Chemistry:List of investigational tinnitus drugs

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Short description: Investigational tinnitus drugs
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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 It is likely to become outdated with time.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) – GABAA receptor positive allosteric modulator and neurosteroid [1]
  • Ebselen (DR-3305; ebselene; ebseleno; ebselenum; harmokisane; PZ-51; SPI-1005; SPI-3005) – various actions [2][1]

Not under development

Suspended

  • Esketamine ((S)-ketamine; AM-101; esketamine otic gel; Keyzilen) – ionotropic glutamate NMDA receptor antagonist [3][2][3]

No development reported

  • AM-102 (AM102) – sodium–potassium–chloride symporter inhibitor [4]
  • AUT-00063 – shaw potassium channel modulator [5]
  • Disufenton/acetylcysteine (disufenton/N-acetylcysteine; HPN-07/NAC; NHPN-1010; NXY-059/NAC) – free radical inhibitor and oxygen radical scavenger [6]
  • EGb-761 (GBE 761; Gingogink; Ginkgo biloba special extract; Tanakan; Tebonin; Tramisal) – various actions [7][4]
  • (R)-Ketoprofen – cyclooxygenase (COX) inhibitor and non-steroidal anti-inflammatory drug (NSAID) [8]
  • Research programme: fluorine-based therapeutics/radiolabelled diagnostics - OcuTerra Therapeutics (SF-0034) – various actions [9]
  • Seliforant (SENS-111; UR-63325) – histamine H4 receptor antagonist [10]

Discontinued

  • Gacyclidine intratympanic controlled release – ionotropic glutamate NMDA receptor antagonist [11]
  • Lidocaine transdermal patch (ADL-87223; LidoPAIN) – sodium channel blocker [12]
  • Neramexane (KRP-209; MRZ 2/579) – ionotropic glutamate NMDA receptor antagonist and nicotinic acetylcholine receptor negative allosteric modulator [13]
  • Selurampanel (BGG-492; BGG-492A) – ionotropic glutamate AMPA and kainate receptor antagonist [14][5]
  • Sodium phenylbutyrate slow-release (4-PB-D-alanin; LU-901; Lunaphen) – histone deacetylase (HDAC) inhibitor [15]
  • Vestipitant (GW-597599; GW-597599B) – neurokinin NK1 receptor antagonist [16]

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 [17][6]
  • Trimetazidine (Adexor; Flavedon; Idaptan; Preductal; S-5016; Trimetazine; Vastarel; Vastinan) – long-chain 3-ketoacyl-CoA thiolase inhibitor and other actions [18][7]

Off-label drugs

See also

References

  1. ↑ "Development of ebselen for the treatment of sensorineural hearing loss and tinnitus". Hear Res 413. January 2022. doi:10.1016/j.heares.2021.108209. PMID 33678494. 
  2. ↑ "Cochlear NMDA receptors as a therapeutic target of noise-induced tinnitus". Cell Physiol Biochem 35 (5): 1905–1923. 2015. doi:10.1159/000374000. PMID 25871611. 
  3. ↑ "Efficacy and safety of AM-101 in the treatment of acute inner ear tinnitus--a double-blind, randomized, placebo-controlled phase II study". Otol Neurotol 35 (4): 589–597. April 2014. doi:10.1097/MAO.0000000000000268. PMID 24603353. 
  4. ↑ "Ginkgo biloba extract EGb 761® versus pentoxifylline in chronic tinnitus: a randomized, double-blind clinical trial". Int J Clin Pharm 40 (5): 1335–1341. October 2018. doi:10.1007/s11096-018-0654-4. PMID 29855986. 
  5. ↑ Efficacy and safety of single- and repeated-selurampanel dosing for 2 weeks in patients with chronic subjective tinnitus: Results of a randomized, double-blind, placebo-controlled, cross-over, proof-of-concept phase IIa study. Progress in Brain Research. 260. 2021. 423–440. doi:10.1016/bs.pbr.2020.12.004. ISBN 978-0-12-821586-9. 
  6. ↑ "Pentoxifylline uses in inner ear diseases". Eur J Clin Pharmacol 81 (7): 955–999. July 2025. doi:10.1007/s00228-025-03844-4. PMID 40332573. 
  7. ↑ "Efficacy of Trimetazidine Dihydrochloride for Relieving Chronic Tinnitus: A Randomized Double-Blind Study". Clin Exp Otorhinolaryngol 9 (3): 192–197. September 2016. doi:10.21053/ceo.2015.00619. PMID 27230273. 
  8. ↑ 8.0 8.1 8.2 8.3 "Therapeutic Approaches to the Treatment of Tinnitus". Annu Rev Pharmacol Toxicol 59: 291–313. January 2019. doi:10.1146/annurev-pharmtox-010818-021556. PMID 30044727. 
  9. ↑ 9.0 9.1 9.2 9.3 "Efficacy of pharmacologic treatment in tinnitus patients without specific or treatable origin: A network meta-analysis of randomised controlled trials". eClinicalMedicine 39. September 2021. doi:10.1016/j.eclinm.2021.101080. PMID 34611615. 
  10. ↑ "Easing the Burden of Tinnitus: A Narrative Review for Exploring Effective Pharmacological Strategies". Cureus 16 (2). February 2024. doi:10.7759/cureus.54861. PMID 38533154. 




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