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.

This list was last comprehensively updated in December 2017. It is likely to become outdated with time.

Receptor modulators

Monoamine receptor modulators

Brilaroxazine (RP5063; oxaripiprazole) – atypical antipsychotic (D_2/3/4 and 5-HT_1A partial agonist and 5-HT_2A/2B/7 antagonist)^[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-Methylamisulpride (LB-102) – D_2,3, 5-HT₇, receptor antagonist (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

Pomaglumetad methionil (DB-103, LY-2140023, LY-2812223) – mGluR₂ and mGluR₃ agonist^[8]
Iclepertin – glycine transporter-1 inhibitor^[9]

Acetylcholine receptor modulators

Emraclidine (CVL-231) – M₄ muscarinic acetylcholine receptor positive allosteric modulator.^[10]
ML-007 – M₁ and M₄ muscarinic acetylcholine receptor agonist.^[11]
NBI-1117568 (HTL 0016878) – M₄ muscarinic acetylcholine receptor agonist.^[12]
NS-136 – M₄ muscarinic acetylcholine receptor positive allosteric modulator^[13]

Cannabinoid receptor modulators

Cannabidiol (CBD; GW-42003, GWP-42003, GWP-42003-P, ECP-012A; Arvisol, Epidiolex) – cannabinoid receptor modulator, antioxidant, other actions^[14]^[15]

Other/mixed receptor modulators

CVN766 – Orexin receptor type 1 antagonist^[16]
Deudextromethorphan (d-DM; AVP-786, CTP-786) – σ₁ receptor agonist, serotonin–norepinephrine reuptake inhibitor, uncompetitive NMDA receptor antagonist, muscarinic acetylcholine receptor agonist, other actions^[17]^[18]
Roluperidone (CYR-101, MIN-101, MT-210) – 5-HT_2A and σ₂ receptor antagonist^[19]
TAK-041 (NBI 1065846) – GPR139 receptor agonist^[20]

Enzyme inhibitors

Luvadaxistat (NBI 1065844, TAK-831) – D-amino acid oxidase inhibitor.^[21] (DAAO is a pathway to NMDAR.^[22])
MK-8189 – phosphodiesterase 10A inhibitor.^[23]
Osoresnontrine (BI-409306, SUB-166499) – phosphodiesterase 9A inhibitor^[24]
Sodium benzoate (SND-11, SND-12, SND-13, SND-14; Clozaben, NaBen) – D-amino acid oxidase inhibitor^[25]

Ion channel modulators

Evenamide (NW-3509; NW-3509A) – Na_v1.3, Na_v1.7, and Na_v1.8 voltage-gated sodium channel blocker^[26]

Others

TS-134 (TS-1341) – undefined mechanism of action^[27]
Kratom – Has shown antipsychotic-like effects on par with haloperidol in animal testing^[28]^[29]

References

^ "Brilaroxazine - Reviva Biopharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "FKF 02SC - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "Masupirdine - Suven Life Sciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "N-methyl amisulpride - LB pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.
^ "Ralmitaront - AdisInsight". adisinsight.springer.com. Springer. Retrieved July 10, 2021.
^ "SEP 363856 - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "SUVN D4010 - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ O'Brien, Erin (June 18, 2024). "New Baseline Data on Iclepertin for Schizophrenia". Vol 41, Issue 6. {{cite journal}}: Cite journal requires |journal= (help)
^ "Emraclidine - Cerevel Therapeutics - AdisInsight". adisinsight.springer.com. Retrieved February 15, 2023.
^ "ML 007 - AdisInsight". adisinsight.springer.com. Retrieved February 15, 2023.
^ "HTL 0016878 - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.
^ "NS 136". AdisInsight. May 15, 2024. Retrieved October 20, 2024.
^ "Cannabidiol - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "Cannabidiol - Echo Pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved February 14, 2020.
^ "CVN 766 - AdisInsight". adisinsight.springer.com. Retrieved February 19, 2023.
^ "Deudextromethorphan - Avanir Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 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 February 14, 2020.
^ "TAK 041 - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.
^ "Luvadaxistat - Takeda - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.
^ Vita, Antonio; Nibbio, Gabriele; Barlati, Stefano (January 2024). "Pharmacological Treatment of Cognitive Impairment Associated With Schizophrenia: State of the Art and Future Perspectives". Schizophrenia Bulletin Open. 5 (1): sgae013. doi:10.1093/schizbullopen/sgae013. ISSN 2632-7899. PMC 11207676. PMID 39144119.
^ "MK 8189 - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.
^ "BI 409306 - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "Sodium benzoate - SyneuRx - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "Evenamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ "TS 134 - AdisInsight". adisinsight.springer.com. Springer. Retrieved February 14, 2020.
^ Vijeepallam, K.; Pandy, V.; Kunasegaran, T.; Murugan, D. D.; Naidu, M. (2016). "Mitragyna speciosa Leaf Extract Exhibits Antipsychotic-Like Effect with the Potential to Alleviate Positive and Negative Symptoms of Psychosis in Mice". Frontiers in Pharmacology. 7: 464. doi:10.3389/fphar.2016.00464. PMC 5138496. PMID 27999544.
^ Johnson, L. E.; Balyan, L.; Magdalany, A.; Saeed, F.; Salinas, R.; Wallace, S.; Veltri, C. A.; Swogger, M. T.; Walsh, Z.; Grundmann, O. (2020). "The Potential for Kratom as an Antidepressant and Antipsychotic". The Yale Journal of Biology and Medicine. 93 (2): 283–289. PMC 7309668. PMID 32607089.

External links

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

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

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

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

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

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

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

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

[9] O'Brien, Erin (June 18, 2024). "New Baseline Data on Iclepertin for Schizophrenia". Vol 41, Issue 6. {{cite journal}}: Cite journal requires |journal= (help)

[10] "Emraclidine - Cerevel Therapeutics - AdisInsight". adisinsight.springer.com. Retrieved February 15, 2023.

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

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

[AdisInsight-13] "NS 136". AdisInsight. May 15, 2024. Retrieved October 20, 2024.

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

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

[16] "CVN 766 - AdisInsight". adisinsight.springer.com. Retrieved February 19, 2023.

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

[18] 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.

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

[20] "TAK 041 - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.

[21] "Luvadaxistat - Takeda - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.

[22] Vita, Antonio; Nibbio, Gabriele; Barlati, Stefano (January 2024). "Pharmacological Treatment of Cognitive Impairment Associated With Schizophrenia: State of the Art and Future Perspectives". Schizophrenia Bulletin Open. 5 (1): sgae013. doi:10.1093/schizbullopen/sgae013. ISSN 2632-7899. PMC 11207676. PMID 39144119.

[23] "MK 8189 - AdisInsight". adisinsight.springer.com. Retrieved February 21, 2023.

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

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

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

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

[28] Vijeepallam, K.; Pandy, V.; Kunasegaran, T.; Murugan, D. D.; Naidu, M. (2016). "Mitragyna speciosa Leaf Extract Exhibits Antipsychotic-Like Effect with the Potential to Alleviate Positive and Negative Symptoms of Psychosis in Mice". Frontiers in Pharmacology. 7: 464. doi:10.3389/fphar.2016.00464. PMC 5138496. PMID 27999544.

[29] Johnson, L. E.; Balyan, L.; Magdalany, A.; Saeed, F.; Salinas, R.; Wallace, S.; Veltri, C. A.; Swogger, M. T.; Walsh, Z.; Grundmann, O. (2020). "The Potential for Kratom as an Antidepressant and Antipsychotic". The Yale Journal of Biology and Medicine. 93 (2): 283–289. PMC 7309668. PMID 32607089.

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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 (+samidorphan) Quetiapine Zotepine Others: Blonanserin Pimavanserin Sertindole
Others	Monoamine-depleting agents: Oxypertine Reserpine Tetrabenazine Muscarinic agonists: Xanomeline/trospium chloride Others/unknown: Azacyclonol
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III