Claims for Patent: 11,911,380

Summary for Patent: 11,911,380

Title:	Compositions and use of varenicline for treating dry eye
Abstract:	Described herein are methods and pharmaceutical formulations for treating dry eye disease.
Inventor(s):	Douglas Michael Ackermann, JR., James LOUDIN, Kenneth J. Mandell
Assignee:	Oyster Point Pharma Inc
Application Number:	US18/125,551
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,911,380
Patent Claims:	1. A method of activating a trigeminal nerve in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a liquid pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms. 2. The method of claim 1, wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors. 3. The method of claim 1, wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms. 4. The method of claim 1, wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms. 5. The method of claim 1, wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms. 6. The method of claim 1, wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects. 7. The method of claim 1, wherein the amount of varenicline so administered does not result in clinically significant vomiting. 8. The method of claim 1, wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer. 9. The method of claim 1, wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4. 10. The method of claim 9, wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4. 11. A method of activating an anterior ethmoidal nerve in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a liquid pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms. 12. The method of claim 11, wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors. 13. The method of claim 11, wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms. 14. The method of claim 11, wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms. 15. The method of claim 11, wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms. 16. The method of claim 11, wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects. 17. The method of claim 11, wherein the amount of varenicline so administered does not result in clinically significant vomiting. 18. The method of claim 11, wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer. 19. The method of claim 11, wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4. 20. The method of claim 19, wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4. 21. A method of activating a nasolacrimal reflex in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is local administration of a spray of a pharmaceutical formulation comprising a solution of varenicline or a pharmaceutically acceptable varenicline salt and one or more pharmaceutically acceptable inactive ingredients, wherein the concentration of varenicline in the formulation is between about 0.1 mg/mL and about 10 mg/mL, into a nasal cavity of the individual, wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms. 22. The method of claim 21, wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors. 23. The method of claim 21, wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms. 24. The method of claim 21, wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms. 25. The method of claim 21, wherein the amount of varenicline so administered into the nasal cavity is between 5 micrograms and 500 micrograms. 26. The method of claim 21, wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects. 27. The method of claim 21, wherein the amount of varenicline so administered does not result in clinically significant vomiting. 28. The method of claim 21, wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer. 29. The method of claim 21, wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4. 30. The method of claim 29, wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4.