This is a list of investigational

antipsychotic Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but ...

s, or antipsychotics 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.''

Receptor modulators

Monoamine receptor modulators

* ATI-9242 –

atypical antipsychotic The atypical antipsychotics (AAP), also known as second generation antipsychotics (SGAs) and serotonin–dopamine antagonists (SDAs), are a group of antipsychotic drugs (antipsychotic drugs in general are also known as major tranquilizers and ne ...

( D₂ and 5-HT_2A receptor

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

, other actions) *

AVN-211 AVN-211 (CD-008-0173) is a drug which acts as a highly selective 5-HT6 receptor antagonist and is under development by Avineuro Pharmaceuticals for the treatment of schizophrenia. In early 2011, it successfully completed phase IIa clinical tr ...

(CD-008-0173) – 5-HT₆ receptor antagonist * Brilaroxazine (RP-5063, RP-5000; oxaripiprazole) – atypical antipsychotic (D₂ receptor partial agonist, 5-HT_2A receptor antagonist, other actions) * F-17464 – D₃ receptor antagonist, 5-HT_1A receptor

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

, and weak D₂ receptor partial agonist * FKF-02SC (TGOF-02N) – atypical antipsychotic (D₂ and 5-HT_2A receptor antagonist, other actions) * LB-102 – D_2,3, 5-HT₇, receptor antagonists (methylated version of

amisulpride Amisulpride is an antiemetic and antipsychotic medication used at lower doses intravenously to prevent and treat postoperative nausea and vomiting; and at higher doses by mouth to treat schizophrenia and acute psychotic episodes. It is sold und ...

) * Lu-AF35700 – D₁, 5-HT_2A, and 5-HT₆ receptor antagonist * Masupirdine (SUVN-502) – 5-HT₆ receptor antagonist *

Ralmitaront Ralmitaront (, ; developmental code names RG-7906 and RO-6889450) is an investigational antipsychotic drug which is undergoing clinical trials for the treatment of acute exacerbation of schizophrenia and schizoaffective disorder. It is a partia ...

(RG-7906, RO-6889450) –

TAAR1 Trace amine-associated receptor 1 (TAAR1) is a trace amine-associated receptor (TAAR) protein that in humans is encoded by the ''TAAR1'' gene. TAAR1 is an intracellular amine-activated and G protein-coupled receptor (GPCR) that is primarily exp ...

agonist * Ulotaront (SEP-856, SEP-363856) – 5-HT_1A receptor and

agonist * SUVN-D4010 – 5-HT₄ receptor partial agonist * TAK-058 (ENV-8058) – 5-HT₃ receptor antagonist

Glutamate receptor modulators

* Neboglamine (CR-2249, XY-2401; nebostinel) –

NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA rece ...

glycine-site

positive allosteric modulator In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to ...

* PF-4958242 – AMPA receptor positive allosteric modulator *

Pomaglumetad methionil Pomaglumetad (LY-404,039) is an amino acid analog drug that acts as a highly selective agonist for the metabotropic glutamate receptor group II subtypes Metabotropic glutamate receptor 2, mGluR2 and Metabotropic glutamate receptor 3, mGluR3. Phar ...

(DB-103, LY-2140023, LY-2812223) – mGluR₂ and mGluR₃ agonist

Acetylcholine receptor modulators

* APN-1125 – α₇

nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ne ...

partial agonist *

KarXT KarXT is an investigational oral dual-drug fixed-dose combination of xanomeline and Trospium chloride, trospium. It is undergoing a phase 3 clinical trial for the treatment of patients suffering from the symptoms of schizophrenia. Xanomeline is a ...

(

xanomeline Xanomeline (LY-246,708; Lumeron, Memcor) is a small molecule muscarinic acetylcholine receptor agonist that was first synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the treatme ...

/ trospium) – combined M₁ and M₄

muscarinic acetylcholine receptor Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end-rece ...

agonist and peripherally-selective

antagonist

Cannabinoid receptor modulators

* AX-1604 –

cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid recepto ...

modulator In electronics and telecommunications, modulation is the process of varying one or more properties of a periodic waveform, called the ''carrier signal'', with a separate signal called the ''modulation signal'' that typically contains informatio ...

(

phytocannabinoid Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tet ...

-based

chewing gum Chewing gum is a soft, cohesive substance designed to be chewed without being swallowed. Modern chewing gum is composed of gum base, sweeteners, softeners/plasticizers, flavors, colors, and, typically, a hard or powdered polyol coating. Its te ...

) *

Cannabidiol Cannabidiol (CBD) is a phytocannabinoid discovered in 1940. It is one of 113 identified cannabinoids in cannabis plants, along with tetrahydrocannabinol (THC), and accounts for up to 40% of the plant's extract. , clinical research on CBD incl ...

(CBD; GW-42003, GWP-42003, GWP-42003-P, ECP-012A; Arvisol, Epidiolex) – cannabinoid receptor modulator,

antioxidant Antioxidants are compounds that inhibit oxidation, a chemical reaction that can produce free radicals. This can lead to polymerization and other chain reactions. They are frequently added to industrial products, such as fuels and lubricant ...

, other actions

Other/mixed receptor modulators

Basmisanil Basmisanil (; developmental codes RG-1662 and RO5186582) is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairmen ...

(RG-1662, RO-5186582) – GABA_A receptor α₅ subunit-containing

negative allosteric modulator In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds t ...

* Deudextromethorphan (d-DM; AVP-786, CTP-786) – σ₁ receptor agonist,

serotonin–norepinephrine reuptake inhibitor Serotonin–norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant drugs used to treat major depressive disorder (MDD), anxiety disorders, obsessive–compulsive disorder (OCD), social phobia, attention-deficit hyperactivity dis ...

, uncompetitive

NMDA receptor antagonist NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor (NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce ...

, muscarinic acetylcholine receptor agonist, other actions *

Erteberel Erteberel (, ; former developmental code name LY-500307; also known as selective estrogen receptor beta agonist-1 or SERBA-1) is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and is under development by Eli Lilly for ...

(LY-500307, SERBA-1) –

ERβ Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen. In humans ERβ is encoded by ...

agonist *

Roluperidone Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity for ...

(CYR-101, MIN-101, MT-210) – 5-HT_2A and σ₂ receptor antagonist * TAK-041 – GPR139 receptor agonist

Enzyme inhibitors

* BI-409306 (SUB-166499) – phosphodiesterase 9A

inhibitor Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...

* Lu-AF11167 – dual phosphodiesterase 2A and 10A inhibitor * OMS-824 (OMS-643762) – phosphodiesterase 10A inhibitor *

Sodium benzoate Sodium benzoate is the sodium salt of benzoic acid, widely used as a food preservative (with an E number of E211) and a pickling agent. It appears as a white crystalline chemical with the formula C6H5COONa. Production Sodium benzoate is commo ...

(SND-11, SND-12, SND-13, SND-14; Clozaben, NaBen) – D-amino acid oxidase inhibitor * TAK-831 – D-amino acid oxidase inhibitor

Ion channel modulators

* AUT-00206 – shaw potassium channel modulator *

Evenamide Evenamide () (developmental code names NW-3509, NW-3509A) is a selective voltage-gated sodium channel blocker, including (and not limited to) subtypes Nav1.3, Nav1.7, and Nav1.8, which is described as an antipsychotic and is under development ...

(NW-3509; NW-3509A) – Na_v1.3, Na_v1.7, and Na_v1.8

voltage-gated sodium channel Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's membrane. They belong to the superfamily of cation channels and can be classified according to the trigger that opens the channel ...

blocker

Others

* ADE-615 – undefined mechanism of action * ADE-616 – undefined mechanism of action * AMG-581 – undefined mechanism of action * ASP-4345 – undefined mechanism of action * ASP-6981 – undefined mechanism of action * ATx11-004 – undefined mechanism of action * MK-8189 – undefined mechanism of action * PF-06266047 – undefined mechanism of action *

Pyridoxamine Pyridoxamine is one form of vitamin B6, vitamin B6. Chemically it is based on a pyridine ring structure, with hydroxyl, methyl, aminomethyl, and hydroxymethyl substituents. It differs from pyridoxine by the substituent at the 4-position. The hydro ...

(BST-4001, K-163, K-163SZ; Pyridorin) – vitamin B₆ analog, advanced glycosylation end-product inhibitor,

free radical A daughter category of ''Ageing'', this category deals only with the biological aspects of ageing. Ageing Ailments of unknown cause Biogerontology Biological processes Causes of death Cellular processes Gerontology Life extension Metabo ...

scavenger * TS-134 (TS-1341) – undefined mechanism of action

References

External links

AdisInsight – Springer

2016 Medicines in Development for Mental Health – PhRMA
{{Antipsychotics Antipsychotics Antipsychotics, investigational Experimental drugs