List of 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 It is likely to become outdated with time.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) – GABA_A receptor positive allosteric modulator and neurosteroid
• Ebselen (DR-3305; ebselene; ebseleno; ebselenum; harmokisane; PZ-51; SPI-1005; SPI-3005) – various actions [1]

Not under development

Suspended

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

No development reported

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

Discontinued

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

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

Off-label drugs

• Antidepressants (e.g., sertraline, nortriptyline, amitriptyline) ^{[8] [9]}
• Benzodiazepines (GABA_A receptor positive allosteric modulators) (e.g., alprazolam, clonazepam) ^[8]
• Corticosteroids (e.g., dexamethasone) ^{[9] [10]}
• Gabapentinoids (α₂δ subunit-containing voltage-gated calcium channel ligands) (e.g., gabapentin) ^{[8] [9]}
• Others (e.g., acamprosate, melatonin) ^{[8] [9]}

See also

• Lists of investigational drugs

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. 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. 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.

External links

• AdisInsight - Springer