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
GABAA receptor potentiators
*
EVT-201 –
GABAA 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 OX
2 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 OX
1 and OX
2 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-HT1A and
5-HT1D 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 GABAB receptor agonis
GABAA 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) – GABAA receptor negative allosteric modulato
See also
* List of investigational drugs
These are lists of investigational drugs:
* List of investigational analgesics
* List of investigational antidepressants
* List of investigational antipsychotics
* List of investigational anxiolytics
* List of investigational attention deficit h ...
References
{{Portal bar , Medicine
Experimental drugs
Hypnotics
Sleep drugs, investigational
Sedatives
Stimulants