This is a list of investigational

sleep Sleep is a sedentary state of mind and body. It is characterized by altered consciousness, relatively inhibited sensory activity, reduced muscle activity and reduced interactions with surroundings. It is distinguished from wakefulness by a de ...

drug A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...

s, or drugs for the treatment of

sleep disorder A sleep disorder, or somnipathy, is a medical disorder of an individual's sleep patterns. Some sleep disorders are severe enough to interfere with normal physical, mental, social and emotional functioning. Polysomnography and actigraphy are test ...

s 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

*

Lorediplon Lorediplon (INN) is a nonbenzodiazepine of the pyrazolopyrimidine family that is being pursued as a treatment for insomnia but has not completed development. See also * List of investigational sleep drugs This is a list of investigational sleep ...

(GF-015535-00) – GABA_A receptor positive allosteric modulato

*

Zuranolone Zuranolone (; developmental code names SAGE-217, S-812217) is an investigational medication which is under development by SAGE Therapeutics for the treatment of depressive disorders and a variety of other indications. It is a synthetic, orally ...

(SAGE-217) – GABA_A receptor positive allosteric modulato

Orexin receptor antagonists

Seltorexant Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin receptor antagonist, orexin antagonist medication which is under development for the treatment of depression (mood), depression and insomnia. It is a b ...

(MIN-202, JNJ,42847922, JNJ-922) – selective OX₂ receptor antagonis

*

Vornorexant Vornorexant, also known by its developmental code names ORN-0829 and TS-142, is an orexin antagonist medication which is under development for the treatment of insomnia Insomnia, also known as sleeplessness, is a sleep disorder in which peo ...

(ORN-0829, TS-142) – dual OX₁ and OX₂ receptor antagonis

Melatonin receptor agonists

Piromelatine Piromelatine (Neu-P11) is a multimodal sleep drug under development by Neurim Pharmaceuticals. It is an agonist at melatonin MT1/ MT2 and serotonin 5-HT1A/ 5-HT1D receptors. Neurim is conducting a phase II randomized, placebo controlled trial ...

(Neu-P11) –

melatonin receptor Melatonin receptors are G protein-coupled receptors (GPCR) which bind melatonin. Three types of melatonin receptors have been cloned. The MT1 (or Mel1A or MTNR1A) and MT2 (or Mel1B or MTNR1B) receptor subtypes are present in humans and other ma ...

agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...

and 5-HT_1A and 5-HT_1D receptor agonis

Nociceptin receptor agonists

* Sunobinop (IMB-115, IT-1315, S-117957, V-117957) –

nociceptin receptor The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the ''OPRL1'' (opioid receptor-like 1) gene. The nociceptin receptor ...

agonis

https://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

Danavorexton Danavorexton (developmental code name TAK-925) is a selective orexin 2 receptor agonist. It is a small-molecule compound and is administered intravenously. The compound was found to dose-dependently produce wakefulness to a similar degree as ...

(TAK-925) – OX₂ receptor-selective agonist via

IV infusion Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrie ...

TAK-994 TAK-994 is an orexin receptor agonist which is under development by Takeda for the treatment of narcolepsy. It is a small-molecule and orally active compound and acts as a highly selective agonist of the orexin receptor 2 (OX2) (>700-fold selec ...

– OX₂ receptor agonist pill ( orally available)

Monoaminergics

* Flecainide/modafinil (THN-102) –

modafinil Modafinil, sold under the brand name Provigil among others, is a central nervous system (CNS) stimulant medication used to treat sleepiness due to narcolepsy, shift work sleep disorder, and obstructive sleep apnea. While it has seen off-label ...

(

dopamine reuptake inhibitor A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopa ...

) and

flecainide Flecainide is a medication used to prevent and treat abnormally fast heart rates. This includes ventricular and supraventricular tachycardias. Its use is only recommended in those with dangerous arrhythmias or when significant symptoms cannot b ...

(

antiarrhythmic Antiarrhythmic agents, also known as cardiac dysrhythmia medications, are a group of pharmaceuticals that are used to suppress abnormally fast rhythms ( tachycardias), such as atrial fibrillation, supraventricular tachycardia and ventricular tac ...

) combinatio

*

Mazindol Mazindol (brand names Mazanor, Sanorex) is a stimulant drug which is used as an appetite suppressant. It was developed by Sandoz Laboratories, Sandoz-Wander in the 1960s. Medical uses Mazindol is used in short-term (i.e., a few weeks) treatment ...

controlled release (NLS-1001, NLS-1) –

norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', ...

-predominant

serotonin–norepinephrine–dopamine reuptake inhibitor A serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI), also known as a triple reuptake inhibitor (TRI), is a type of drug that acts as a combined reuptake inhibitor of the monoamine neurotransmitters serotonin, norepinephrine, and ...

(SNDR

*

Reboxetine Reboxetine, sold under the brand name Edronax among others, is a drug of the norepinephrine reuptake inhibitor (NRI) class, marketed as an antidepressant by Pfizer for use in the treatment of major depression, although it has also been used off-l ...

(AXS-12) –

norepinephrine reuptake inhibitor A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epineph ...

(NRI

GHB receptor agonists

* FT-218 (

sodium oxybate Sodium oxybate, sold under the brand name Xyrem among others, is a medication used to treat two symptoms of narcolepsy: sudden muscle weakness and excessive daytime sleepiness. It is used sometimes in France and Italy as an anesthetic given i ...

controlled release) –

GHB ''gamma''-Hydroxybutyric acid (or γ-hydroxybutyric acid (GHB), also known as 4-hydroxybutanoic acid) is a naturally occurring neurotransmitter and a depressant drug. It is a precursor to GABA, glutamate, and glycine in certain brain areas. ...

and GABA_B receptor agonis

GABA_A receptor inhibitors

Pentylenetetrazole Pentylenetetrazol, also known as pentylenetetrazole, leptazol, metrazol, pentetrazol (INN), pentamethylenetetrazol, Corazol, Cardiazol, Deumacard, or PTZ, is a drug formerly used as a circulatory and respiratory stimulant. High doses cause convuls ...

(BTD-001) – GABA_A receptor negative allosteric modulato

References

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