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[]

Monoamine receptor modulators[]

– atypical antipsychotic (D₂ and 5-HT_2A receptor antagonist, other actions)^[1]
AVN-211 (CD-008-0173) – 5-HT₆ receptor antagonist^[2]
Brilaroxazine (RP-5063, RP-5000; oxaripiprazole) – atypical antipsychotic (D₂ receptor partial agonist, 5-HT_2A receptor antagonist, other actions)^[3]
– D₃ receptor antagonist, 5-HT_1A receptor partial agonist, and weak D₂ receptor partial agonist^[4]
(TGOF-02N) – atypical antipsychotic (D₂ and 5-HT_2A receptor antagonist, other actions)^[5]
– D₁, 5-HT_2A, and 5-HT₆ receptor antagonist^[6]
(SUVN-502) – 5-HT₆ receptor antagonist^[7]
Ralmitaront (RG-7906, RO-6889450) – TAAR1 agonist^[8]
Ulotaront (SEP-856, SEP-363856) – 5-HT_1A receptor and TAAR1 agonist^[9]
– 5-HT₄ receptor partial agonist^[10]
(ENV-8058) – 5-HT₃ receptor antagonist^[11]

Glutamate receptor modulators[]

Neboglamine (CR-2249, XY-2401; nebostinel) – NMDA receptor glycine-site positive allosteric modulator^[12]
PF-4958242 – AMPA receptor positive allosteric modulator^[13]
(DB-103, LY-2140023, LY-2812223) – mGluR₂ and mGluR₃ agonist^[14]

Acetylcholine receptor modulators[]

– α₇ nicotinic acetylcholine receptor partial agonist^[15]
(Trospium chloride/xanomeline) – combined M₁ and M₄ muscarinic acetylcholine receptor agonist and peripherally-selective muscarinic acetylcholine receptor antagonist^[16]

Cannabinoid receptor modulators[]

– cannabinoid receptor modulator (phytocannabinoid-based chewing gum)^[17]
Cannabidiol (CBD; GW-42003, GWP-42003, GWP-42003-P, ECP-012A; Arvisol, Epidiolex) – cannabinoid receptor modulator, antioxidant, other actions^[18]^[19]

Other/mixed receptor modulators[]

Basmisanil (RG-1662, RO-5186582) – GABA_A receptor α₅ subunit-containing negative allosteric modulator^[20]
Deudextromethorphan (d-DM; AVP-786, CTP-786) – σ₁ receptor agonist, serotonin–norepinephrine reuptake inhibitor, uncompetitive NMDA receptor antagonist, muscarinic acetylcholine receptor agonist, other actions^[21]^[22]
Erteberel (LY-500307, SERBA-1) – ERβ agonist^[23]
Olanzapine/samidorphan (ALKS-3831) – combined atypical antipsychotic (D₂ and 5-HT_2A receptor antagonist, other actions) and μ-opioid receptor antagonist^[24]
Roluperidone (CYR-101, MIN-101, MT-210) – 5-HT_2A and σ₂ receptor antagonist^[25]

Enzyme inhibitors[]

(SUB-166499) – phosphodiesterase 9A inhibitor^[26]
– dual phosphodiesterase 2A and 10A inhibitor^[27]
(OMS-643762) – phosphodiesterase 10A inhibitor^[28]
Sodium benzoate (SND-11, SND-12, SND-13, SND-14; Clozaben, NaBen) – D-amino acid oxidase inhibitor^[29]
– D-amino acid oxidase inhibitor^[30]

Ion channel modulators[]

– shaw potassium channel modulator^[31]
Evenamide (NW-3509; NW-3509A) – Na_v1.3, Na_v1.7, and Na_v1.8 voltage-gated sodium channel blocker^[32]

Others[]

– undefined mechanism of action^[33]
– undefined mechanism of action^[34]
– undefined mechanism of action^[35]
– undefined mechanism of action^[36]
– undefined mechanism of action^[37]
– undefined mechanism of action^[38]
– undefined mechanism of action^[39]
– undefined mechanism of action^[40]
Pyridoxamine (BST-4001, K-163, K-163SZ; Pyridorin) – vitamin B₆ analog, advanced glycosylation end-product inhibitor, oxygen radical scavenger^[41]
(TS-1341) – undefined mechanism of action^[42]

References[]

^ "ATI 9242 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "AVN 211 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Brilaroxazine - Reviva Biopharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "F 17464 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "FKF 02SC - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Lu AF35700 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Masupirdine - Suven Life Sciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "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.
^ "TAK 058 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Neboglamine - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "BIIB 104 - 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.
^ "APN 1125 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "APN 1125 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "AX 1604 - Axim Biotech - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Cannabidiol - GW Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Cannabidiol - Echo Pharmaceuticals - AdisInsight". adisinsight.springer.com. Retrieved 14 February 2020.
^ "Basmisanil - Roche - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "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.
^ "Erteberel - Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Olanzapine/samidorphan - Alkermes plc - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Roluperidone - Minerva Neurosciences - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "BI 409306 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Lu AF11167 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "OMS 824 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Sodium benzoate - SyneuRx - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "TAK 831 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "AUT 00206 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Evenamide - Newron Pharmaceuticals - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "ADE 615 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "ADE 616 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "AMG 581 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "ASP 4345 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "ASP 6981 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Atx11 004 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "MK 8189 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "PF 06266047 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "Pyridoxamine - NephroGenex/Kowa - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.
^ "TS 134 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

External links[]

[1] "ATI 9242 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[2] "AVN 211 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

[4] "F 17464 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

[6] "Lu AF35700 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

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

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

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

[11] "TAK 058 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[12] "Neboglamine - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[13] "BIIB 104 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

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

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

[17] "AX 1604 - Axim Biotech - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

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

[20] "Basmisanil - Roche - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

[22] 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.

[23] "Erteberel - Eli Lilly and Company - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[24] "Olanzapine/samidorphan - Alkermes plc - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

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

[27] "Lu AF11167 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[28] "OMS 824 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

[30] "TAK 831 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[31] "AUT 00206 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

[33] "ADE 615 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[34] "ADE 616 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[35] "AMG 581 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[36] "ASP 4345 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[37] "ASP 6981 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[38] "Atx11 004 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[39] "MK 8189 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[40] "PF 06266047 - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

[41] "Pyridoxamine - NephroGenex/Kowa - AdisInsight". adisinsight.springer.com. Springer. Retrieved 14 February 2020.

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

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v t 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