List of investigational antipsychotics

This is a list of investigational antipsychotics, 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[edit]

Monoamine receptor modulators[edit]

Brilaroxazine (RP-5063, RP-5000; oxaripiprazole) – atypical antipsychotic (D₂ receptor partial agonist, 5-HT_2A receptor antagonist, other actions)^[1]
FKF-02SC (TGOF-02N) – atypical antipsychotic (D₂ and 5-HT_2A receptor antagonist, other actions)^[2]
Masupirdine (SUVN-502) – 5-HT₆ receptor antagonist^[3]
N-methyl amisulpride (LB-102) – D_2,3, 5-HT₇, receptor antagonists (methylated version of amisulpride) ^[4]
Ralmitaront (RG-7906, RO-6889450) – TAAR1 agonist^[5]
Ulotaront (SEP-856, SEP-363856) – 5-HT_1A receptor and TAAR1 agonist^[6]
Usmarapride (SUVN-D4010) – 5-HT₄ receptor partial agonist^[7]

Glutamate receptor modulators[edit]

Pomaglumetad methionil (DB-103, LY-2140023, LY-2812223) – mGluR₂ and mGluR₃ agonist^[8]

Acetylcholine receptor modulators[edit]

Emraclidine (CVL-231) – M₄ muscarinic acetylcholine receptor positive allosteric modulator.^[9]
KarXT (xanomeline/trospium) – combined M₁ and M₄ muscarinic acetylcholine receptor agonist and peripherally-selective muscarinic acetylcholine receptor antagonist.^[10]
ML-007 – M₁ and M₄ muscarinic acetylcholine receptor agonist.^[11]
NBI-1117568 (HTL 0016878) – M₄ muscarinic acetylcholine receptor agonist.^[12]

Cannabinoid receptor modulators[edit]

Cannabidiol (CBD; GW-42003, GWP-42003, GWP-42003-P, ECP-012A; Arvisol, Epidiolex) – cannabinoid receptor modulator, antioxidant, other actions^[13]^[14]

Other/mixed receptor modulators[edit]

CVN766 – Orexin receptor type 1 antagonist^[15]
Deudextromethorphan (d-DM; AVP-786, CTP-786) – σ₁ receptor agonist, serotonin–norepinephrine reuptake inhibitor, uncompetitive NMDA receptor antagonist, muscarinic acetylcholine receptor agonist, other actions^[16]^[17]
Roluperidone (CYR-101, MIN-101, MT-210) – 5-HT_2A and σ₂ receptor antagonist^[18]
TAK-041 (NBI 1065846) – GPR139 receptor agonist^[19]

Enzyme inhibitors[edit]

Luvadaxistat (NBI 1065844, TAK-831) – D-amino acid oxidase inhibitor.^[20]
MK-8189 – phosphodiesterase 10A inhibitor.^[21]
Osoresnontrine (BI-409306, SUB-166499) – phosphodiesterase 9A inhibitor^[22]
Sodium benzoate (SND-11, SND-12, SND-13, SND-14; Clozaben, NaBen) – D-amino acid oxidase inhibitor^[23]

Ion channel modulators[edit]

Evenamide (NW-3509; NW-3509A) – Na_v1.3, Na_v1.7, and Na_v1.8 voltage-gated sodium channel blocker^[24]

Others[edit]

TS-134 (TS-1341) – undefined mechanism of action^[25]

References[edit]

^ "Brilaroxazine - Reviva Biopharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "FKF 02SC - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Masupirdine - Suven Life Sciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "N-methyl amisulpride - LB pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.
^ "Ralmitaront - AdisInsight". adisinsight.springer.com. Springer. Retrieved 10 July 2021.
^ "SEP 363856 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "SUVN D4010 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Emraclidine - Cerevel Therapeutics - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-15.
^ "APN 1125 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "ML 007 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-15.
^ "HTL 0016878 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.
^ "Cannabidiol - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Cannabidiol - Echo Pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved 14 February 2020.
^ "CVN 766 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-19.
^ "Deudextromethorphan - Avanir Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ Nguyen, Linda; Thomas, Kelan L.; Lucke-Wold, Brandon P.; Cavendish, John Z.; Crowe, Molly S.; Matsumoto, Rae R. (March 2016). "Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders". Pharmacology & Therapeutics. 159: 1–22. doi:10.1016/j.pharmthera.2016.01.016. ISSN 1879-016X. PMID 26826604.
^ "Roluperidone - Minerva Neurosciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "TAK 041 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.
^ "Luvadaxistat - Takeda - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.
^ "MK 8189 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.
^ "BI 409306 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Sodium benzoate - SyneuRx - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Evenamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "TS 134 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

External links[edit]

[1] "Brilaroxazine - Reviva Biopharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[2] "FKF 02SC - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[3] "Masupirdine - Suven Life Sciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[4] "N-methyl amisulpride - LB pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.

[5] "Ralmitaront - AdisInsight". adisinsight.springer.com. Springer. Retrieved 10 July 2021.

[6] "SEP 363856 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[7] "SUVN D4010 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[8] "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[9] "Emraclidine - Cerevel Therapeutics - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-15.

[10] "APN 1125 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[11] "ML 007 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-15.

[12] "HTL 0016878 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.

[13] "Cannabidiol - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[14] "Cannabidiol - Echo Pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved 14 February 2020.

[15] "CVN 766 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-19.

[16] "Deudextromethorphan - Avanir Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[17] Nguyen, Linda; Thomas, Kelan L.; Lucke-Wold, Brandon P.; Cavendish, John Z.; Crowe, Molly S.; Matsumoto, Rae R. (March 2016). "Dextromethorphan: An update on its utility for neurological and neuropsychiatric disorders". Pharmacology & Therapeutics. 159: 1–22. doi:10.1016/j.pharmthera.2016.01.016. ISSN 1879-016X. PMID 26826604.

[18] "Roluperidone - Minerva Neurosciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[19] "TAK 041 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.

[20] "Luvadaxistat - Takeda - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.

[21] "MK 8189 - AdisInsight". adisinsight.springer.com. Retrieved 2023-02-21.

[22] "BI 409306 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[23] "Sodium benzoate - SyneuRx - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[24] "Evenamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[25] "TS 134 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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v t e Antipsychotics (N05A)
Typical	Butyrophenones: Benperidol Bromperidol Bromperidol decanoate Droperidol Haloperidol^# Haloperidol decanoate Moperone Pipamperone Spiperone Timiperone Trifluperidol Diphenylbutylpiperidines: Fluspirilene Penfluridol Pimozide Phenothiazines: Acepromazine Acetophenazine Butaperazine Carphenazine (carfenazine)^‡ Chlorpromazine Cyamemazine Dixyrazine Fluphenazine Fluphenazine decanoate Fluphenazine enanthate Levomepromazine (methotrimeprazine) Mesoridazine Perazine Periciazine Perphenazine BL-1020 Perphenazine decanoate Perphenazine enanthate Piperacetazine Pipotiazine Pipotiazine palmitate Pipotiazine undecylenate Prochlorperazine Promazine Sulforidazine Thiopropazate Thioproperazine Thioridazine Trifluoperazine Triflupromazine Thioxanthenes: Chlorprothixene Clopenthixol Clopenthixol decanoate Flupentixol Flupentixol decanoate Tiotixene (thiothixene) Zuclopenthixol Zuclopenthixol acetate Zuclopenthixol decanoate
Disputed	Benzamides: Amisulpride Levosulpiride Nemonapride Remoxipride^‡ Sulpiride Sultopride Tiapride Veralipride^‡ Butyrophenones: Melperone Tricyclics: Carpipramine Clocapramine Clorotepine Clotiapine Loxapine Mosapramine Oxyprothepin decanoate Others: Molindone
Atypical	Benzisoxazole/benzisothiazoles: Iloperidone Lurasidone Paliperidone Paliperidone palmitate Perospirone Risperidone^# Ziprasidone Butyrophenones: Lumateperone Phenylpiperazines/quinolinones: Aripiprazole Aripiprazole lauroxil Brilaroxazine^† Brexpiprazole Cariprazine Tricyclics: Asenapine Clozapine^# Olanzapine Quetiapine Zotepine Others: Blonanserin Pimavanserin Sertindole
Others	Monoamine-depleting agents: Oxypertine Reserpine Tetrabenazine Others/unknown: Azacyclonol
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III