List of investigational tinnitus drugs

This is a list of investigational tinnitus drugs, or drugs that are currently under development for clinical use in the treatment of tinnitus 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 It is likely to become outdated with time.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 2

• Brexanolone (allopregnanolone; SAGE-547; SGE-102; Zulresso) – GABA_A receptor positive allosteric modulator and neurosteroid https://adisinsight.springer.com/drugs/800039944
• Ebselen (DR-3305; ebselene; ebseleno; ebselenum; harmokisane; PZ-51; SPI-1005; SPI-3005) – various actions https://adisinsight.springer.com/drugs/800000622

Not under development

Suspended

• Esketamine ((S)-ketamine; AM-101; esketamine otic gel; Keyzilen) – ionotropic glutamate NMDA receptor antagonist https://adisinsight.springer.com/drugs/800023242

No development reported

• AM-102 (AM102) – sodium–potassium–chloride symporter inhibitor https://adisinsight.springer.com/drugs/800057079
• AUT-00063 – shaw potassium channel modulator https://adisinsight.springer.com/drugs/800038170
• Disufenton/acetylcysteine (disufenton/N-acetylcysteine; HPN-07/NAC; NHPN-1010; NXY-059/NAC) – free radical inhibitor and oxygen radical scavenger https://adisinsight.springer.com/drugs/800040379
• EGb-761 (GBE 761; Gingogink; Ginkgo biloba special extract; Tanakan; Tebonin; Tramisal) – various actions https://adisinsight.springer.com/drugs/800002008
• (R)-Ketoprofen – cyclooxygenase (COX) inhibitor and non-steroidal anti-inflammatory drug (NSAID) https://adisinsight.springer.com/drugs/800007136
• Research programme: fluorine-based therapeutics/radiolabelled diagnostics - OcuTerra Therapeutics (SF-0034) – various actions https://adisinsight.springer.com/drugs/800038297
• Seliforant (SENS-111; UR-63325) – histamine H₄ receptor antagonist https://adisinsight.springer.com/drugs/800031434

Discontinued

• Gacyclidine intratympanic controlled release – ionotropic glutamate NMDA receptor antagonist https://adisinsight.springer.com/drugs/800039283
• Lidocaine transdermal patch (ADL-87223; LidoPAIN) – sodium channel blocker https://adisinsight.springer.com/drugs/800018527
• Neramexane (KRP-209; MRZ 2/579) – ionotropic glutamate NMDA receptor antagonist and nicotinic acetylcholine receptor negative allosteric modulator https://adisinsight.springer.com/drugs/800009609
• Selurampanel (BGG-492; BGG-492A) – ionotropic glutamate AMPA and kainate receptor antagonist https://adisinsight.springer.com/drugs/800030122
• Sodium phenylbutyrate slow-release (4-PB-D-alanin; LU-901; Lunaphen) – histone deacetylase (HDAC) inhibitor https://adisinsight.springer.com/drugs/800024870
• Vestipitant (GW-597599; GW-597599B) – neurokinin NK₁ receptor antagonist https://adisinsight.springer.com/drugs/800015473

Clinically used drugs

Approved drugs

• Caroverine (Spasmium, Tinnitin, Tinnex) – calcium channel blocker, NMDA receptor antagonist, and other actions
• Pentoxifylline (BL-191; Claudicat; Dospan Pento; Elorgan; oxpentifylline; Trental) – non-selective phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist https://adisinsight.springer.com/drugs/800008036
• Trimetazidine (Adexor; Flavedon; Idaptan; Preductal; S-5016; Trimetazine; Vastarel; Vastinan) – long-chain 3-ketoacyl-CoA thiolase inhibitor and other actions https://adisinsight.springer.com/drugs/800008502

Off-label drugs

• Antidepressants (e.g., sertraline, nortriptyline, amitriptyline)
• Benzodiazepines (GABA_A receptor positive allosteric modulators) (e.g., alprazolam, clonazepam)
• Corticosteroids (e.g., dexamethasone)
• Gabapentinoids (α₂δ subunit-containing voltage-gated calcium channel ligands) (e.g., gabapentin)
• Others (e.g., acamprosate, melatonin)

See also

• Lists of investigational drugs

References

External links

• AdisInsight - Springer