List of investigational anxiety disorder drugs

Investigational anxiety disorder drugs From Wikipedia, the free encyclopedia

This is a list of investigational anxiety disorder drugs, or drugs that are currently under development for clinical use in the treatment of anxiety disorders (type unspecified) 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 It is likely to become outdated with time.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

Lysergic acid diethylamide (LSD; lysergide; MM-120; MM120) – non-selective serotonin receptor agonist and psychedelic hallucinogen ^[1]
Ranquilon (6-phenylhexanoyl)glycyl-L-tryptophan amide; GB-115) – cholecystokinin (CCK) receptor antagonist
Soclenicant (BNC-210; BNC210; IW-2143; L-isoleucyl-L-tryptophan) – α₇-nicotinic acetylcholine receptor negative allosteric modulator

Phase 2

BAER-101 (AZ-7325; AZD-7325) – selective GABA_A α₂ and α₃ subunit-containing receptor positive allosteric modulator and nonbenzodiazepine/cinnoline^[2]^[3]^[4]
Brexanolone caprilcerbate (Glyph Allopregnanolone; GlyphAllo; LYT-300; SPT-300; allopregnanolone prodrug) – GABA_A receptor positive allosteric modulator and neurosteroid (brexanolone prodrug)
Cannabidiol (CBD; Arvisol) – cannabinoid receptor modulator and other actions
Cenobamate (ONO-2017; Ontozry; X-Copri; Xcopri; YKP-3089) – atypical voltage-gated sodium channel blocker and GABA_A receptor positive allosteric modulator ^[5]
JNJ-42165279 (JNJ-5279) – fatty acid amide hydrolase (FAAH) inhibitor
Maritupirdine (CD-008-0045) – serotonin 5-HT₆ receptor antagonist
Psilocybin low dose (APEX-52) – non-selective serotonin receptor agonist and psychedelic hallucinogen
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
Zuranolone (BIIB-125; S-812217; SAGE-217; SGE-797; Zurzuvae) – GABA_A receptor positive allosteric modulator and neurosteroid

Phase 1

Etifoxine deuterated (deuterated etifoxine; GRX-917) – GABA_A receptor positive allosteric modulator, translocator protein (TSPO) agonist, and nonbenzodiazepine/benzoxazine
KAR-2618 (GFB-887; TRPC4/5 inhibitor) – transient receptor potential TRPC4 and TRPC5 cation channel inhibitor
SNTX-2643 (SENS-01) – atypical serotonin reuptake inhibitor (SRI) (kanna-derived) ^[6]
Transient receptor potential channel 4/5 inhibitor - Bristol-Myers Squibb – transient receptor potential TRPC4 and TRPC5 cation channel inhibitor

Preclinical

EB-002 (EB-373; psilocin prodrug) – non-selective serotonin receptor agonist and psychedelic hallucinogen
Midomafetamine (MDMA; ecstasy) microneedle patch – serotonin–norepinephrine–dopamine releasing agent, weak serotonin 5-HT₂ receptor agonist, and entactogen
Nerinetide (NA-1; Tat-NR2B9c) – PDZ domain inhibitor
OV-4041 – potassium–chloride-cotransporter agonist
PSIL-025 – serotonin 5-HT₁ receptor modulator

Phase unknown

INV-407 – undefined mechanism of action

Not under development

No development reported

ACH-36 – undefined mechanism of action
Alprazolam sublingual – GABA_A receptor positive allosteric modulator and benzodiazepine
Antalarmin (CP-154526) – corticotropin-releasing hormone (CRH) inhibitor
Buspirone controlled release (Buspirone ER) – serotonin 5-HT_1A receptor partial agonist and other actions
BW-723C86 – serotonin 5-HT_2B and 5-HT_2C receptor agonist
Cannabidiol dry powder inhalation (RLS-103) – cannabinoid receptor modulator and other actions
Darigabat (CVL-865; PF-06372865; PF-6372865) – GABA_A receptor positive allosteric modulator
Divaplon (RU-32698) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/imidazolpyrimidine
Fananserin (RP-62203) – serotonin 5-HT_2A receptor antagonist and dopamine D₄ receptor antagonist
FR260010 (FR-260010) – serotonin 5-HT_2C receptor antagonist
GSK-588045 (GSK588045) – serotonin 5-HT_1A, 5-HT_1B, and 5-HT_1D receptor antagonist
GSK-1360707 – serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI)
GT-001 – GABA_A receptor positive allosteric modulator
Guanfacine extended release (Connexyn; Intuniv; Intuniv XR; S-877503; SHP-503; SPD-503) – α₂-adrenergic receptor agonist
Itriglumide (CR-2945) – cholecystokinin B (CCK_B) receptor antagonist
Lohocla-201 (Kindolor) – various actions
LY-293284 – serotonin 5-HT_1A receptor agonist
NMRA-511 (BTRX-323511; NMRA-323511) – vasopressin V_1A receptor antagonist
Paroxetine (Aropax; BRL-29060; Deroxat; Divarius; FG-7051; Frosinor; Motivan; NNC-207051; Paxil; Seroxat; SI-211103; Tagonis) – selective serotonin reuptake inhibitor (SSRI)
Psilocybin (MYCO-001; MYCO-003) – non-selective serotonin receptor agonist and psychedelic hallucinogen
PT-00114 (PT100114) – corticotropin-releasing hormone (CRH) inhibitor
Research programme: allosteric modulators - Addex Therapeutics – various actions
Research programme: AMPA receptor agonists - RespireRx (ampakines; CX compounds) – AMPA receptor agonists and brain-derived neurotrophic factor (BDNF) stimulants
Research programme: anxiety and neurological disorder therapeutics - AstraZeneca – various actions
Research programme: cannabis-based therapeutics - Skye Bioscience – cannabinoid receptor agonists
Research programme: neuropeptide S receptor modulators - Pfizer (WYE-198232) – neuropeptide receptor agonists
Research programme: oxytocin receptor agonist - Wyeth – oxytocin receptor agonists
RGH-618 – metabotropic glutamate mGlu₅ receptor negative allosteric modulator ^[7]
Riluzole (PK-26124; Rilutek; RP-54274) – various actions
Risperidone (JNJ-410397-AAA; R-64766; R064766; Risperdal; Risperdal Consta; Risperdal Depot) – atypical antipsychotic (non-selective monoamine receptor modulator)
Saripidem (SL-850274) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/imidazopyridine
SB-242084 (SB242084) – serotonin 5-HT_2C receptor antagonist
SRX-246 (API-246) – vasopressin V_1A receptor antagonist
SYT-510 – anandamide reuptake inhibitor
Tebideutorexant (JNJ-3215; JNJ-61393215; Orexin-1) – orexin OX₁ receptor antagonist
WAY-100135 – serotonin 5-HT_1A receptor antagonist
Ziprasidone (CP-88059-01; CP-88059-1; Geodon; ME-2112; RQ-00000003; Zeldox) – atypical antipsychotic (non-selective monoamine receptor modulator)

Discontinued

1-Amino-5-bromouracil (ABU) – undefined mechanism of action
ABT-418 – nicotinic acetylcholine receptor agonist
ABT-436 – vasopressin V_1B receptor antagonist
Adipiplon (NG-273) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine
Alnespirone (S-20499) – serotonin 5-HT_1A receptor agonist
Alosetron (GR-68755; GR-68755C; Lotronex) – serotonin 5-HT₃ receptor antagonist
Alpidem (Ananxyl; S-800342-001; SL-800342) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/imidazopyridine
Alprazolam lingual spray – GABA_A receptor positive allosteric modulator and benzodiazepine
AN-788 (IP-2018; NSD788) – serotonin–dopamine reuptake inhibitor (SDRI)
AP-521 – serotonin 5-HT_1A receptor partial agonist
Aprepitant (Emend; L-754030; MK-0869; MK-869; ONO-7436) – neurokinin NK₁ receptor antagonist
AVN-211 (CD-008-0173) – serotonin 5-HT₆ receptor antagonist
AVN-397 – undefined mechanism of action
AZD-2327 – δ-opioid receptor (DOR) agonist
AZD-8129 (AR-A000002; AR-A2XX; AR-A2) – serotonin 5-HT_1B receptor antagonist
Befloxatone (MD-370503) – reversible inhibitor of monoamine oxidase A (RIMA)
Blarcamesine (AE-37; ANA001; ANAVEX 2-73) – sigma σ₁ receptor agonist, muscarinic acetylcholine M₁ receptor agonist, and ionotropic glutamate NMDA receptor agonist
Bretazenil (RO-166028) – GABA_A receptor positive allosteric modulator and benzodiazepine
Brofaromine (Brofaremine; CGP-11305A; Consonar; Consonev) – reversible inhibitor of monoamine oxidase A (RIMA) and serotonin reuptake inhibitor (SRI)
Buspirone transdermal (BuSpar Patch) – serotonin 5-HT_1A receptor partial agonist and other actions
CGS-12066 – serotonin 5-HT_1B receptor partial agonist and other actions
Coluracetam (BCI-540; MKC-231) – ionotropic glutamate AMPA receptor positive allosteric modulator, choline uptake and acetylcholine synthesis enhancer, and racetam
DAA-1097 – translocator protein (TSPO) agonist
Devazepide (Devacade; L-364718; MK-329) – Cholecystokinin A (CCK_A) receptor antagonist
Dipraglurant (ADX-48621; mGluR5-NAM) – metabotropic glutamate mGlu₅ receptor negative allosteric modulator
Eglumetad (eglumegad; LY-354740) – metabotropic glutamate mGlu₂ and mGlu₃ receptor agonist
Emapunil (AC-5216; XBD173) – translocator protein (TSPO) agonist
Emicerfont (GW-876008; GW876008) – corticotropin releasing factor CRF₁ receptor antagonist
Enciprazine (D-3112; WY-48624) – serotonin 5-HT_1A receptor agonist and α₁-adrenergic receptor ligand
Eplivanserin (Ciltyri; Sliwens; SR-46349; SR-46349B; SR-46615A) – serotonin 5-HT_2A receptor antagonist
Eptapirone (F-11440) – serotonin 5-HT_1A receptor agonist
Esprolol ((S)-ACC-9369) – beta blocker (β-adrenergic receptor antagonist) (amoxolol prodrug) ^[8]
Flesinoxan (DU-29373) – serotonin 5-HT_1A receptor agonist
Gabapentin (CI-945; Gabapen; GOE-3450; Neurontin) – gabapentinoid (α₂δ subunit-containing voltage-gated calcium channel ligand)
Girisopam (EGIS-5810; GYKI-51189) – GABA_A receptor positive allosteric modulator and benzodiazepine
GT-2203 – histamine H₃ receptor agonist
Guanfacine (Guanfacine Carrier Wave project; SPD-554) – α₂-adrenergic receptor agonist
Ipsapirone (BAY-Q-7821; TVX-Q-7821) – serotonin 5-HT_1A receptor partial agonist
Isamoltane (CGP-361A) – beta blocker (β-adrenergic receptor antagonist) and serotonin 5-HT_1A and 5-HT_1B receptor antagonist
Itasetron (DAU-6215; U-98079) – serotonin 5-HT₃ receptor antagonist
ITI-333 – serotonin 5-HT_2A receptor antagonist, dopamine D₁ receptor antagonist, α_1A-adrenergic receptor antagonist, and μ-opioid receptor (MOR) partial agonist
JNJ-19567470 (CRA-5626; R-317573) – corticotropin releasing factor CRF₁ receptor antagonist
Levetiracetam (Keppra; L-059; SIB-S1; UCB-059; UCB-22059; UCB-L059) – synaptic vesicle glycoprotein 2A (SV2A) ligand
Lorazepam intranasal – GABA_A receptor positive allosteric modulator and benzodiazepine
Mavoglurant (AFQ-056; STP-7) – metabotropic glutamate mGlu₅ receptor antagonist
Midazolam intranasal (ITI-111; midazolam nasal spray; Nayzilam; USL-261) – GABA_A receptor positive allosteric modulator and benzodiazepine
MK-0777 (L-830982; TPA-023) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/triazolopyridazine
NBI-34041 (SB-723620) – corticotropin-releasing hormone (CRH) inhibitor
Nerisopam (EGIS-6775; GYKI-52322) – GABA_A receptor positive allosteric modulator and benzodiazepine
Nivasorexant (ACT-539313; SORA) – orexin OX₁ receptor antagonist
NS-11821 (NS11821) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine ^[3]^[9]
Orvepitant (GW-823296; GW823296X) – neurokinin NK₁ receptor antagonist
Osanetant (ACER-801; SR-142801; SR-142806) – neurokinin NK₃ receptor antagonist
Panadiplon (FD-10571; FG-10571; NNC-140571; U-78875) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/pyrazolopyrimidine
Pazinaclone (A-77000; DN-2327) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/cyclopyrrolone
Pozanicline (A-87089.0; ABT-089) – nicotinic acetylcholine receptor agonist
Psilocybin (CYB-001; INT0052/2020) – non-selective serotonin receptor agonist and psychedelic hallucinogen
Research programme: depression and anxiety therapies - Roche/Vernalis – undefined mechanism of action
Research programme: GPCR modulators - Nxera Pharma – various actions
Research programme: monoamine oxidase A inhibitors - CeNeRx BioPharma – monoamine oxidase A (MAO-A) inhibitors
Ritanserin (R-55667) – serotonin 5-HT₂ receptor antagonist and other actions
Robalzotan (AZD-7371; NAD-299) – serotonin 5-HT_1A receptor antagonist
RS-127445 (MT-500) – serotonin 5-HT_2B receptor antagonist
SAX-187 (WAY-181187) – serotonin 5-HT₆ receptor agonist
Sergolexole (LY-281067) – serotonin 5-HT₂ receptor antagonist
Siramesine (LU-28179) – sigma σ₂ receptor agonist
SKL-PSY (FZ-016) – serotonin 5-HT_1A receptor agonist
SSR-241586 (SSR241586) – neurokinin NK₂ and NK₃ receptor antagonist
SUN-8399 – serotonin 5-HT_1A receptor agonist
Suriclone (RP-31264) – GABA_A receptor positive allosteric modulator and nonbenzodiazepine/cyclopyrrolone
Talaglumetad (LY-544344) – metabotropic glutamate mGlu₂ and mGlu₃ receptor agonist (eglumetad prodrug)
Tiagabine (A-70569; CEP-6671; Gabitril; NO-050328; NO-328) – GABA transporter 1 (GAT-1) blocker and GABA reuptake inhibitor^[10]
Troriluzole (BHV-4157; Dazluma; FC-4157; trigriluzole) – various actions (riluzole prodrug)
Vestipitant (GW-597599) – neurokinin NK₁ receptor antagonist
Zabaglurant (TMP-301; TMP301; Heptares 25; HTL-0014242; HTL14242) – metabotropic glutamate mGlu₅ receptor negative allosteric modulator
Zalospirone (WY-47846) – serotonin 5-HT_1A receptor agonist

Clinically used drugs

Approved drugs

Emoxypine (ethylmethylhydroxypyridine; Mexidol) – antioxidant and unknown mechanism of action
Tandospirone (metanopirone; Sediel; SM-3997) – serotonin 5-HT_1A receptor partial agonist
Tianeptine (Coaxil; Stablon; Tatinol) – weak atypical μ-opioid receptor agonist and other actions

References

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Robison R, Barrow R, Conant C, Foster E, Freedman JM, Jacobsen PL, Jemison J, Karas SM, Karlin DR, Solomon TM, Halperin Wernli M, Fava M (September 2025). "Single Treatment With MM120 (Lysergide) in Generalized Anxiety Disorder: A Randomized Clinical Trial". JAMA. doi:10.1001/jama.2025.13481. PMID 40906494.
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"BAER 101". AdisInsight.
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Maramai S, Benchekroun M, Ward SE, Atack JR (April 2020). "Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABAAR) Modulators Acting at the Benzodiazepine Binding Site: An Update". J Med Chem. 63 (7): 3425–3446. doi:10.1021/acs.jmedchem.9b01312. hdl:11365/1214874. PMID 31738537.
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Roberti R, De Caro C, Iannone LF, Zaccara G, Lattanzi S, Russo E (June 2021). "Pharmacology of Cenobamate: Mechanism of Action, Pharmacokinetics, Drug-Drug Interactions and Tolerability". CNS Drugs. 35 (6): 609–618. doi:10.1007/s40263-021-00819-8. PMID 33993416.
[6]
Cross, Ryan (19 August 2025). "Exclusive: Sensorium raises $25M to test succulent-derived drug for anxiety". Endpoints News. The company zeroed in on a molecule derived from a South African succulent known to scientists as Sceletium tortuosum and commonly referred to as kanna. [...] the company's drug "was inspired by a unique natural product found among the diverse molecules," but did not confirm if it came from mesembrine. Chewing kanna is linked to rapid calming action within 30 to 60 minutes, [...] Other researchers have previously shown that kanna inhibits the serotonin transporter, an important protein that moves serotonin in and out of the junctions between brain cells. Antidepressants called selective serotonin reuptake inhibitors (SSRIs) also block the serotonin transporter, but typically take four to six weeks for their effects to kick in, creating a puzzle about why the succulent compound worked so quickly. "We were convinced, quite frankly, that it must be hitting some target that we don't know about," Hooker said. "And we went deep. We looked at many hundreds, if not a thousand or more targets." It turned out that the molecule was binding to the serotonin transporter — a bit of a disappointment at first, given the startup's novel mechanism mandate. However, while SSRIs directly block the ability of serotonin to bind to the transporter, Hooker said he was surprised to find that Sensorium's compound binds to a different site on the protein that doesn't compete with serotonin binding. Hooker is writing a paper to describe the mechanism in more detail. The company is also still trying to figure out exactly why touching the transporter differently has such a seemingly rapid action. Early work suggests it is rooted in downstream signaling proteins called kinases that "fundamentally tune the circuit differently," he said. [...] Sensorium has created hundreds of derivatives of the natural molecule to make a version dubbed SNTX-2643, which can be taken orally once a day. Hooker hopes it will provide an alternative to anxiety medications, including SSRIs and benzodiazepines. Hooker declined to say when the Phase 1 study would wrap up.
[7]
Galambos J, Domány G, Nógrádi K, Wágner G, Keserű GM, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Kóti J, Szakács Z, Béni Z, Gál K, Szombathelyi Z, Greiner I (February 2016). "4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate". Bioorg Med Chem Lett. 26 (4): 1249–1252. doi:10.1016/j.bmcl.2016.01.024. PMID 26774652.
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Matier WL, Patil G (2000). "Esprolol hydrochloride: a new beta adrenergic antagonist with a rapid onset of effect". Heart Dis. 2 (2): 146–150. PMID 11728252.
[9]
Zuiker RG, Chen X, Østerberg O, Mirza NR, Muglia P, de Kam M, Klaassen ES, van Gerven JM (March 2016). "NS11821, a partial subtype-selective GABAA agonist, elicits selective effects on the central nervous system in randomized controlled trial with healthy subjects". J Psychopharmacol. 30 (3): 253–262. doi:10.1177/0269881115620435. PMID 26655084.
[10]
"Tiagabine". AdisInsight. 24 October 2021. Retrieved 17 January 2026.