Acoltremon

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

Acoltremon

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
Identifiers
IUPAC name (1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-propan-2-ylcyclohexane-1-carboxamide
CAS Number	68489-09-8
PubChem CID	11266244
DrugBank	DB19202
ChemSpider	9441255
UNII	1L7BVT4Z4Z
ChEMBL	ChEMBL2441929
CompTox Dashboard (EPA)	DTXSID10460636
Chemical and physical data
Formula	C18H27NO2
Molar mass	289.419 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@@H]1CC[C@H]([C@@H](C1)C(=O)NC2=CC=C(C=C2)OC)C(C)C
InChI 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

Medical uses

Acoltremon was approved for medical use in the United States in May 2025 or the treatment of signs and symptoms associated with dry eye disease.^[2][3] Alcon anticipates launching the product in the U.S. during the third quarter of 2025.^[4]

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 (of which acoltremon is a chemical analogue of). ^[5] It is slightly less potent as a TRPM8 activator compared to icilin, but is much more selective for TRPM8 over related calcium channels.^[6]

Animal studies

It produces analgesic and anti-inflammatory effects in animal models with similar efficacy to menthol and a reduced side effect profile.^{[7][8][9][10][11]}

Clinical trials

Although the precise mechanism in treating dry eye remains unclear, Phase 3 clinical trials showed that a greater proportion of patients using acoltremon experienced increased tear production compared to those using a placebo.^[12]