List of investigational agitation drugs

This is a dynamic list and may never be able to satisfy particular standards for completeness. You can help by adding missing items with reliable sources.

This is a list of investigational agitation drugs, or drugs that are currently under development for clinical use in the treatment of agitation, for instance in people with dementia or autism, 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 February 2025. It is likely to become outdated with time.

Under development

Phase 3

• Aripiprazole (Abilify) – atypical antipsychotic (non-selective monoamine receptor modulator) ^[1]
• Bupropion/dextromethorphan (AXS-05; Auvelity) – sigma σ₁ receptor agonist, serotonin reuptake inhibitor, norepinephrine and dopamine reuptake inhibitor, nicotinic acetylcholine receptor negative allosteric modulator, ionotropic glutamate NMDA receptor antagonist, other actions, and CYP2D6 inhibitor combination ^[2]
• Deudextromethorphan/quinidine (AVP-786; CTP-786; d-DM) – sigma σ₁ receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions, and CYP2D6 inhibitor combination ^[3]
• Masupirdine (SUVN502; SVN-502) – serotonin 5-HT₆ receptor antagonist ^[4]

Phase 2

• Cyclobenzaprine (KRL-102; TNX-102; Tonmya) – tricyclic antidepressant (monoamine reuptake inhibitor and monoamine receptor modulator) ^[5]
• Deulumateperone (ITI-1284; lumateperone deuterated) – atypical antipsychotic (non-selective monoamine receptor modulator) ^[6]
• Dexmedetomidine transdermal patch (DMTS; TPU-006) – α₂-adrenergic receptor agonist ^[7]
• Dronabinol/palmitoylethanolamide (SCI-110; THX OSA01; THX RS01; THX-110; THX-TS01) – cannabinoid receptor modulator and other actions combination ^[8]
• ONO-2020 – immunomodulator and inflammation modulator – specifically for agitation in Alzheimer's disease ^[9]
• Pimavanserin (ACP-103; BVF-048; Nuplazid) – serotonin 5-HT_2A receptor antagonist/inverse agonist ^[10]
• Soclenicant (BNC-210; IW-2143; L-isoleucyl-L-tryptophan) – α₇ nicotinic acetylcholine receptor negative allosteric modulator ^[11]

Phase 1

• Dexmedetomidine sublingual (iXB-120) – α₂-adrenergic receptor agonist ^[12]
• NMRA-511 (BTRX-323511; NMRA-323511) – vasopressin V_1A receptor antagonist ^[13]
• SAL-0114 – undefined mechanism of action ^[14]

Preclinical

• BXCL-502 – "potent and selective antagonist for a GPCR target affecting serotonergic signaling in the cerebral cortex" ^{[15] [16]}

Not under development

No development reported

• Cannabidiol (RLS-102) – cannabinoid receptor modulator ^[17]
• Scyllo-inositol – β-amyloid inhibitor – specifically for agitation in Alzheimer's disease ^[18]
• SEP-380135 – undefined mechanism of action ^[19]
• Zolmitriptan (ML-004) – serotonin 5-HT_1B and 5-HT_1D receptor agonist ^[20]

Development discontinued

• ALKS-7119 ((9α,13α)-17-methylmorphinan-3-carboxamide; dextromethorphan analogue) – serotonin reuptake inhibitor and μ-opioid, α_1A-adrenergic, α_1B-adrenergic, NMDA, and sigma σ₁ receptor modulator ^{[21] [22]}
• Dextromethorphan/quinidine (AVP-923; Neurodex; Nuedexta; Zenvia) – sigma σ₁ receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions, and CYP2D6 inhibitor combination ^[23]
• Mibampator (LY-451395) – ionotropic glutamate AMPA receptor positive allosteric modulator ^[24]
• Olanzapine intranasal (INP-105; POD™ olanzapine) – atypical antipsychotic (non-selective monoamine receptor modulator) ^[25]

Clinically used drugs

Approved drugs

• Brexpiprazole (Rexulti) – atypical antipsychotic (non-selective monoamine receptor modulator) ^[26]
• Dexmedetomidine (Igalmi) – α₂-adrenergic receptor agonist ^[27]
• Loxapine inhalation (Adasuve; ALXZ-004; AZ-004; Staccato Loxapine) – antipsychotic (non-selective monoamine receptor modulator) ^[28]
• Paliperidone (Invega) – atypical antipsychotic (non-selective monoamine receptor modulator) ^[29]

See also

• List of investigational drugs
• List of investigational aggression drugs
• List of investigational autism and pervasive developmental disorder drugs

References

1. "Bristol-Myers Squibb/Otsuka Pharmaceutical". AdisInsight. 24 January 2025. Retrieved 24 February 2025.
2. "Bupropion/dextromethorphan". AdisInsight. 18 February 2025. Retrieved 24 February 2025.
3. "Avanir Pharmaceuticals". AdisInsight. 29 January 2025. Retrieved 24 February 2025.
4. "Suven Life Sciences". AdisInsight. 28 August 2022. Retrieved 24 February 2025.
5. "Cyclobenzaprine hydrochloride very low dose". AdisInsight. 26 December 2024. Retrieved 24 February 2025.
6. "Intra-Cellular Therapies". AdisInsight. 29 January 2025. Retrieved 24 February 2025.
7. "Dexmedetomidine transdermal patch". AdisInsight. 16 October 2023. Retrieved 24 February 2025.
8. "Dronabinol/palmitoylethanolamide". AdisInsight. 19 December 2024. Retrieved 24 February 2025.
9. "ONO 2020". AdisInsight. 5 February 2025. Retrieved 24 February 2025.
10. "ACADIA Pharmaceuticals". AdisInsight. 22 November 2024. Retrieved 24 February 2025.
11. "BNC 210". AdisInsight. 30 December 2024. Retrieved 24 February 2025.
12. "Dexmedetomidine sublingual". AdisInsight. 28 January 2025. Retrieved 24 February 2025.
13. "NMRA 511". AdisInsight. 28 November 2024. Retrieved 24 February 2025.
14. "SAL 0114". AdisInsight. 15 July 2022. Retrieved 24 February 2025.
15. "BXCL 502". AdisInsight. 15 March 2022. Retrieved 24 February 2025.
16. Therapeutics, BioXcel (10 March 2022). "BioXcel Therapeutics Reports Fourth Quarter and Full Year 2021 Financial Results and Recent Operational Highlights". GlobeNewswire News Room. Retrieved 24 February 2025.
17. "Cannabidiol oral formulation". AdisInsight. 28 August 2024. Retrieved 24 February 2025.
18. "Transition Therapeutics Ireland". AdisInsight. 1 June 2021. Retrieved 24 February 2025.
19. "SEP 380135". AdisInsight. 28 August 2024. Retrieved 24 February 2025.
20. "ML 004". AdisInsight. 28 December 2024. Retrieved 24 February 2025.
21. "ALKS 7119". AdisInsight. 4 March 2017. Retrieved 24 February 2025.
22. Dijkstra FM, Zuiker RG, Siebenga PS, Leigh-Pemberton RA, Sun L, Manthis JD, de Kam ML, Lin R, von Moltke LL, Rezendes D, van Gerven JM (June 2022). "Pharmacological profile of ALKS 7119, an investigational compound evaluated for the treatment of neuropsychiatric disorders, in healthy volunteers". Br J Clin Pharmacol. 88 (6): 2909–2925. doi:10.1111/bcp.15229. PMC   9302689 . PMID   35014069.
23. "Dextromethorphan/quinidine". AdisInsight. 5 November 2023. Retrieved 24 February 2025.
24. "Mibampator". AdisInsight. 2 October 2021. Retrieved 24 February 2025.
25. "Olanzapine intranasal". AdisInsight. 13 October 2023. Retrieved 24 February 2025.
26. "Lundbeck/Otsuka". AdisInsight. 14 January 2025. Retrieved 24 February 2025.
27. "BioXcel Therapeutics". AdisInsight. 17 October 2024. Retrieved 24 February 2025.
28. "Alexza Pharmaceuticals". AdisInsight. 2 October 2021. Retrieved 24 February 2025.
29. "Johnson & Johnson". AdisInsight. 1 July 2020. Retrieved 24 February 2025.

External links

• AdisInsight - Springer