Acoltremon

{{Infobox drug

| image = WS-12_structure.png

| width =

| alt =

| caption = molecular structure

| image2 = Acoltremon 3D.png

| alt2 =

| caption2 = 3D representation

| pronounce =

| tradename = Tryptyr

| Drugs.com =

| MedlinePlus =

| DailyMedID = Acoltremon

| pregnancy_AU =

| pregnancy_AU_comment =

| pregnancy_category =

| routes_of_administration =

| class =

| ATC_prefix = None

| ATC_suffix =

| ATC_supplemental =

| legal_AU =

| legal_AU_comment =

| legal_BR =

| legal_BR_comment =

| legal_CA =

| legal_CA_comment =

| legal_DE =

| legal_DE_comment =

| legal_NZ =

| legal_NZ_comment =

| legal_UK =

| legal_UK_comment =

| legal_US = Rx-only

| legal_US_comment =

| legal_EU =

| legal_EU_comment =

| legal_UN =

| legal_UN_comment =

| legal_status =

| bioavailability =

| protein_bound =

| metabolism =

| metabolites =

| onset =

| elimination_half-life =

| duration_of_action =

| excretion =

| CAS_number = 68489-09-8

| PubChem = 11266244

| IUPHAR_ligand =

| DrugBank = DB19202

| ChemSpiderID = 9441255

| UNII = 1L7BVT4Z4Z

| KEGG =

| ChEBI =

| ChEMBL = 2441929

| NIAID_ChemDB =

| PDB_ligand =

| synonyms = AVX-012, WS-12

| IUPAC_name = (1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-propan-2-ylcyclohexane-1-carboxamide

| C = 18

| H = 27

| N = 1

| O = 2

| SMILES = C[C@@H]1CC[C@H]([C@@H](C1)C(=O)NC2=CC=C(C=C2)OC)C(C)C

| StdInChI = 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

| StdInChIKey = HNSGVPAAXJJOPQ-XOKHGSTOSA-N

| density =

| density_notes =

| melting_point =

| melting_high =

| melting_notes =

| boiling_point =

| boiling_notes =

| solubility =

| sol_units =

| specific_rotation =

}}

Acoltremon sold under the brand name Tryptyr, is a medication used for the treatment of dry eye syndrome.{{cite web | title = Acoltremon - Alcon | url = https://adisinsight.springer.com/drugs/800048064 | work = AdisInsight | publisher = Springer Nature Switzerland AG }}

Acoltremon was approved for medical use in the United States in May 2025.{{cite web | title=Novel Drug Approvals for 2025 | website=U.S. Food and Drug Administration (FDA) | date=29 May 2025 | url=https://www.fda.gov/drugs/novel-drug-approvals-fda/novel-drug-approvals-2025 | access-date=29 May 2025}}{{cite press release | title=Alcon Announces FDA Approval of Tryptyr (acoltremon ophthalmic solution) 0.003% for the Treatment of the Signs and Symptoms of Dry Eye Disease | publisher=Alcon | via=Business Wire | date=28 May 2025 | url=https://www.businesswire.com/news/home/20250526316115/en/Alcon-Announces-FDA-Approval-of-TRYPTYR-acoltremon-ophthalmic-solution-0.003-for-the-Treatment-of-the-Signs-and-Symptoms-of-Dry-Eye-Disease | access-date=29 May 2025}}

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. It is slightly less potent as a TRPM8 activator compared to icilin, but is much more selective for TRPM8 over related calcium channels. It produces analgesic and anti-inflammatory effects in animal models with similar efficacy to menthol and a reduced side effect profile.{{cite journal | vauthors = Bödding M, Wissenbach U, Flockerzi V | title = Characterisation of TRPM8 as a pharmacophore receptor | journal = Cell Calcium | volume = 42 | issue = 6 | pages = 618–28 | date = December 2007 | pmid = 17517434 | doi = 10.1016/j.ceca.2007.03.005 }}{{cite journal | vauthors = Sherkheli MA, Vogt-Eisele AK, Bura D, Beltrán Márques LR, Gisselmann G, Hatt H | title = Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship | journal = Journal of Pharmacy & Pharmaceutical Sciences |date=2010| volume = 13 | issue = 2 | pages = 242–53 | pmid = 20816009 | doi = 10.18433/j3n88n | doi-access = free }}{{cite journal | vauthors = Liu B, Fan L, Balakrishna S, Sui A, Morris JB, Jordt SE | title = TRPM8 is the principal mediator of menthol-induced analgesia of acute and inflammatory pain | journal = Pain | volume = 154 | issue = 10 | pages = 2169–77 | date = October 2013 | pmid = 23820004 | doi = 10.1016/j.pain.2013.06.043 | pmc = 3778045 }}{{cite journal | vauthors = Peixoto-Neves D, Soni H, Adebiyi A | title = Oxidant-induced increase in norepinephrine secretion from PC12 cells is dependent on TRPM8 channel-mediated intracellular calcium elevation | journal = Biochemical and Biophysical Research Communications | volume = 506 | issue = 3 | pages = 709–715 | date = November 2018 | pmid = 30376995 | doi = 10.1016/j.bbrc.2018.10.120 | s2cid = 53107273 }}{{cite journal | vauthors = Yin Y, Le SC, Hsu AL, Borgnia MJ, Yang H, Lee SY | title = Structural basis of cooling agent and lipid sensing by the cold-activated TRPM8 channel | journal = Science | volume = 363 | issue = 6430 | date = March 2019 | pmid = 30733385 | doi = 10.1126/science.aav9334| pmc=6478609 | doi-access = free }}

References

Category:Ion channel openers