Acoltremon

Acoltremon

AR-15512

CAS 68489-09-8

WeightAverage: 289.419
Monoisotopic: 289.204179113

Chemical FormulaC₁₈H₂₇NO₂

FDA 2025, 5/28/2025, To treat the signs and symptoms of dry eye disease

Tryptyr

1L7BVT4Z4Z

• OriginatorInstituto de Neurociencias de Alicante
• DeveloperAlcon; AVX Pharma
• ClassCyclohexanes; Ethers; Eye disorder therapies; Small molecules
• Mechanism of ActionTRPM8 protein stimulants

• RegisteredDry eyes
• 30 May 2025Alcon plans to launch Acoltremon for Dry eyes in USA in the third quarter of 2025
• 28 May 2025Registered for Dry eyes in USA (Ophthalmic) – First global approval
• 05 May 2025FDA assigns PDUFA action date of 30/05/2025 for Acoltremon for Dry eyes

Acoltremon sold under the brand name Tryptyr, is a medication used for the treatment of dry eye syndrome.^[1]

PATENT

US 217370

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2023114986&_fid=RU437402572

https://patentscope.wipo.int/search/en/detail.jsf?docId=US193167995&_cid=P11-MCE7BB-27500-1

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012032209&_fid=US193167995

Medical uses

Acoltremon was approved for medical use in the United States in May 2025, for the treatment of signs and symptoms associated with dry eye disease.^[2]

Pharmacology

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]

Society and culture

Legal status

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

References

1. ^ Jump up to:^a b https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/217370s000lbl.pdf
2. ^ “Novel Drug Approvals for 2025”. U.S. Food and Drug Administration (FDA). 29 May 2025. Archived from the original on 3 March 2025. Retrieved 29 May 2025.
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.

External links

• Clinical trial number NCT05285644 for “Study Evaluating the Safety and Efficacy of AR-15512 (COMET-2)” at ClinicalTrials.gov
• Clinical trial number NCT05360966 for “Study Evaluating the Safety and Efficacy of AR-15512 (COMET-3)” at ClinicalTrials.gov

molecular structure
3D representation
Clinical data
Trade names	Tryptyr
Other names	AVX-012, WS-12
License data	US DailyMed: Acoltremon
ATC code	None
Legal status
Legal status	US: ℞-only[1]
Identifiers
showIUPAC name
CAS Number	68489-09-8
PubChem CID	11266244
DrugBank	DB19202
ChemSpider	9441255
UNII	1L7BVT4Z4Z
KEGG	D13125
ChEMBL	ChEMBL2441929
CompTox Dashboard (EPA)	DTXSID10460636
Chemical and physical data
Formula	C18H27NO2
Molar mass	289.419 g·mol−1
3D model (JSmol)	Interactive image
showSMILES
showInChI

• [1]. Beck B, et al. Prospects for prostate cancer imaging and therapy using high-affinity TRPM8 activators. Cell Calcium. 2007 Mar;41(3):285-94.  [Content Brief][2]. Ma S, et al. Menthol derivative WS-12 selectively activates transient receptor potential melastatin-8 (TRPM8) ion channels. Pak J Pharm Sci. 2008 Oct;21(4):370-8.  [Content Brief]

///////Acoltremon, FDA 2025, APPROVALS 2025, WS-12, WS 12, Fema No. 4681, Tryptyr, 1L7BVT4Z4Z, AR-15512