List of investigational agitation drugs
From Wikipedia, the free encyclopedia
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 It is likely to become outdated with time.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]
- 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[2]
- Masupirdine (SUVN502; SVN-502) – serotonin 5-HT6 receptor antagonist[3]
Phase 2/3
- Deramciclane (EXV-801) – serotonin 5-HT2A receptor antagonist, serotonin 5-HT2C receptor inverse agonist, GABA reuptake inhibitor, and weak CYP2D6 inhibitor[4][5]
- 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 σ1 receptor agonist, serotonin reuptake inhibitor, ionotropic glutamate NMDA receptor antagonist, other actions)[4][5]
Phase 2
- Cyclobenzaprine (KRL-102; TNX-102; Tonmya) – tricyclic antidepressant (monoamine reuptake inhibitor and monoamine receptor modulator)[6]
- Deulumateperone (ITI-1284; lumateperone deuterated) – atypical antipsychotic (non-selective monoamine receptor modulator)[7]
- Dexmedetomidine transdermal patch (DMTS; TPU-006) – α2-adrenergic receptor agonist[8]
- Dronabinol/palmidrol (THC/PEA; SCI-110; THX OSA01; THX RS01; THX-110; THX-TS01) – cannabinoid receptor modulator and other actions combination[9]
- Irafamdastat (BMS-986368; CC-97489) – dual fatty acid amide hydrolase (FAAH) inhibitor and monoacylglycerol lipase (MAGL) inhibitor[10]
- KNX-100 (SOC-1) – 15-lipoxygenase (15-LOX; ALOX15) inhibitor and oxytocin-like drug or indirect oxytocin receptor modulator [11][12][13]
- ONO-2020 – immunomodulator and inflammation modulator – specifically for agitation in Alzheimer's disease[14]
- Pimavanserin (ACP-103; BVF-048; Nuplazid) – serotonin 5-HT2A receptor antagonist/inverse agonist[15]
- SAL-0114 – undefined mechanism of action[16]
- Soclenicant (BNC-210; IW-2143; L-isoleucyl-L-tryptophan) – α7 nicotinic acetylcholine receptor negative allosteric modulator[17]
Phase 1
- Dexmedetomidine sublingual (iXB-120) – α2-adrenergic receptor agonist[18]
- NMRA-511 (BTRX-323511; NMRA-323511) – vasopressin V1A receptor antagonist[19]
- SEP-380135 – undefined mechanism of action[20]
Preclinical
Not under development
No development reported
- Cannabidiol (RLS-102) – cannabinoid receptor modulator[21]
- Scyllo-inositol – β-amyloid inhibitor – specifically for agitation in Alzheimer's disease[22]
- Zolmitriptan (ML-004) – serotonin 5-HT1B and 5-HT1D receptor agonist[23]
Suspended
- Latrepirdine (BXCL-502) – various actions[24][25]
Discontinued
- ALKS-7119 ((9α,13α)-17-methylmorphinan-3-carboxamide; dextromethorphan analogue) – serotonin reuptake inhibitor and μ-opioid, α1A-adrenergic, α1B-adrenergic, NMDA, and sigma σ1 receptor modulator[26][27]
- 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[28]
- Mibampator (LY-451395) – ionotropic glutamate AMPA receptor positive allosteric modulator[29]
- Olanzapine intranasal (INP-105; POD™ olanzapine) – atypical antipsychotic (non-selective monoamine receptor modulator)[30]
Clinically used drugs
Approved drugs
Antipsychotics
- Brexpiprazole (Rexulti) – atypical antipsychotic (non-selective monoamine receptor modulator)[31]
- Loxapine inhalation (Adasuve; ALXZ-004; AZ-004; Staccato Loxapine) – antipsychotic (non-selective monoamine receptor modulator)[32]
- Paliperidone (Invega) – atypical antipsychotic (non-selective monoamine receptor modulator)[33]
Others
- 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[34]
- Dexmedetomidine (Igalmi) – α2-adrenergic receptor agonist[35]
Off-label drugs
- Benzodiazepines (GABAA receptor positive allosteric modulators) (e.g., diazepam, lorazepam, midazolam)[36][37]
- Beta blockers (β-adrenergic receptor antagonists) (e.g., propranolol, pindolol, nadolol)[38]
- Cannabinoids (cannabinoid receptor agonists) (e.g., cannabis, dronabinol, nabilone)[39][40][41]
- Dissociative anesthetics (NMDA receptor antagonists) (e.g., ketamine)[42][43][44]