List of investigational generalized anxiety disorder drugs

This is a list of investigational generalized anxiety disorder drugs, or drugs that are currently under development for clinical use in the treatment of generalized anxiety disorder (GAD) but are not yet approved.

Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. The format of list items is "Name (Synonyms) – Mechanism of Action [Reference]".

This list was last comprehensively updated in September 2025. It is likely to become outdated with time.

Under development

Phase 3

• Gepirone (Ariza; BMY-13805; Exxua; Gepirone ER; MJ-13805; Org-33062; TGFK-07AD; TGFK07AD; Travivo; Variza) – serotonin 5-HT_1A receptor partial agonist https://adisinsight.springer.com/drugs/800000684
• Lysergic acid diethylamide (LSD; lysergide; MM-120; MM120) – non-selective serotonin receptor agonist and psychedelic hallucinogen https://adisinsight.springer.com/drugs/800058011 https://synapse.patsnap.com/drug/365101e3ebb7498395b34fcd68f19a5c
• Toludesvenlafaxine extended release (4-methylbenzoate desvenlafaxine; ansofaxine; desvenlafaxine prodrug; LPM-570065; LY-03005; Ruoxinlin) – serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) https://adisinsight.springer.com/drugs/800039935
• Vilazodone (EMD-68843; SB-659746A; Viibryd) – serotonin reuptake inhibitor (SRI) and serotonin 5-HT_1A receptor partial agonist https://adisinsight.springer.com/drugs/800008976

Phase 2/3

• Ulotaront (SEP-363856; SEP-856) – trace amine-associated receptor 1 (TAAR1) agonist and serotonin 5-HT_1A receptor partial agonist https://adisinsight.springer.com/drugs/800036955

Phase 2

• Desmethylcariprazine prodrug (ABBV-932; RGH-932) – dopamine D₂ and D₃ receptor partial agonist and other actions https://adisinsight.springer.com/drugs/800072633
• FKW-00GA (FKW00GA; TGW-00AA; TGW00AA) – serotonin 5-HT_1A receptor partial agonist and serotonin 5-HT_2A receptor antagonist https://adisinsight.springer.com/drugs/800029565
• Lumateperone deuterated (ITI-1284) – atypical antipsychotic (non-selective monoamine receptor modulator https://adisinsight.springer.com/drugs/800062544
• ONO-1110 – endocannabinoid synthesis regulator and indirect cannabinoid receptor modulator https://adisinsight.springer.com/drugs/800072581 https://synapse.patsnap.com/drug/4a1d21a5511d57cc2a2c1e7a98310f74 https://pryzm.ozmosi.com/product/29482
• TGFK-08AA (TGFK08AA) – serotonin 5-HT_1A receptor modulator https://adisinsight.springer.com/drugs/800032500
• Vortioxetine (Brintellix; Lu-AA21004; Trintellix; Vortidif) – serotonin reuptake inhibitor, serotonin 5-HT_1A and 5-HT_1B receptor agonist, and serotonin 5-HT_1D, 5-HT₃, and 5-HT₇ receptor antagonist https://adisinsight.springer.com/drugs/800020088

Phase 1/2

• PT-00114 (PT100114; TCAP-1) – corticotropin-releasing hormone inhibitor https://adisinsight.springer.com/drugs/800049398

Phase 1

• SPT-320 (LYT-320) – agomelatine prodrug (melatonin receptor agonist and weak serotonin 5-HT_2B and 5-HT_2C receptor antagonist)

Preclinical

• Duloxetine oral liquid – serotonin–norepinephrine reuptake inhibitor (SNRI) https://adisinsight.springer.com/drugs/800059188
• Generalised anxiety disorder therapeutic - SIMR Biotech – undefined mechanism of action https://adisinsight.springer.com/drugs/800082955
• OV-4041 – potassium–chloride cotransporter agonist https://adisinsight.springer.com/drugs/800081956
• XYL-3001 (PSYLO-3001) – serotonin 5-HT_2A receptor agonist and non-hallucinogenic psychoplastogen https://adisinsight.springer.com/drugs/800074516

Phase unknown

• Oxybutynin controlled release – non-selective muscarinic acetylcholine receptor antagonist https://adisinsight.springer.com/drugs/800046690

Not under development

Preregistration submission withdrawal

• Quetiapine (FK-949; FK949; ICI-204636; Seroquel; Seroquel XL; Seroquel XR) – atypical antipsychotic (non-selective monoamine receptor modulator) https://adisinsight.springer.com/drugs/800001768

Suspended

• Agomelatine (AGO-178; AGO178; Alodil; Melitor; S-20098; Thymanax; Valdoxan; Vestin) – melatonin MT₁ and MT₂ receptor agonist and weak serotonin 5-HT_2C receptor antagonist https://adisinsight.springer.com/drugs/800004111

No development reported

• Guanfacine extended release (Connexyn; Intuniv; Intuniv XR; S-877503; SHP-503; SPD-503) – α₂-adrenergic receptor agonist https://adisinsight.springer.com/drugs/800011997
• Riluzole sublingual (BHV-0223; Nurtec) – various actions https://adisinsight.springer.com/drugs/800043098
• Sertraline (Aremis; Besitran; CP-51974; Gladem; Lustral; Serad; Serlain; Tatig; Zoloft) – selective serotonin reuptake inhibitor (SSRI) https://adisinsight.springer.com/drugs/800006147

Discontinued

• Amibegron (SR-58611; SR-58611A) – β₃-adrenergic receptor agonist https://adisinsight.springer.com/drugs/800001600
• BTG-1640 (ABIO-08/01; ABIO-0801) – undefined mechanism of action https://adisinsight.springer.com/drugs/800003900
• Darigabat (CVL-865; PF-06372865; PF-6372865) – GABA_A receptor positive allosteric modulator https://adisinsight.springer.com/drugs/800039009
• Imagabalin (PD-0332334; PD-332334; PF-00195889) – α₂δ subunit-containing voltage-gated calcium channel ligand https://adisinsight.springer.com/drugs/800025526
• Naluzotan (PRX-00023) – serotonin 5-HT_1A receptor agonist and sigma σ₁ receptor agonist https://adisinsight.springer.com/drugs/800019899
• Ocinaplon (CL-273547) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/pyrazolopyrimidine https://adisinsight.springer.com/drugs/800001407
• Pagoclone (IP-456; Panex; RP-62955) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/cyclopyrrolone https://adisinsight.springer.com/drugs/800002118
• PF-572778 – undefined mechanism of action https://adisinsight.springer.com/drugs/800025528
• Rufinamide (Banzel; CGP-33101; E-2080; Inovelon; RUF-331; SYN-111) – sodium channel blocker and other actions https://adisinsight.springer.com/drugs/800002231
• Talaglumetad (LY-544344) – metabotropic glutamate mGlu₂ and mGlu₃ receptor agonist (eglumetad prodrug) https://adisinsight.springer.com/drugs/800018821
• Tedatioxetine (Lu-AA24530) – serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI), serotonin 5-HT_2A, 5-HT_2C, and 5-HT₃ receptor antagonist, and α_1A-adrenergic receptor antagonist https://adisinsight.springer.com/drugs/800023694

Clinically used drugs

Approved drugs

Selective serotonin reuptake inhibitors (SSRIs)

• Escitalopram (Cipralex; Entact; Lexapro; LU-26054; MLD-55; (S)-citalopram; Seroplex; Sipralex; Sipralexa) – selective serotonin reuptake inhibitor (SSRI) https://adisinsight.springer.com/drugs/800013914
• Paroxetine (Aropax; BRL-29060; Deroxat; Divarius; FG-7051; Frosinor; Motivan; NNC-207051; Paxil; Seroxat; SI-211103; Tagonis) – selective serotonin reuptake inhibitor (SSRI) https://adisinsight.springer.com/drugs/800006148
• Paroxetine (Dropax; Dropaxin; Serestill) – selective serotonin reuptake inhibitor (SSRI) https://adisinsight.springer.com/drugs/800034798

Serotonin–norepinephrine reuptake inhibitors (SNRIs)

• Duloxetine (Ariclaim; Cymbalta; LY-227942; LY-248686; Xeristar; Yentreve) – serotonin–norepinephrine reuptake inhibitor (SNRI) https://adisinsight.springer.com/drugs/800001785
• Venlafaxine (Dobupal; Efexor XR; Effexor; Effexor XR; Elafax; WY-45030; WY-45651; WY-45655) – serotonin–norepinephrine reuptake inhibitor (SNRI) https://adisinsight.springer.com/drugs/800000568

Azapirones (serotonin 5-HT_1A receptor agonists)

• Buspirone (Buspar) – serotonin 5-HT_1A receptor partial agonist and other actions
• Tandospirone (metanopirone; Sediel; SM-3997) – serotonin 5-HT_1A receptor partial agonist https://adisinsight.springer.com/drugs/800000567

GABA_A receptor positive allosteric modulators

• Alpidem (Ananxyl; SL800342; SL-800342) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/imidazopyridine – discontinued/withdrawn due to toxicity https://adisinsight.springer.com/drugs/800000646
• Alprazolam (Xanax) – GABA_A receptor positive allosteric modulator and benzodiazepine

Other drugs

• Opipramol (Ensidon; G-33040; Insidon; Nisidana) – tricyclic antidepressant (TCA) (non-selective monoamine receptor modulator and other actions) https://adisinsight.springer.com/drugs/800002007
• Pregabalin (CI-1008; isobutylgaba; Lyrica; PD-144723) – gabapentinoid (α₂δ subunit-containing voltage-gated calcium channel ligand) https://adisinsight.springer.com/drugs/800005758

Off-label drugs

• α₂-Adrenergic receptor agonists (e.g., guanfacine)
• Atypical antipsychotics (non-selective monoamine receptor modulators) (e.g., aripiprazole, olanzapine, quetiapine, risperidone, ziprasidone)
• Benzodiazepines (GABA_A receptor positive allosteric modulators) (e.g., chlordiazepoxide, clonazepam, diazepam, lorazepam)
• Beta blockers (β-adrenergic receptor antagonists) (e.g., propranolol)
• Gabapentinoids (α₂δ subunit-containing voltage-gated calcium channel ligands) (e.g., gabapentin, gabapentin enacarbil)
• GABA reuptake inhibitors (e.g., tiagabine)
• Monoamine oxidase inhibitors (MAOIs) (e.g., phenelzine, tranylcypromine)
• NMDA receptor antagonists (e.g., esketamine, ketamine)
• Nonbenzodiazepines/Z-drugs (GABA_A receptor positive allosteric modulators) (e.g., eszopiclone)
• Selective serotonin reuptake inhibitors (SSRIs) (e.g., citalopram, fluoxetine, fluvoxamine, sertraline)
• Serotonin antagonists and reuptake inhibitors (SARIs) (e.g., trazodone, nefazodone)
• Serotonin modulators and stimulators (SMSs) (e.g., vilazodone, vortioxetine)
• Tetracyclic antidepressants (TeCAs) (e.g., mirtazapine)
• Tricyclic antidepressants (TCAs) (e.g., amitriptyline, clomipramine, doxepin, imipramine)
• Others (e.g., agomelatine, bupropion, hydroxyzine)

See also

• Lists of investigational drugs
• List of investigational anxiety disorder drugs
• List of investigational social anxiety disorder drugs
• List of investigational panic disorder drugs
• List of investigational post-traumatic stress disorder drugs

References

External links

• AdisInsight - Springer