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[1]
• Lorediplon (GF-015535-00) – GABA_A receptor positive allosteric modulator[2]
• Remimazolam (HR-7056) – GABA_A receptor positive allosteric modulator[3]
• SAGE-217 – GABA_A receptor positive allosteric modulator[4]

Orexin receptor antagonists

• Filorexant (MK-6096) – orexin receptor antagonist[5]
• Lemborexant (E-2006, LEM-10, LEM-5) – orexin receptor antagonist[6]
• Nemorexant (ACT-541468) – orexin receptor antagonist[7]
• Seltorexant (MIN-202, JNJ,42847922, JNJ-922) – selective OX₂ receptor antagonist[8]

Melatonin receptor agonists

• Piromelatine (Neu-P11) – melatonin receptor agonist and 5-HT_1A and 5-HT_1D receptor agonist[9]

Others/undefined

• Brexpiprazole (Lu AF41156, OPC-34712; Rexulti) – atypical antipsychotic / complex mechanism of action[10]
• Lumateperone (ITI-007, ITI-722) – atypical antipsychotic / complex mechanism of action[11]
• S-117957 (V-117957) – undefined mechanism of action[12]

Hypersomnia/narcolepsy

Monoaminergics

• Flecainide/modafinil (THN-102) – modafinil (dopamine reuptake inhibitor) and flecainide (antiarrhythmic) combination[13]
• JZP-507 – dopamine receptor agonist[14]
• Mazindol controlled release (NLS-1001, NLS-1) – norepinephrine-predominant serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI)[15]
• Phacetoperane (NLS-3) – norepinephrine–dopamine reuptake inhibitor (NDRI)[16]
• Solriamfetol (JZP-110, ADX-N05) – weak NDRI[17]

GHB receptor agonists

• FT-218 (sodium oxybate controlled release) – GHB and GABA_B receptor agonist[18]
• JZP-258 (oxybate mixed salt solution) – GHB and GABA_B receptor agonist[19]
• JZP-386 (C-10323; deuterated sodium oxybate) – GHB and GABA_B receptor agonist [20]
• JZP-507 (oxybate mixed salt solution) – GHB and GABA_B receptor agonist[21]

H₃ receptor inverse agonists

• LGD-3437 – H₃ receptor antagonist[22]
• Pitolisant (Wakix; BF2.649) – H₃ receptor inverse agonist[23]

GABA_A receptor inhibitors

• GR-3027 – GABA_A receptor negative allosteric modulator[24]
• Pentylenetetrazole (BTD-001) – GABA_A receptor negative allosteric modulator[25]

Others/undefined

• TS-091 (TS-0911) – undefined mechanism of action[26]

See also

• List of investigational drugs

External links

• AdisInsight – Springer