Claims for Patent: 10,028,920

Summary for Patent: 10,028,920

Title:	Methods for treating occular irritation involving tearing by administering modulators of TRPM8
Abstract:	The invention relates to therapeutic compositions for the treatment of dry eye, more specifically to compositions comprising a TRPM8 receptor agonist ligand. Furthermore, the invention relates to therapeutic compositions for the treatment of epiphora, more specifically to compositions comprising a TRPM8 receptor antagonist.
Inventor(s):	Carlos Belmonte Martínez, Juana Gallar Martínez, Antonio Ferrer Montiel, Asia Fernández Carvajal, Félix Viana De La Iglesia
Assignee:	Consejo Superior de Investigaciones Cientificas CSIC , Universidad Miguel Hernandez de Elche UMH
Application Number:	US15/350,938
Patent Claims:	1. A method for treating and/or relieving ocular irritation involving tearing in a subject in need thereof comprising administering an effective amount of a composition comprising a molecule binding specifically to the TRPM8 (Transient receptor potential cation channel subfamily Member 8) receptor to the subject, wherein the binding of the molecule to the TRPM8 receptor modulates the activity of the TRPM8 channel. 2. The method according to claim 1, wherein the irritation is caused by an external stimulus. 3. The method according to claim 2, wherein the external stimulus is a foreign body. 4. The method according to claim 1, wherein the molecule binding specifically to the TRPM8 receptor is a TRPM8 receptor agonist or a TRPM8 receptor antagonist. 5. The method according to claim 4, wherein the molecule binding specifically to the TRPM8 receptor comprises a 5-methyl-2-isopropyl cyclohexane core structure. 6. The method according to claim 5, wherein the molecule binding specifically to the TRPM8 receptor comprising a 5-methyl-2-isopropyl cyclohexane core structure is selected from the group consisting of WS-5, CPS-369, CPS-368, CPS-125, menthyl lactate, menthone glycerin acetal, Coolant Agent 10, (−)-Isopulegol, Cubebol, Hasegawa's cooling compound, WS-11, WS-12, WS-30, WS-3, WS-14, menthol, IFF's New GRAS cooling material, MAD1d, MAD2e, and combinations thereof. 7. The method according to claim 5, wherein the molecule binding specifically to the TRPM8 receptor comprising a 5-methyl-2-isopropyl cyclohexane core structure is WS12. 8. The method according to claim 1, wherein the composition comprises at least two molecules binding specifically to the TRPM8 receptor. 9. The method according to claim 1, wherein the composition comprises at least two TRPM8 receptor agonists or two TRPM8 receptor antagonists. 10. The method according to claim 1, wherein the composition is formulated as a liquid solution. 11. The method according to claim 10, wherein the liquid solution is formulated for ophthalmic administration. 12. The method according to claim 1, wherein the composition comprises a molecule binding specifically to the TRPM8 receptor and comprises at least one additional drug useful for treating and/or relieving ocular irritation. 13. The method according to claim 12, wherein at least one additional drug is selected from the group consisting of a corticoid, a vitamin, a muscarinic acetylcholine receptor agonist, an immunosuppressant, an antibiotic, and a combination thereof. 14. The method according to claim 13, wherein the vitamin is vitamin A. 15. The method according to claim 13, wherein the muscarinic acetylcholine receptor agonist is pylocarpine. 16. The method according to claim 13, wherein the immunosuppressant is cyclosporine. 17. The method according to claim 1, wherein the composition further comprises a lubricant. 18. The method according to claim 17, wherein the lubricant is selected from the group consisting of glycerol, hydroxypropyl methylcellulose, hydroxymethyl cellulose, carboxymethyl cellulose, polyethylene glycol, polyvinyl alcohol, hyaluronic acid, castor oil, mineral oil, hypromellose, carbomer, and combinations thereof. 19. The method according to claim 1, wherein the composition can be administered a variable number of times a day. 20. The method according to claim 1, wherein the binding of the molecule to the TRPM8 receptor increases or decreases tear secretion.