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
GABAA receptor potentiators
- EVT-201 – GABAA receptor positive allosteric modulator[1]
- Lorediplon (GF-015535-00) – GABAA receptor positive allosteric modulator [2]
- Zuranolone (SAGE-217) – GABAA 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-HT1A and 5-HT1D 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]
GABAA receptor inhibitors
- Pentylenetetrazole (BTD-001) – GABAA receptor negative allosteric modulator [16]
See also
References
- ^ "ALKS 2680". AdisInsight. 7 June 2024. Retrieved 31 July 2024.
- ^ a b "Takeda". www.ox2rsparkleprogram.com. Retrieved 2019-11-15.
- ^ "E-2086". AdisInsight. 15 July 2024. Retrieved 31 July 2024.
- ^ 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.
- v
- t
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positive modulators
- Benzodiazepines: Brotizolam
- Cinolazepam
- Climazolam
- Clorazepate
- Doxefazepam
- Estazolam
- Etizolam
- Flunitrazepam
- Flurazepam
- Flutoprazepam
- Haloxazolam
- Loprazolam
- Lormetazepam
- Midazolam
- Nimetazepam
- Nitrazepam
- Quazepam
- Temazepam
- Triazolam
- Others: Alcohols (e.g., ethchlorvynol, amylene hydrate, ethanol)
- Barbiturates (e.g., amobarbital, pentobarbital, phenobarbital, secobarbital)
- Bromides (e.g., potassium bromide, sodium bromide)
- Carbamates (e.g., meprobamate)
- Chloral hydrate
- Clomethiazole
- Kava
- Neurosteroids (e.g., progesterone, zuranolone†)
- Paraldehyde
- Piperidinediones (e.g., glutethimide)
- Quinazolinones (e.g., methaqualone)
- Sulfonmethane
- Valerian
inverse agonists)
- Alimemazine
- Captodiame
- Dimenhydrinate
- Diphenhydramine
- Doxylamine
- Etodroxizine
- Hydroxyzine
- Meclizine
- Methapyrilene
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Promethazine
- Propiomazine
- Pyrilamine
- Tricyclic antidepressants (e.g., amitriptyline, doxepin, trimipramine)
- Tetracyclic antidepressants (e.g., mirtazapine)
- Triprolidine
- Melatonin
- Ramelteon
- Tasimelteon
- Antipsychotics (e.g., quetiapine, olanzapine, risperidone, chlorpromazine)
- Ashwagandha
- Benzoctamine
- Cannabinoids (e.g., cannabis, dronabinol (THC), nabilone)
- Chamomile
- Fenadiazole
- Gabapentinoids (e.g., gabapentin, pregabalin, phenibut)
- Hops
- Lavender
- Menthyl isovalerate
- Niaprazine
- Opioids (e.g., hydrocodone, oxycodone, morphine)
- Passion flower
- Scopolamine
- Serotonin precursors (tryptophan, 5-HTPTooltip 5-hydroxytryptophan)
- Sodium oxybate (GHB)
- Sympatholytics (e.g., clonidine, guanfacine, prazosin)
- Theanine
- Trazodone
- Tricyclic antidepressants (e.g., amitriptyline, doxepin, trimipramine)
- Tetracyclic antidepressants (e.g., mirtazapine)
- Valnoctamide
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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