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.

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 .