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Investigational antipsychotics

This is a list of investigational antipsychotics, or drugs that are currently under development for clinical use as antipsychotics for the treatment of schizophrenia and other psychotic disorders but are not yet approved. Psychotic disorders include schizophrenia, schizoaffective disorder, and others such as psychotic depression, Parkinson's disease psychosis, and Alzheimer's disease psychosis.

Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. The format of list items is "Name (Synonyms) – Mechanism of Action – Indication [Reference]".

This list was last comprehensively updated in June 2026. It is likely to become outdated with time.

Under development

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Preregistration

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  • Olanzapine long acting injectable (mdc-TJK; TEV-749; TV-44749) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Roluperidone (CYR-101; MIN-101; MT-210) – serotonin 5-HT2A receptor antagonist, sigma σ2 receptor antagonist, and other actions – schizophrenia

Phase 3

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  • Brilaroxazine (RP-5000; RP-5063; oxaripiprazole) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Direclidine (HTL-0016878; NBI-1117568; NBI-568) – muscarinic acetylcholine M4 receptor agonist – schizophrenia
  • Evenamide (EA-8001; NW-3509; NW-3509A) – voltage-gated sodium channel (VGSC) blocker – schizophrenia
  • Iclepertin (BI-425809) – glycine transporter 1 (GlyT1) inhibitor – schizophrenia
  • N-Methylamisulpride (LB-102) – dopamine D2 and D3 receptor antagonist, serotonin 5-HT2B receptor antagonist, and serotonin 5-HT7 receptor antagonist – schizophrenia
  • Remlifanserin (ACP-204) – serotonin 5-HT2A receptor inverse agonist – psychotic disorders
  • Risperidone extended release (LYN-005) – dopamine D2 receptor antagonist and serotonin 5-HT2A receptor antagonist – schizophrenia, schizoaffective disorder
  • Ulotaront (SEP-363856; SEP-856) – trace amine-associated receptor 1 (TAAR1) agonist and serotonin 5-HT1A receptor agonist – schizophrenia
  • Valbenazine (Dysval; Ingrezza; MT-5199; NBI-98854; Remleas) – vesicular monoamine transporter 2 (VMAT2) blocker and monoamine depleting agent – schizophrenia
  • Xanomeline enteric coated (BMS-986519; KarX-EC; LY-246708; Memcor; NNC-110232) – muscarinic acetylcholine M1 and M4 receptor agonist – psychotic disorders
  • Xanomeline/trospium chloride (BMS-986510; Cobenfy; KarXT; trospium/LY-246708; trospium/xanomeline) – combination of xanomeline (muscarinic acetylcholine M1 and M4 receptor agonist) and trospium chloride (peripherally selective non-selective muscarinic acetylcholine receptor antagonist) – psychotic disorders

Phase 2/3

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  • AVN-211 (CD-008-0173) – serotonin 5-HT6 receptor antagonist – schizophrenia
  • Deudextromethorphan (AVP-786; CTP-786; d-DM; d6-DM; deudextromethorphan/quinidine; deuterated dextromethorphan; deuterated-DM) – combination of deudextromethorphan (sigma receptor agonist, ionotropic glutamate NMDA receptor antagonist, serotonin reuptake inhibitor, other actions) and quinidine (CYP2D6 inhibitor) – schizophrenia
  • Sodium benzoate (benzoate; Clozaben; NaBen; SND-51; SND-11; SND-12; SND-13; SND-14; Tannquilynne; Ω-NaBen) – D-amino acid oxidase inhibitor – schizophrenia

Phase 2

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  • ANAVEX 3-71 (ANAVEX3-71; AF710B; AF-710B) – muscarinic acetylcholine M1 receptor positive allosteric modulator and sigma σ1 receptor agonist – schizophrenia
  • Balipodect (AXS-20; TAK-063) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Brenipatide (LY-3537031) – glucagon-like peptide-1 (GLP-1) receptor agonist and gastric inhibitory polypeptide (GIP) receptor agonist – schizophrenia
  • Brilaroxazine (RP-5000; RP-5063; oxaripiprazole) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizoaffective disorder
  • CPL-500036 (CPL'36; CPL-500-036-02; CPL500036; CZ20; PG203; SUB193569) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Emraclidine (CVL-231; PF-06852231) – muscarinic acetylcholine M4 receptor positive allosteric modulator – schizophrenia
  • FKF-02SC (FKF02SC; TGOF-02N) – dopamine D2 receptor antagonist and serotonin 5-HT2A receptor antagonist – schizophrenia
  • GXV-813 (EX-A8078) – muscarinic acetylcholine M4 receptor agonist – schizophrenia
  • HS-10380 – undefined mechanism of action – schizophrenia
  • Idazoxan extended release (TR-01-IR; TR-01-XR; TR-01-XRR; TR-01-XRS) – α2-adrenergic receptor antagonist – schizophrenia
  • Iloperidone (Fanapt; Fanaptum; Fiapta; HP-873; ILO-522; VYV-683; Zomaril) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • KYN-5356 (MT-5356) – kynurenine aminotransferase 2 (KAT-II) inhibitor – schizophrenia
  • Lu AF11167 (Lu-AF-11167) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Lumateperone deuterated (ITI-1284; ITI-1284 ODT-SL) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • Luvadaxistat (NBI-1065844; TAK-831) – D-amino acid oxidase inhibitor – schizophrenia
  • LY-03017 (LPM-526000133; LPM526000133) – serotonin 5-HT2A and 5-HT2C receptor antagonist – schizophrenia
  • LY-03020 (LPM-787000048; LPM787000048) – trace amine-associated receptor 1 (TAAR1) agonist and serotonin 5-HT2C receptor agonist – schizophrenia
  • Masupirdine (M1; M1 of SUVN-502; SUVN502; SVN-502) – serotonin 5-HT6 receptor antagonist – schizophrenia
  • ML-007/muscarinic antagonist (ML-007/PAC; ML-007C-MA) – combination of ML-007 (muscarinic acetylcholine M1 and M4 receptor agonist) and a muscarinic acetylcholine receptor antagonist – schizophrenia, psychotic disorders
  • Neboglamine (nebostinel; CR-2249; XY-2401) – ionotropic glutamate NMDA receptor glycine site positive allosteric modulator – schizophrenia
  • NS-136 – muscarinic acetylcholine M4 receptor positive allosteric modulator – schizophrenia
  • Osoresnontrine (BI-409306; SUB-166499) – phosphodiesterase PDE9A inhibitor – schizophrenia, psychotic disorders
  • Pomaglumetad methionil (DB103; DB-103; LY-2140023; LY2140023; LY-2812223; LY-404039 prodrug) – metabotropic glutamate mGlu2 and mGlu3 receptor agonist (pomaglumetad prodrug) – schizophrenia
  • Pyridoxamine (BST-4001; K-163; K163SZ; Pyridorin) – vitamin B6 and antioxidant – schizophrenia
  • Sodium benzoate (benzoate; Clozaben; NaBen; SND-51; SND-11; SND-12; SND-13; SND-14; Tannquilynne; Ω-NaBen) – D-amino acid oxidase inhibitor – psychotic disorders
  • Vafidemstat (ORY-2001) – lysine-specific demethylase 1 (LSD-1) inhibitor and monoamine oxidase B (MAO-B) inhibitor – schizophrenia

Phase 1/2

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  • Cariprazine depot – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Forvisirvat (SP-624) – sirtuin-6 (SIRT6) activator – schizophrenia
  • PF-6412562 (PF6412562; PF-06412562; PF06412562) – dopamine D1 and D5 receptor partial agonist – schizophrenia
  • SKL-15508 (SKL–A4R; SKL15508) – α7 nicotinic acetylcholine receptor agonist – schizophrenia

Phase 1

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  • DSP-0038 – serotonin 5-HT1A receptor agonist and serotonin 5-HT2A receptor antagonist – psychotic disorders
  • HTL-0048149 (HTL'149; HTL-0048149; HTL-A; NXE-0048149; NXE-149) – GPR52 agonist – schizophrenia
  • LTX-001 – glutaminase inhibitor – schizophrenia
  • MK-5720 – undefined mechanism of action – schizophrenia
  • ML-007 – muscarinic acetylcholine M1 and M4 receptor agonist – psychotic disorders
  • NMRA-861 – muscarinic acetylcholine M4 receptor positive allosteric modulator – schizophrenia
  • NMRA-898 – muscarinic acetylcholine M4 receptor positive allosteric modulator – schizophrenia
  • OV-4071 – K+Cl– cotransporter 2 (KCC2) direct activator – psychotic disorders
  • SEP-380135 – undefined mechanism of action – schizophrenia
  • Squalamine (ENT-01; Enterin-01; kenterin) – various actions – psychotic disorders
  • VV-119 (VV119) – undefined mechanism of action (dopamine and serotonin receptor modulator) – schizophrenia
  • Zelquistinel (AGN-241751; GATE-251) – ionotropic glutamate NMDA receptor positive allosteric modulator – schizophrenia

Clinical phase unknown

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  • Quetiapine oral suspension – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia

Preclinical

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  • BrAD-R13 (R13; Braegen-01) – tropomyosin receptor kinase B (TrkB) agonist (tropoflavin (7,8-dihydroxyflavone; 7,8-DHF) prodrug) – schizophrenia
  • DPX-101 – α5 subunit-containing GABAA receptor positive allosteric modulator – schizophrenia
  • EM-221 – phosphodiesterase PDE10A inhibitor – schizophrenia
  • NMRA-861 – muscarinic acetylcholine M4 receptor positive allosteric modulator – psychotic disorders
  • OV-4071 – K+Cl– cotransporter 2 (KCC2) direct activator – schizphrenia
  • TPT-0901 – cannabinoid CB1 and CB2 receptor agonist – schizophrenia
  • Xanomeline/trospium prodrug (TerXT) – prodrug of xanomeline (muscarinic acetylcholine M1 and M4 receptor agonist) and trospium chloride (peripherally selective non-selective muscarinic acetylcholine receptor antagonist) – schizophrenia

Phase unknown

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  • Quetiapine long acting injection (CP-103) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders

Not under development

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No development reported

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  • ADE-616 – undefined mechanism of action – schizophrenia
  • AGX-201 (histamine dihydrochloride) – non-selective histamine receptor agonist – schizophrenia
  • AMG-579 – phosphodiesterase PDE10A inhibitor – schizophrenia, schizoaffective disorder
  • AMG-581 – undefined mechanism of action – schizophrenia, schizoaffective disorder
  • Aripiprazole controlled release (ZY-102) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Aripiprazole oral soluble film – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Aripiprazole transdermal (AQS-1301) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • ASP-4345 (ASP4345) – dopamine D1 receptor positive allosteric modulator – schizophrenia
  • BIMG-80 – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Brexpiprazole long-acting injectable (MTD-211) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Buspirone controlled release (buspirone ER) – serotonin 5-HT1A receptor agonist – schizophrenia
  • Cannabidiol (CBD; Arvisol) – atypical cannabinoid and various actions – schizophrenia
  • Cariprazine (CarMP-214; Reagila; RGH-188; Symvenu; Vraylar WID-RGC20) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Clozapine modified-release – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • CM-182 – undefined mechanism of action – schizophrenia
  • CVL-047 – phosphodiesterase PDE4 inhibitor – schizophrenia
  • CY-150112 – undefined mechanism of action – schizophrenia
  • GSK-729327 (GSK729327) – ionotropic glutamate AMPA receptor positive allosteric modulator – schizophrenia
  • GT-001 (GT001) – GABAA receptor positive allosteric modulator – psychotic disorders
  • HW-165 – dopamine D2 and D3 receptor partial agonist – schizophrenia
  • JNJ-17305600 – glycine transporter 1 (GlyT1) inhibitor – schizophrenia
  • JNJ-37822681 – dopamine D2 receptor antagonist – schizophrenia
  • LM-007 – undefined mechanism of action – schizophrenia
  • MCD-386 (CDD-0102; CDD-0102-J; MCD-386 Forte/Transderm; MCD-386CR) – muscarinic acetylcholine M1 receptor agonist – schizophrenia
  • Mesdopetam (IRL-790) – atypical dopamine D2 and D3 receptor antagonist and other actions – psychotic disorders
  • ML-007 – muscarinic acetylcholine M1 and M4 receptor agonist – schizophrenia
  • Olanzapine – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • Olanzapine/samidorphan (ALKS-33/olanzapine; ALKS-3831; Lybalvi; olanzapine/ALKS 33; OLZ/SAM; Samidorphan/olanzapine) – combination of olanzapine (dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions) and samidorphan (non-selective opioid receptor antagonist) – psychotic disorders
  • Paliperidone controlled-release (DLP-115) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • PF-06266047 (PF06266047; PF-6266047; PF6266047) – undefined mechanism of action – schizophrenia
  • Plazinemdor (CAD-9303) – ionotropic glutamate NMDA receptor positive allosteric modulator – schizophrenia
  • Prochlorperazine sublingual – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonists, and other actions – psychotic disorders
  • Research programme: AMPA receptor agonists - RespireRx (Ampakines; CX-929; CX1501; CX1763; CX1796; CX1837; CX1846; CX1942; CX2007; CX2076; CX516; CX614; CX707) – ionotropic glutamate AMPA receptor positive allosteric modulators – schizophrenia
  • Research programme: CNS disorder therapeutics - Promentis Pharmaceuticals – antioxidants, glutamate receptor modulators, and SLC7A11 modulators – schizophrenia
  • Research programme: CNS disorders therapeutics - Sage Therapeutics – GABAA receptor modulators and ionotropic glutamate NMDA receptor modulators – schizophrenia, psychotic disorders
  • Research programme: psychiatric disorder therapeutics - NeuroProfile – neuron modulators – schizophrenia
  • Research programme: psychiatric disorder therapies - Chakra Biotech/Tikvah Therapeutics (CB-010002; CB-020001; CB-030004; CB-030006) – serotonin 5-HT2C receptor antagonists, adrenergic receptor antagonists, dopamine D2 receptor antagonists, serotonin 5-HT2A receptor modulators, and serotonin 5-HT6 receptor antagonists – schizophrenia
  • Research programme: psychotic disorders therapeutics - GeNeuro (New anti-HERV-W Ab; New anti-HERV-W mab) – Env gene product inhibitors – psychotic disorders
  • Research programme: schizophrenia therapeutics - Lundbeck/Vanderbilt University – dopamine release inhibitors – schizophrenia
  • Research programme: small molecule therapeutics - Saniona/Boehringer Ingelheim – α4β2 nicotinic acetylcholine receptor modulators – schizophrenia
  • RO-5545965 (RO5545965; RG-7203) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • SDZ-PSD-958 – dopamine D1 receptor antagonist – psychotic disorders
  • TAK-058 (ENV-8058) – serotonin 5-HT3 receptor antagonist – schizophrenia
  • Talnetant (SB-223242; SB-223412; SB-223412A) – neurokinin NK3 receptor antagonist – schizophrenia
  • Tetrahydrocannabinol/cannabidiol (THC/CBD; cannabidiol/tetrahydrocannabinol; CBD/THC; CanChew; MedChew) – combination of tetrahydrocannabinol (THC; cannabinoid CB1 and CB2 receptor agonist) and cannabidiol (CBD; atypical cannabinoid and various actions) – psychotic disorders
  • TPN-672 – serotonin 5-HT1A receptor agonist, dopamine D2 receptor antagonist, and serotonin 5-HT2A receptor antagonist – schizophrenia
  • TS-134 (TS-1341) – undefined mechanism of action – schizophrenia
  • TV-48438 – undefined mechanism of action – schizophrenia
  • Usmarapride (SUVN-D-4010) – serotonin 5-HT4 receptor agonist – schizophrenia
  • VLT-015 (FAP-2015) – undefined mechanism of action – schizophrenia
  • Zagociguat (CY-6463; IW-6463) – soluble guanylyl cyclase (sGC) agonist – schizophrenia
  • Ziprasidone extended release – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia

Suspended

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  • Loxapine film (INT 0036/2012; INT 0036/2013; INT0036; Loxapine VersaFilm) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • OMS-824 (OMS-643762) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Pimavanserin (ACP-103; BVF-048; Nuplazid) – serotonin 5-HT2A receptor inverse agonist – schizophrenia

Discontinued

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  • A-69024 – dopamine D1 receptor antagonist – psychotic disorders
  • ABT-925 (A-437203; BSF-201640; DTA-201; LU-201640) – dopamine D3 receptor antagonist – schizophrenia
  • ACP-319 (VU0467319; VU-0467319; VU319; VU-319) – muscarinic acetylcholine M1 receptor positive allosteric modulator – schizophrenia
  • Adipiplon (NG-273; NG2-73) – GABAA receptor positive allosteric modulator – schizophrenia
  • ADX-71149 (JNJ-1813; JNJ-40411813; JNJ-mGluR2-PAM) – metabotropic glutamate mGlu2 receptor positive allosteric modulator – schizophrenia
  • Alosetron (GR-68755; GR-68755C; Lotronex) – serotonin 5-HT3 receptor antagonist – schizophrenia
  • AM-831 (AM831; PCAP programme) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and muscarinic acetylcholine M1 receptor agonist – schizophrenia
  • Aplindore (DAB-452; Palindore; SLS-006; WAY-DAB 452) – dopamine D2 receptor agonist – schizophrenia
  • Aprepitant (Emend; L-754030; MK-0869; MK-869; ONO-7436) – neurokinin NK1 receptor antagonist – schizophrenia
  • Aripiprazole (Abilify; Abilify Asimtufii; Abilify Maintena; Abilify MyCite; Abilitat; Ao Pai; Arlemide; Asimtufii; OPC-14597; OPC-31) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • Armodafinil (CEP-10953; Nuvigil; R-modafinil) – atypical dopamine reuptake inhibitor (DRI) – schizophrenia
  • ASP-2535 (ASP2535) – undefined mechanism of action – schizophrenia
  • ASP-2905 (ASP2905) – undefined mechanism of action – schizophrenia
  • AUT-00201 – voltage-gated potassium channel Kv3.1, Kv3.2, and Kv3.4 positive allosteric modulator – schizophrenia
  • AUT-00206 – voltage-gated potassium channel Kv3.1 and Kv3.2 positive allosteric modulator – schizophrenia
  • AZD-0328 (AZD0328) – α7 nicotinic acetylcholine receptor agonist – schizophrenia
  • Basmisanil (NTX-1511; RG-1662; RO-5186582) – α5 subunit-containing GABAA receptor negative allosteric modulator – schizophrenia
  • Batelapine (CGS-13429; CGS-13429A) – undefined mechanism of action (clozapine analogue) – psychotic disorders
  • Berupipam (NNC 22-0010) – dopamine D1 receptor antagonist – psychotic disorders
  • Bifeprunox (DU-127090) – dopamine D2 receptor partial agonist and serotonin 5-HT1A receptor agonist – schizophrenia
  • Bitopertin (DISC-1459; R-1678; RG-6718; RG-6178; RG1678; RO-4917838; RO4917838) – glycine transporter 1 (GlyT1) inhibitor – schizophrenia
  • BL-1020 (AN-168; CYP-1020; perphenazine GABA ester; perphenazine-4-aminobutyrate) – prodrug of perphenazine (dopamine D2 receptor antagonist, other actions) and γ-aminobutyric acid (GABA) (GABA receptor agonist) – schizophrenia, schizoaffective disorder
  • BMS-181100 (BMY-14802; MJ-14802) – serotonin 5-HT1A receptor agonist, sigma receptor antagonist, and other actions – psychotic disorders
  • Cannabidiol (CBD; Epidiolex; Epidyolex; GW-42003; GWP-42003; GWP-42003-P; JZP-926) – atypical cannabinoid and various actions – schizophrenia
  • Cerlapirdine (PF-05212365; PF-5212365; SAM-531; WAY-262531) – serotonin 5-HT6 receptor antagonist – schizophrenia
  • CX-516 (1-BCP; AMPAlex; BDP-12; SPD-420) – ionotropic glutamate AMPA receptor positive allosteric modulator – schizophrenia
  • Davunetide intranasal (AL-108; NAP; NAPVSIPQ) – microtubule modulator – schizophrenia
  • DB-105 (ORM-12741) – α2C-adrenergic receptor antagonist – schizophrenia
  • Deutarserine (C-21692; CTP-692; D-serine deuterated) – ionotropic glutamate NMDA receptor agonist – schizophrenia
  • DHA-clozapine (Clozaprexin; docosahexaenoic acid-clozapine) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions (clozapine prodrug with enhanced central penetration) – schizophrenia
  • Drinabant (AVE-1625; INDV-5004; OPNT-004) – cannabinoid CB1 receptor antagonist – schizophrenia
  • DSP-6745 – serotonin 5-HT2A and 5-HT2C receptor antagonist – psychotic disorders
  • Ecopipam (EBS-101; PSYRX-101; SCH-39166) – dopamine D1 receptor antagonist – schizophrenia
  • Eglumetad (eglumegad; LY-354740) – metabotropic glutamate mGlu2 and mGlu3 receptor agonist – schizophrenia, psychotic disorders
  • Elinzanetant (BAY-3427080; GSK-1144814A; GSK-1144814; Lynkuet; NT-814) – neurokinin NK1 and NK3 receptor antagonist – schizophrenia
  • Eltoprazine (DU-28853) – serotonin 5-HT1A and 5-HT1B receptor agonist – psychotic disorders
  • Erteberel (LY-500307; SERBA-1) – estrogen receptor beta (ERβ) agonist – schizophrenia
  • Ethyl eicosapentaenoic acid (AMR-101; eicosapentaenoic acid ethyl ester; ethyl eicosapentaenoate; ethyl icopenate; ethyl-EPA; icosapent ethyl-LAX-101; LAX-101c; Miraxion; Vascepa; Vazkepa) – omega-3 fatty acid – psychotic disorders
  • F-17464 – dopamine D3 receptor antagonist and serotonin 5-HT1A receptor agonist – schizophrenia
  • Fananserin (RP-62203) – dopamine D4 receptor antagonist and serotonin 5-HT2 receptor antagonist – schizophrenia
  • Farampator (CX-691; ORG-24448) – ionotropic glutamate AMPA receptor positive allosteric modulator – schizophrenia
  • Fluperlapine (NB-106689) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions (clozapine analogue) – schizophrenia
  • FRM-6308 (EVP-6308) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • GSK-239512 (GSK239512) – histamine H3 receptor antagonist – schizophrenia
  • HP-370 – undefined mechanism of action – psychotic disorders
  • Idazoxan (CGP-25811A; RX-781094) – α2-adrenergic receptor antagonist – schizophrenia
  • Ibipinabant (BMS-646256; SLV-319) – cannabinoid CB1 receptor antagonist – psychotic disorders
  • Itasetron (DAU-6215; U-98079) – serotonin 5-HT3 receptor antagonist – psychotic disorders
  • JNJ-39393406 – α7 nicotinic acetylcholine receptor positive allosteric modulator – schizophrenia
  • Lamotrigine (BW-430C78; BW-430C; Labileno; Lamactil; Lamictal; Lamictin; Lamitrin) – voltage-gated sodium channel (VGSC) blocker – schizophrenia
  • Lisdexamfetamine (Elvanse; LDX; NRP-104; S-877489; SHP-489; SPD-489; Tyvense; Venvanse; Vyvanse) – norepinephrine–dopamine releasing agent (NDRA) – schizophrenia
  • LU-35138 – dopamine D4 receptor antagonist – schizophrenia
  • Lu AA39959 (LUAA-399599) – undefined mechanism of action (ion channel modulator) – schizophrenia
  • Lu AF35700 (d8-zicronapine) – dopamine D1 and D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, serotonin 5-HT6 receptor antagonist, and other actions – schizophrenia, schizoaffective disorder
  • Mardepodect (MP-10; PF-02545920; PF02545920; PF-2545920; PF2545920) – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Meclinertant (reminertant; SR-48692) – neurotensin NTS1 receptor antagonist – schizophrenia
  • Melperone (Bunil; Buronil; Melperon; Methylperon; Methylperone; Metylperon; Metylperone) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • Mifepristone (C-1073; Corlux; Corluxin; Korlym; Mifegyne; Mifeprex; RU-38486; RU-486) – glucocorticoid receptor antagonist, progesterone receptor antagonist, and other actions – psychotic affective disorders
  • MIN-301 (NRG-101) – ERBB4 (HER4) receptor agonist – schizophrenia
  • MK-0249 – histamine H3 receptor antagonist – schizophrenia
  • MK-0777 (L-830982; TPA-023) – GABAA receptor positive and negative allosteric modulator – schizophrenia
  • MK-8189 – phosphodiesterase PDE10A inhibitor – schizophrenia
  • Nerisopam (EGIS-6775; GYKI-52322) – undefined mechanism of action (atypical benzodiazepine analogue) – psychotic disorders
  • NGD-931 – undefined mechanism of action – psychotic disorders
  • NLX-101 (F-15599; F15599) – serotonin 5-HT1A receptor agonist – schizophrenia
  • NNC 01-0687 (ADX-10061; CEE-03-310; NNC-687) – dopamine D1 receptor antagonist – schizophrenia
  • NS-626 – calcium channel blocker – psychotic disorders
  • Ocaperidone (R-79598) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia, psychotic disorders
  • Odapipam (NNC 01-0756, NNC-756, NO-756) – dopamine D1 receptor antagonist – psychotic disorders
  • ORM-10921 – α2C-adrenergic receptor antagonist – schizophrenia
  • Oxytocin intranasal – oxytocin receptor agonist – schizophrenia
  • Panamesine (EMD-57445) – sigma σ1 and σ2 receptor antagonist
  • Pavinetant (AZ-12472520; AZD-2624; AZD-4901; MLE-4901) – neurokinin NK3 receptor antagonist – schizophrenia
  • PF-3463275 (PF3463275; PF-03463275; PF03463275) – glycine transporter 1 (GlyT1) inhibitor – schizophrenia
  • PF-5180999 (PF5180999; PF-05180999; PF05180999) – phosphodiesterase PDE2 inhibitor – schizophrenia
  • Pozanicline (A-87089.0; ABT-089) – α4β2 nicotinic acetylcholine receptor agonist, nicotinic acetylcholine receptor agonist – schizophrenia
  • Pramipexole (BI-Sifrol; Daquiran; Mirapex; Mirapex ER; Mirapex LA; Mirapexin; Pexola; Sifrol; Sirfrol ER; SND-919; SND-919Y) – dopamine D2, D3, and D4 receptor agonist – schizophrenia
  • Preclamol (3-PPP) – dopamine D2 receptor partial agonist – schizophrenia, psychotic disorders
  • Pridopidine (ACR-16; ASP-2314; FNP-253; FNP-254; FR-310826; Huntexil; Nurzigma; TV-7820) – sigma σ1 receptor agonist – schizophrenia
  • Quetiapine (FK-949; FK949E; ICI-204636; Seroquel; Seroquel XL; Seroquel XR) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • Ralmitaront (NTX-2001; RG-7906; RO-6889450) – trace amine-associated receptor 1 (TAAR1) agonist – schizophrenia, schizoaffective disorder
  • Research programme: CEB 1310 series - Vernalis – undefined mechanism of action – psychotic disorders
  • Research programme: dopamine D4 receptor antagonists - Sanofi-Aventis/NPS Allelix – dopamine D4 receptor antagonists – schizophrenia
  • Research programme: metabotropic glutamate receptor 5 modulators - Addex Therapeutics (ADX-47273; ADX-50938; ADX-63365; ADX63365 CDPPB) – metabotropic glutamate mGlu5 receptor positive allosteric modulators – schizophrenia
  • Research programme: mGluR2 modulators - Addex Pharmaceuticals/Ortho-McNeil (ADX-92639; JNJ-40068782) – metabotropic glutamate mGlu2 receptor modulators – schizophrenia
  • Research programme: NMDA receptor modulators - AbbVie (NRX-1050; NRX-1051; NRX-1059; NRX-105x; NRX-1060; NRX-2085; NRX-20xx) – ionotropic glutamate NMDA receptor modulators – schizophrenia
  • Research programme: schizophrenia therapeutics - Myrobalan Therapeutics – synaptic transmission modulators – schizophrenia
  • RG-7410 (RG7410) – trace amine-associated receptor 1 (TAAR1) agonist – schizophrenia
  • Riluzole (PK-26124; Rilutek; RP-54274) – various actions – psychotic disorders
  • Rimonabant (Acomplia; SR-141716; SR-141716A; Zimulti) – cannabinoid CB1 receptor antagonist – schizophrenia
  • Risperidone (Risperidone LAI) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone controlled-release implant (BB0817; EN-3342) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone extended release (Risperisphere) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Roflumilast (APTA-2217; B-9302-107; BY-217; BYK-20869; Daliresp; Daxas; IN-ALR-01; Libertek) – phosphodiesterase PDE4 inhibitor – schizophrenia
  • S-14506 – serotonin 5-HT1A receptor agonist – psychotic disorders
  • Sabcomeline (BCI-224; CEB 242; Memric; SB-202026) – muscarinic acetylcholine M1 receptor agonist – schizophrenia
  • Savoxepin (CGP-19486; CGP-19486A; cipazoxapine; savoxepine) – dopamine D2 receptor antagonist – psychotic disorders
  • SDZ 208-912 (SDZ-208912; HDC-912; MAR-327; SDZ-HDC-912; SDZ-MAR-327) – dopamine D2 receptor partial agonist and other actions – psychotic disorders
  • Secretin (INN-329; RG-1068; SecreFlo) – imaging enhancer – schizophrenia (diagnosis)
  • SLV-354 (ABT-354) – serotonin 5-HT6 receptor antagonist – schizophrenia
  • Sonepiprazole (U-101387; PNU-101387) – dopamine D4 receptor antagonist – schizophrenia
  • Squalamine (ENT-01; Enterin-01; kenterin) – various actions – schizophrenia
  • SR-31742A (SR-31742) – sigma receptor modulator – schizophrenia
  • SSR-241586 (SSR241586) – neurokinin NK2 and NK3 receptor antagonist – schizophrenia
  • SSR-504734 (SSR504734) – glycine transporter 1 (GlyT1) inhibitor – schizophrenia
  • Surinabant (SR-147778; SR147778) – cannabinoid CB1 receptor antagonist – psychotic disorders
  • Suvecaltamide (CX-8998; JZP-385; MK-8998) – T-type calcium channel blocker – schizophrenia
  • TAK-915 (TAK915) – phosphodiesterase PDE2 inhibitor – schizophrenia
  • Talipexole (BHT-920; Domin) – dopamine D2 receptor agonist and α2-adrenergic receptor agonist – psychotic disorders
  • Terguride (Dironyl; Mysalfon; SH-406; Teluron; transdihydrolisuride; VUFB-6638; ZK-31224) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor partial agonist, and other actions – schizophrenia
  • Tiospirone (BMY-13859) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – psychotic disorders
  • TS-032 (PF-4802540; PF4802540; PF-04802540; PF04802540) – metabotropic glutamate mGlu2 receptor agonist – schizophrenia
  • Ulotaront (SEP-363856; SEP-856) – trace amine-associated receptor 1 (TAAR1) agonist and serotonin 5-HT1A receptor agonist – schizophrenia
  • Umespirone (KC-7218; KC-9172) – dopamine D2 receptor partial agonist, serotonin 5-HT1A receptor agonist, and α1-adrenergic receptor antagonist – psychotic disorders
  • Vabicaserin (PF-05208769; PF-5208769; SCA-136) – serotonin 5-HT2C receptor agonist – schizophrenia
  • Volinanserin (M-100907; MDL-100907) – serotonin 5-HT2A receptor antagonist – schizophrenia
  • Y-20024 – dopamine D2 receptor antagonist – psychotic disorders
  • YKP-1447 (YKP-1358) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • ZD-3638 – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, and serotonin 5-HT2 receptor antagonist – schizophrenia, psychotic disorders
  • Zelatriazin (TAK-041; NBI-1065846; NBI-846) – GPR139 agonist – schizophrenia

Clinically used drugs

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Approved drugs

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First-generation antipsychotics

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  • Chlorpromazine (Thorazine, Largactil) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Haloperidol (Haldol) – dopamine D2 and D3 receptor antagonist, sigma σ1 receptor antagonist, and other actions – schizophrenia
  • Many others...

Second-generation antipsychotics

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  • Asenapine (Atisenap; ME2136; ORG-5222; Saphris; SCH-900274; Sycrest) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Asenapine transdermal (HP-3070; Secuado) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Blonanserin (AD-5423; DSP-5423; DSP-5423P; Lonasen) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Clozapine (Clozaril) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Clozapine (clozapine ODT; clozapine once-daily; Clozapine QD; FazaClo HD; FazaClo LD; FazaClo ODT; Versacloz) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Iloperidone (Fanapt; Fanaptum; Fiapta; HP-873; ILO-522; VYV-683; Zomaril) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Lurasidone (DSP-1349M; Latuda; SM-13496; SMP-13496) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Melperone (Buronil) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Milsaperidone (Bysanti; P-88; VHX-869; VHX-896) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Olanzapine (BR-5402; LY-170053; LY-170052; Midax; Zypadhera; Zyprexa; Zyprexa Relprevv; Zyprexa Velotab; Zyprexa Zydis) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Paliperidone (9-hydroxyrisperidone; Invega; JNS-007ER; R0-76477; RO-76477) – dopamine D2 receptor antagonist and serotonin 5-HT2 receptor antagonist – schizophrenia, schizoaffective disorder
  • Paliperidone palmitate (Byannli; Invega Hafyera; Invega Sustenna; Invega Trinza; paliperidone palmitate 1–6-month; R0-92670; RO-92670; Sustenna; Trevicta; Xeplion) – dopamine D2 receptor antagonist and serotonin 5-HT2 receptor antagonist – schizophrenia, schizoaffective disorder
  • Paliperidone palmitate extended-release (Erzofri; LY-03010; Meibirui; Ruibailai) – dopamine D2 receptor antagonist and serotonin 5-HT2 receptor antagonist – schizophrenia, schizoaffective disorder
  • Perospirone (Lullan; SM-9018) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Quetiapine (FK-949; FK949E; ICI-204636; Seroquel; Seroquel XL; Seroquel XR) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone (JNJ-410397-AAA; R-64766; R064766; Risperdal; Risperdal Consta; Risperdal Depot) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone extended release (LY-03004; risperidone ER microspheres for injection; Rykindo) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone extended release (Doria; Okedi; Risperidona ISM; Risperidone-ISM; Risvan) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Risperidone long-acting injectable (Longavo; mdc-IRM; TEV-46000; TV-46000; Uzedy) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Sertindole (Serdolect) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Ziprasidone (CP-88059-01; CP-88059-1; Geodon; ME-2112; RQ-00000003; Zeldox) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Zotepine (Lodopin; Nipolept; Zoleptil) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia

Third-generation antipsychotics

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  • Aripiprazole (Abilify; Abilify Asimtufii; Abilify Maintena; Abilify MyCite; Abilitat; Ao Pai; Arlemide; Asimtufii; OPC-14597; OPC-31) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Aripiprazole lauroxil (ALNCD; ALKS-9070; ALKS-9072; Aripiprazole Lauroxil NanoCrystal Dispersion; Aristada; Aristada Initio) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Brexpiprazole (Lu-AF41156; OPC-34712; OPDC-34712; Rexulti; Rxulti) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Cariprazine (CarMP-214; Reagila; RGH-188; Symvenu; Vraylar WID-RGC20) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Lumateperone (Caplyta; ITI-007; ITI-722) – dopamine D2 receptor partial agonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia

Disputed-generation antipsychotics

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  • Amisulpride (aminosultopride; Amitrex; DAN-2163; Deniban; Enorden; Socian; Solian; Sulamid) – dopamine D2 and D3 receptor antagonist, serotonin 5-HT2B receptor antagonist, serotonin 5-HT7 receptor antagonist, and other actions – schizophrenia
  • Levosulpiride (L-sulpiride; Levobren; Levopraid; levosulpride; RV-12309) – dopamine D2 receptor antagonist, serotonin 5-HT4 receptor agonist, and other actions – psychotic disorders
  • Loxapine (Loxitane) – dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia
  • Molindone (Moban) – dopamine D2 receptor antagonist, serotonin 5-HT2B receptor antagonist, and other actions – schizophrenia
  • Nemonapride (emonapride; Emilace; YM-09151) – dopamine D2, D3, and D4 receptor antagonist and other actions – schizophrenia
  • Remoxipride (Roxiam) – dopamine D2 and D3 receptor antagonist and sigma receptor modulator – schizophrenia
  • Sulpiride (Dogmatil) – dopamine D2 and D3 receptor antagonist and other actions – schizophrenia
  • Sultopride (Barnetil, Barnotil, Topral) – dopamine D2 and D3 receptor antagonist and other actions – schizophrenia

Other antipsychotics

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  • Azacyclonol (γ-pipradrol; Ataractan; Calmeran; Frenoton; Frenquel; Psychosan) – unknown mechanism of action – schizophrenia
  • Olanzapine/samidorphan (ALKS-33/olanzapine; ALKS-3831; Lybalvi; olanzapine/ALKS 33; OLZ/SAM; Samidorphan/olanzapine) – combination of olanzapine (dopamine D1 receptor antagonist, dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions) and samidorphan (non-selective opioid receptor antagonist) – schizophrenia
  • Pimavanserin (ACP-103; BVF-048; Nuplazid) – serotonin 5-HT2A receptor inverse agonist – psychotic disorders (specifically Parkinson's disease psychosis)
  • Xanomeline/trospium chloride (BMS-986510; Cobenfy; KarXT; trospium/LY-246708; trospium/xanomeline) – combination of xanomeline (muscarinic acetylcholine M1 and M4 receptor agonist) and trospium (peripherally selective non-selective muscarinic acetylcholine receptor antagonist) – schizophrenia

Market withdrawal

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  • Remoxipride (A-33547; FLA-731; Remide; Roxiam) – dopamine D2 and D3 receptor antagonist and sigma receptor modulator – psychotic disorders
  • Risperidone sustained-release (Perseris RBP-7000) – dopamine D2 receptor antagonist, serotonin 5-HT2A receptor antagonist, and other actions – schizophrenia

Off-label drugs

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  • Reserpine (Serpasil) – vesicular monoamine transporter 2 (VMAT2) blocker and monoamine depleting agent – schizophrenia
  • Tetrabenazine (Nitoman, Xenazine) – vesicular monoamine transporter 2 (VMAT2) blocker and monoamine depleting agent – schizophrenia

See also

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References

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