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 It is likely to become outdated with time.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) – 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. ^ Kil J, Harruff EE, Longenecker RJ (January 2022). "Development of ebselen for the treatment of sensorineural hearing loss and tinnitus". Hear Res. 413 108209. doi:10.1016/j.heares.2021.108209. PMID 33678494.
  2. ^ Bing D, Lee SC, Campanelli D, Xiong H, Matsumoto M, Panford-Walsh R, Wolpert S, Praetorius M, Zimmermann U, Chu H, Knipper M, Rüttiger L, Singer W (2015). "Cochlear NMDA receptors as a therapeutic target of noise-induced tinnitus". Cell Physiol Biochem. 35 (5): 1905–1923. doi:10.1159/000374000. PMID 25871611.
  3. ^ van de Heyning P, Muehlmeier G, Cox T, Lisowska G, Maier H, Morawski K, Meyer T (April 2014). "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. doi:10.1097/MAO.0000000000000268. PMC 3966923. PMID 24603353.
  4. ^ Procházková K, Šejna I, Skutil J, Hahn A (October 2018). "Ginkgo biloba extract EGb 761® versus pentoxifylline in chronic tinnitus: a randomized, double-blind clinical trial". Int J Clin Pharm. 40 (5): 1335–1341. doi:10.1007/s11096-018-0654-4. PMC 6208604. PMID 29855986.
  5. ^ Kucher K, Johns D, Wagner F, Abd-Elaziz K, Derne C, Sverdlov O, Pfister CU, Langguth B (2021). 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. Vol. 260. pp. 423–440. doi:10.1016/bs.pbr.2020.12.004. ISBN 978-0-12-821586-9. PMID 33637230.
  6. ^ Ramzi A, Maya S, Balousha N, Amin M, Rouby RA, Aljarrah G, Elnady DG, Samir A, Ghanm TI, Bhaya ZN, Altarras A, Abdelsalam F, Yasser M, Samir M, Shiha MR (July 2025). "Pentoxifylline uses in inner ear diseases". Eur J Clin Pharmacol. 81 (7): 955–999. doi:10.1007/s00228-025-03844-4. PMID 40332573.
  7. ^ Kumral TL, Yıldırım G, Berkiten G, Saltürk Z, Ataç E, Atar Y, Uyar Y (September 2016). "Efficacy of Trimetazidine Dihydrochloride for Relieving Chronic Tinnitus: A Randomized Double-Blind Study". Clin Exp Otorhinolaryngol. 9 (3): 192–197. doi:10.21053/ceo.2015.00619. PMC 4996095. PMID 27230273.
  8. ^ a b c d Langguth B, Elgoyhen AB, Cederroth CR (January 2019). "Therapeutic Approaches to the Treatment of Tinnitus". Annu Rev Pharmacol Toxicol. 59: 291–313. doi:10.1146/annurev-pharmtox-010818-021556. PMID 30044727.
  9. ^ a b c d Chen JJ, Chen YW, Zeng BY, Hung CM, Zeng BS, Stubbs B, Carvalho AF, Thompson T, Roerecke M, Su KP, Tu YK, Wu YC, Smith L, Chen TY, Lin PY, Liang CS, Hsu CW, Hsu SP, Kuo HC, Wu MK, Tseng PT (September 2021). "Efficacy of pharmacologic treatment in tinnitus patients without specific or treatable origin: A network meta-analysis of randomised controlled trials". eClinicalMedicine. 39 101080. doi:10.1016/j.eclinm.2021.101080. PMC 8478678. PMID 34611615.
  10. ^ Kim SH, Kim I, Kim H (February 2024). "Easing the Burden of Tinnitus: A Narrative Review for Exploring Effective Pharmacological Strategies". Cureus. 16 (2) e54861. doi:10.7759/cureus.54861. PMC 10964395. PMID 38533154.
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