ORN-0829, TS-142) dual OX₁ and OX₂ receptor antagonist https://adisinsight.springer.com/drugs/800049420

Melatonin receptor agonists

• Piromelatine (Neu-P11) melatonin receptor agonist and 5-HT_1A and 5-HT_1D receptor agonist http://adisinsight.springer.com/drugs/800032086

Nociceptin receptor agonists

• Sunobinop (IMB-115, IT-1315, S-117957, V-117957) nociceptin receptor agonist https://adisinsight.springer.com/drugs/800035863https://www.imbriumthera.com/news/imbrium-therapeutics-announces-first-patient-dosed-in-phase-2-study-of-potential-first-in-class-molecule-for-insomnia-associated-with-alcohol-cessation/

Hypersomnia/narcolepsy

Orexin receptor agonists

• ALKS-2680 – selective OX₂ receptor agonist^[1]
• Danavorexton (TAK-925) selective OX₂ receptor agonist via IV infusion^[2] https://adisinsight.springer.com/drugs/800050631
• E-2086 – selective OX₂ receptor agonist^[3]
• Firazorexton (TAK-994) OX₂ receptor agonist pill (orally available)https://adisinsight.springer.com/drugs/800054722
• Suntinorexton (TAK-861) selective OX₂ receptor agonist (orally available) https://adisinsight.springer.com/drugs/800063888^[4]

Monoaminergics

• Flecainide/modafinil (THN-102) modafinil (dopamine reuptake inhibitor) and flecainide (antiarrhythmic) combination http://adisinsight.springer.com/drugs/800045045

• Mazindol controlled release (NLS-1001, NLS-1) norepinephrine-predominant serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI)http://adisinsight.springer.com/drugs/800041870
• Reboxetine (AXS-12) norepinephrine reuptake inhibitor (NRI) https://adisinsight.springer.com/drugs/800053169

H₃ receptor inverse agonists

• Samelisant (SUVN-G3031) – H₃ receptor antagonist https://adisinsight.springer.com/drugs/800032317

GABA_A receptor inhibitors

• Pentylenetetrazole (BTD-001) GABA_A receptor negative allosteric modulator http://adisinsight.springer.com/drugs/800038901

See also

• List of investigational drugs

Notes and References

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