List of investigational antipsychotics explained

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

• 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-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

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

Acetylcholine receptor modulators

• 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

• 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

• 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

• 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

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

Others

• TS-134 (TS-1341) – undefined mechanism of action^[25]
• Kratom – Has shown antipsychotic-like effects on par with haloperidol in animal testing^{[26] [27]}

See also

• List of investigational drugs

External links

• AdisInsight – Springer
• 2016 Medicines in Development for Mental Health – PhRMA

Notes and References

1. Web site: Brilaroxazine - Reviva Biopharmaceuticals - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
2. Web site: FKF 02SC - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
3. Web site: Masupirdine - Suven Life Sciences - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
4. Web site: N-methyl amisulpride - LB pharmaceuticals - AdisInsight . 2023-02-21 . adisinsight.springer.com.
5. Web site: Ralmitaront - AdisInsight . adisinsight.springer.com . Springer . 10 July 2021.
6. Web site: SEP 363856 - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
7. Web site: SUVN D4010 - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
8. Web site: Pomaglumetad methionil - Denovo Biopharma/Eli Lilly and Company - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
9. Web site: Emraclidine - Cerevel Therapeutics - AdisInsight . 2023-02-15 . adisinsight.springer.com.
10. Web site: APN 1125 - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
11. Web site: ML 007 - AdisInsight . 2023-02-15 . adisinsight.springer.com.
12. Web site: HTL 0016878 - AdisInsight . 2023-02-21 . adisinsight.springer.com.
13. Web site: Cannabidiol - GW Pharmaceuticals - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
14. Web site: Cannabidiol - Echo Pharmaceuticals - AdisInsight . adisinsight.springer.com . 14 February 2020.
15. Web site: CVN 766 - AdisInsight . 2023-02-19 . adisinsight.springer.com.
16. Web site: Deudextromethorphan - Avanir Pharmaceuticals - AdisInsight . adisinsight.springer.com . Springer . 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. 10.1016/j.pharmthera.2016.01.016. 1879-016X. 26826604.
18. Web site: Roluperidone - Minerva Neurosciences - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
19. Web site: TAK 041 - AdisInsight . 2023-02-21 . adisinsight.springer.com.
20. Web site: Luvadaxistat - Takeda - AdisInsight . 2023-02-21 . adisinsight.springer.com.
21. Web site: MK 8189 - AdisInsight . 2023-02-21 . adisinsight.springer.com.
22. Web site: BI 409306 - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
23. Web site: Sodium benzoate - SyneuRx - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
24. Web site: Evenamide - Newron Pharmaceuticals - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
25. Web site: TS 134 - AdisInsight . adisinsight.springer.com . Springer . 14 February 2020.
26. Mitragyna speciosa Leaf Extract Exhibits Antipsychotic-Like Effect with the Potential to Alleviate Positive and Negative Symptoms of Psychosis in Mice . 2016 . 5138496 . Vijeepallam . K. . Pandy . V. . Kunasegaran . T. . Murugan . D. D. . Naidu . M. . Frontiers in Pharmacology . 7 . 464 . 10.3389/fphar.2016.00464 . 27999544 . free .
27. The Potential for Kratom as an Antidepressant and Antipsychotic . 2020 . 7309668 . Johnson . L. E. . Balyan . L. . Magdalany . A. . Saeed . F. . Salinas . R. . Wallace . S. . Veltri . C. A. . Swogger . M. T. . Walsh . Z. . Grundmann . O. . The Yale Journal of Biology and Medicine . 93 . 2 . 283–289 . 32607089 .