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List of investigational agitation drugs

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 It is likely to become outdated with time.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)
  • Bupropion/dextromethorphan (AXS-05; Auvelity) – sigma σ<sub>1</sub> 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
  • Deudextromethorphan/quinidine (AVP-786; CTP-786; d-DM) – sigma σ<sub>1</sub> receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions, and CYP2D6 inhibitor combination
  • Masupirdine (SUVN502; SVN-502) – serotonin 5-HT<sub>6</sub> receptor antagonist

Phase 2/3

  • Deramciclane (EXV-801) – serotonin 5-HT2A receptor antagonist, serotonin 5-HT2C receptor inverse agonist, GABA reuptake inhibitor, and weak CYP2D6 inhibitor
  • Deramciclane/dextromethorphan (EXV-802; Deraphan) combination of deramciclane (serotonin 5-HT2A receptor antagonist, serotonin 5-HT2C receptor inverse agonist, GABA reuptake inhibitor, and weak CYP2D6 inhibitor) and dextromethorphan (sigma σ<sub>1</sub> receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions)

Phase 2

  • Cyclobenzaprine (KRL-102; TNX-102; Tonmya) – tricyclic antidepressant (monoamine reuptake inhibitor and monoamine receptor modulator)
  • Deulumateperone (ITI-1284; lumateperone deuterated) – atypical antipsychotic (non-selective monoamine receptor modulator)
  • Dexmedetomidine transdermal patch (DMTS; TPU-006) – α<sub>2</sub>-adrenergic receptor agonist
  • Dronabinol/palmitoylethanolamide (SCI-110; THX OSA01; THX RS01; THX-110; THX-TS01) – cannabinoid receptor modulator and other actions combination
  • KNX-100 (SOC-1) – oxytocin-like drug / indirect oxytocin receptor modulator https://adisinsight.springer.com/drugs/800056121 https://synapse.patsnap.com/drug/42d34da2e8a3426084cdfc75bfeaf334
  • ONO-2020 – immunomodulator and inflammation modulator – specifically for agitation in Alzheimer's disease
  • Pimavanserin (ACP-103; BVF-048; Nuplazid) – serotonin 5-HT<sub>2A</sub> receptor antagonist/inverse agonist
  • Soclenicant (BNC-210; IW-2143; <small>L</small>-isoleucyl-<small>L</small>-tryptophan) – α<sub>7</sub> nicotinic acetylcholine receptor negative allosteric modulator

Phase 1

  • Dexmedetomidine sublingual (iXB-120) – α<sub>2</sub>-adrenergic receptor agonist
  • NMRA-511 (BTRX-323511; NMRA-323511) – vasopressin V<sub>1A</sub> receptor antagonist
  • SAL-0114 – undefined mechanism of action

Preclinical

  • BXCL-502 – "potent and selective antagonist for a GPCR target affecting serotonergic signaling in the cerebral cortex"

Not under development

No development reported

  • Cannabidiol (RLS-102) – cannabinoid receptor modulator
  • Scyllo-inositol – β-amyloid inhibitor – specifically for agitation in Alzheimer's disease
  • SEP-380135 – undefined mechanism of action
  • Zolmitriptan (ML-004) – serotonin 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptor agonist

Development discontinued

  • ALKS-7119 ((9α,13α)-17-methylmorphinan-3-carboxamide; dextromethorphan analogue) – serotonin reuptake inhibitor and μ-opioid, α<sub>1A</sub>-adrenergic, α<sub>1B</sub>-adrenergic, NMDA, and sigma σ<sub>1</sub> receptor modulator
  • Dextromethorphan/quinidine (AVP-923; Neurodex; Nuedexta; Zenvia) – sigma σ<sub>1</sub> receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions, and CYP2D6 inhibitor combination
  • Mibampator (LY-451395) – ionotropic glutamate AMPA receptor positive allosteric modulator
  • Olanzapine intranasal (INP-105; POD™ olanzapine) – atypical antipsychotic (non-selective monoamine receptor modulator)

Clinically used drugs

Approved drugs

  • Brexpiprazole (Rexulti) – atypical antipsychotic (non-selective monoamine receptor modulator)
  • Dexmedetomidine (Igalmi) – α<sub>2</sub>-adrenergic receptor agonist
  • Loxapine inhalation (Adasuve; ALXZ-004; AZ-004; Staccato Loxapine) – antipsychotic (non-selective monoamine receptor modulator)
  • Paliperidone (Invega) – atypical antipsychotic (non-selective monoamine receptor modulator)

Off-label drugs

See also

References

External links