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Acoltremon

(Redirected from WS-12)

Acoltremon sold under the brand name Tryptyr, is a medication used for the treatment of dry eye syndrome.[1] Acoltremon is a transient receptor potential melastatin 8 (TRPM8) thermoreceptor agonist.[1] It is used as an eye drop.[1]

Acoltremon
molecular structure
Clinical data
Trade namesTryptyr
Other namesAVX-012, WS-12
AHFS/Drugs.comMonograph
MedlinePlusa625071
License data
Routes of
administration		Eye drop
ATC code
  • None
Legal status
Legal status
Identifiers
  • (1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-propan-2-ylcyclohexane-1-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H27NO2
Molar mass289.419 g·mol−1
3D model (JSmol)
  • C[C@@H]1CC[C@H]([C@@H](C1)C(=O)NC2=CC=C(C=C2)OC)C(C)C
  • InChI=1S/C18H27NO2/c1-12(2)16-10-5-13(3)11-17(16)18(20)19-14-6-8-15(21-4)9-7-14/h6-9,12-13,16-17H,5,10-11H2,1-4H3,(H,19,20)/t13-,16+,17-/m1/s1
  • Key:HNSGVPAAXJJOPQ-XOKHGSTOSA-N

The most common treatment-emergent adverse event experienced during the clinical studies was instillation site pain (burning or stinging) events.[2]

Acoltremon was approved for medical use in the United States in May 2025.[2]

Medical uses

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Acoltremon is indicated for the treatment of the signs and symptoms of dry eye disease.[1][2]

Pharmacology

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Acoltremon acts as a potent and selective activator (opener) of the TRPM8 calcium channel, which is responsible for the sensation of coldness produced by menthol.[3] It is slightly less potent as a TRPM8 activator compared to icilin, but is a much more selective TRPM8 ligand when compared to menthol.[4]

History

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The US Food and Drug Administration (FDA) approved acoltremon based on evidence from two clinical trials (COMET-2 and COMET-3) of 931 participants with dry eye disease.[2] The trials were conducted at 46 sites in the United States.[2] Two additional studies: COMET-1 and COMET-4 were included in the evaluation of safety benefit of acoltremon.[2] The number of participants representing efficacy findings may differ from the number of participants representing safety findings due to different pools of study participants analyzed for efficacy and safety.[2] Both COMET-2 and COMET-3 are phase III, multi-center, vehicle-controlled, double-masked, randomized studies whose primary endpoint was proportion of participants with ≥10 mm increase from baseline in unanesthetized Schirmer Score on day 14.[2] COMET-1 was a phase IIb multi-center, vehicle-controlled, double-masked, randomized study conducted at 15 sites in the United States which randomized 369 participants with a history of dry eye disease.[2] COMET-4 was a multi-center, vehicle-controlled, double-masked, randomized study conducted at approximately 10 sites in the United States which enrolled 275 participants with a history of dry eye disease.[2] Study COMET-2 and COMET-3 have a similar design.[2] Each study is a multi-center, randomized, double-masked, vehicle-controlled phase III study.[2] The primary objective of these studies was to evaluate the safety and efficacy of acoltremon compared to vehicle.[2] Participants 30 years and older with a history of artificial tear use for dry eye disease were qualified based on signs and symptoms of dry eye disease at screening, and were requalified at baseline (day 1) following a 14-day vehicle run-in.[2] COMET 2 enrolled 465 participants at 23 study sites, whereas COMET-3 enrolled 466 participants at 23 sites.[2]

Society and culture

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Acoltremon was approved for medical use in the United States in May 2025.[5]

Names

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Acoltremon is the international nonproprietary name.[6]

Acoltremon is sold under the brand name Tryptyr.[2]

References

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  1. ^ a b c d e "Tryptyr- acoltremon solution". DailyMed. 12 June 2025. Retrieved 6 July 2025.
  2. ^ a b c d e f g h i j k l m n o p "Drug Trials Snapshot: Tryptyr". U.S. Food and Drug Administration. 28 May 2025. Retrieved 24 August 2025.   This article incorporates text from this source, which is in the public ___domain.
  3. ^ Ma S, Gisselmann G, Vogt-Eisele AK, Doerner JF, Hatt H (October 2008). "Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels". Pakistan Journal of Pharmaceutical Sciences. 21 (4): 370–378. PMID 18930858.
  4. ^ Kühn FJ, Kühn C, Lückhoff A (February 2009). "Inhibition of TRPM8 by icilin distinct from desensitization induced by menthol and menthol derivatives". The Journal of Biological Chemistry. 284 (7): 4102–4111. doi:10.1074/jbc.M806651200. PMID 19095656.
  5. ^ "Alcon Announces FDA Approval of Tryptyr (acoltremon ophthalmic solution) 0.003% for the Treatment of the Signs and Symptoms of Dry Eye Disease" (Press release). Alcon. 28 May 2025. Archived from the original on 29 May 2025. Retrieved 29 May 2025 – via Business Wire.
  6. ^ World Health Organization (2023). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 89". WHO Drug Information. 37 (1). hdl:10665/366661.
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