- Introduction
- Antipsychotics under Development（As of June 1, 2026）
- Muscarinic agonists（Muscarinic acetylcholine receptor agonists）
- TAAR1 agonists（Trace Amine-Associated Receptor 1 Agonists）
- PDE inhibitors（Phosphodiesterase inhibitors）
- Glutamate modulators
- Neuroplasticity promoters
- New atypical antipsychotics
- Other mechanisms of action
- Medications for cognitive impairment
- Medications for negative symptoms
- References
Introduction
This article provides a list of antipsychotic drugs currently under development in the United States. While this list is not intended to be exhaustive, I believe it is significantly more comprehensive and detailed than the list of antipsychotics found on the Wikipedia.
The text below is quite long, so feel free to skip this section for now. You can just look at the list if you prefer. Please read the text if you feel like it.
Percentage of Drugs in Phases 1–3 That Reach Market Release
What this blog offers that Wikipedia does not is information on the development stage as of June 2026. I have listed which stage each drug is in: Phase 1, Phase 2, Phase 3, or preclinical.
For schizophrenia medications, the percentage of drugs in each phase that ultimately reach the market is as follows:
- Phase 1: 6–8%
- Phase 2: 12–15%
- Phase 3: 45–55%
The number of drugs that actually reach the market is quite low. This is because trials sometimes fail to demonstrate efficacy or safety. Even if a drug reaches Phase 3 trials, half of them will not be released.
Time to market for drugs in Phases 1–3
In general, the time it takes for a drug in each phase to reach the market is as follows:
- 6–9 years from the start of Phase 1 trials
- 4–7 years from the start of Phase 2 trials
- 2–4 years from the start of Phase 3 trials
For example, if a drug is listed as “Phase 1 (US)” in the list below, it means it will be released in the U.S. within 6 to 9 years. However, as mentioned earlier, only 6–8% of drugs in Phase 1 actually make it to market.
Alternatively, if a drug is listed as “Phase 3 (US),” it will be released in the U.S. within 2 to 4 years. However, since clinical trials can fail, only 45–55% of these drugs ultimately reach the market.
However, in recent years, the FDA, the regulatory authority, has sometimes granted designations such as Fast Track, Breakthrough Therapy, and Priority Review. In such cases, the development timeline is shortened by 1 to 3 years.
In the list below, drugs are categorized by mechanism of action, with each category forming a separate section. Additionally, sections for drugs treating cognitive impairment and negative symptoms have been included at the end.
Antipsychotics under Development（As of June 1, 2026）
Muscarinic agonists（Muscarinic acetylcholine receptor agonists）
| ML-007 | M1/M4 agonist（Acts on M1 & M4 receptor subtypes） | Phase２(US) |
| NBI-1117570 | M1/M4 agonist | Phase２(US) |
| ST-905 | M1/M4 agonist | Phase１(US) |
| Gilgamesh Pharma‘s drug | M1/M4 agonist | Preclinical (US) |
| Direclidine(NBI-1117568) | M4 agonist（Acts on M4 receptor subtype） | Phase３(US) |
| GXV813 | M4 agonist | Phase２(US) |
| ANAVEX3-71 | M1 agonist、Sigma-1 receptor agonist | Phase２(US) |
| NS-136 | M4 allosteric agonist（M4 positive allosteric modulator, M4 PAM） | Phase２(US) |
| Emraclidine | M4 allosteric agonist | Phase２(US) |
| NMRA-861 | M4 allosteric agonist | Phase１(US) |
| NMRA-898 | M4 allosteric agonist | Phase１(US) |
| NTX-253 | M4 allosteric agonist | Phase１(US) |
TAAR1 agonists（Trace Amine-Associated Receptor 1 Agonists）
| Ulotaront(SEP-363856) | TAAR1 agonist、Serotonin 1A receptor agonist | Phase３(US) |
| LY03020 | TAAR1 agonist、Serotonin 2C receptor agonist | Phase１(China) |
| Ralmitaront(RG7906、RO6889450) | TAAR1 partial agonist | Phase２Discontinued(US) |
PDE inhibitors（Phosphodiesterase inhibitors）
| CPL’36 | PDE10A inhibitor | Phase３(US) |
| Balipodect | PDE10A inhibitor | Phase３(US) |
| EM-221 | PDE10A inhibitor | Phase２(US) |
| Osoresnontrine(BI-409306) | PDE９A inhibitor | Phase２(US) |
Glutamate modulators
| Evenamide(EA8001) | Selective inhibitor of voltage-gated sodium channels | Phase３(US) |
| Pomaglumetad methionil(DB-103) | mGluR2 and mGluR3 agonist（Agonist of the Group II & Ⅲ metabotropic glutamate receptors） | Phase２(US) |
| SKL20540 | mGluR5 agonist（Agonist of the Group Ⅴ metabotropic glutamate receptors） | Phase１(US) |
| LTX-001 | Glutaminase inhibitor | Phase１(US) |
Neuroplasticity promoters
| Tazbentetol(SPG302) | Synaptic transmission modulators | Phase２(US) |
| Delix Therapeutics‘s drug | Neuroplastogen | Preclinical (US) |
New atypical antipsychotics
| Brilaroxazine(oxaripiprazole) | Dopamine2 receptor partial agonist Serotonin2A receptor antagonist, other actions | Phase３(US) |
| LB-102(N-methyl amisulpride) | Dopamine2、Dopamine3 & Serotonin7、Serotonin2B receptor antagonist | Phase３(US) |
| FKF-02SC(TGOF-02N) | Dopamine2 & Serotonin2A receptors antagonist, other actions | Phase２(US) |
Other mechanisms of action
| AM-01 | (Medications that reduce the life-threatening side effects of clozapine.) | Phase３(US) |
| NaBen(Sodium Benzoate, Clozaben) | D-amino acid oxidase inhibitor | Phase2/3(US) |
| Deudextromethorphan(AVP-786, CTP-786) | Sigma-1 receptor agonist, Serotonin-Norepinephrine Reuptake Inhibitor、non-competitive NMDA receptor antagonist, Muscarinic agonist, other actions | Phase2/3(US) |
| Masupirdine(SUVN-502) | Serotonin６receptor antagonist | Phase２(US) |
| Luvadaxistat(TAK-831) | D-amino acid oxidase inhibitor | Phase２(US) |
| SP-624 | SIRT6 stimulants(anti-aging, DNA repair, and metabolic regulation) | Phase１/2(US) |
| AVAT-021(Cannabidiol, CBD) | Cannabinoid receptor modulator, antioxidant, other actions | Phase１(US) |
| CVN766 | Orexin receptor type 1 antagonist | Phase１(US) |
| TS-134 | undefined mechanism of action | Phase１(US) |
| NXE0048149 | GPR52 agonist（G protein-coupled receptor 52） | Phase１(US) |
| OV4071 | KCC2 direct activator (Potassium-chloride cotransporter 2 direct activator) | Phase１(US) |
| Autifony Therapeutics‘s drug | Kv3 potassium channel modulator | Preclinical (US) |
Medications for cognitive impairment
| Inidascamine(RL-007) | Acetylcholine receptor modulator, GABA_B receptor modulator, NMDA receptor modulator | Phase２(US) |
| KYN-5356 | Kynurenine-oxoglutarate transaminase inhibitor | Phase２(US) |
| VQW-765 | Alpha7 nicotinic acetylcholine receptor agonist | Phase２(US) |
| ASP-4345 | Dopamine D1 receptor positive allosteric modulator | Phase２(US) |
| GT-002 | GABA_A receptor positive allosteric modulator | Phase２(Denmark) |
| ALTO-101 | PDE４ inhibitor | Phase２Failure(US) |
| SKL-15508 | Alpha7 nicotinic acetylcholine receptor agonist | Phase1/２(US) |
| MT1988 | Nicotinic receptor agonists | Phase１(US) |
| Plazinemdor | NMDA receptor positive allosteric modulator | Phase１(US) |
| NXE0041178 | GPR52 agonist（G protein-coupled receptor 52） | Unknown |
| Samelisant | Histamine H3 receptor inverse agonist | Unknown |
| Usmarapride(SUVN-D4010) | Serotonin4 receptor partial agonist | Unknown |
| BMS-955829 | ｍGluR5 positive allosteric modulator（Positive allosteric modulator of metabotropic glutamate 5） | Unknown |
| ASP-5736 | Serotonin5A receptor antagonist | Unknown |
Medications for negative symptoms
| Roluperidone | Serotonin2A & Sigma-2 receptors agonist | Phase３(US) |
| CT-155 | Smartphone app | Phase３(US) |
| Vafidemstat | LSD1 inhibitor（Lysine specific demethylase 1 inhibitor） | Phase２(US) |
| LY03017 | Serotonin2A inverse agonist | Phase１(US) |
For more information about drugs for cognitive and negative symptoms, see this article.
22 Drugs for Cognitive and Negative Symptoms of Schizophrenia