Claims for Patent: 11,903,943

Summary for Patent: 11,903,943

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:	US18/125,562
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,903,943
Patent Claims:	1. A method of improving ocular discomfort in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is by locally administering a pharmaceutical formulation comprising 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, and 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 pharmaceutical formulation is a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 7. The method of claim 6, wherein the pharmaceutical formulation comprises a solution of the varenicline or varenicline salt. 8. The method of claim 7, wherein the pharmaceutical formulation is a liquid administered as a nasal spray. 9. The method of claim 1, wherein the ocular discomfort is associated with dry eye disease or symptoms of dry eye disease. 10. The method of claim 1, wherein the ocular discomfort is associated with symptoms of dry eye disease and wherein the improvement is measurable by recording dry eye disease symptom severity on a visual analog scale. 11. The method of claim 1, wherein the ocular discomfort is associated with dryness or sticky feeling with dry eye disease. 12. The method of claim 1, wherein the amount of varenicline so administered does not result in clinically significant undesired psychoactive side effects. 13. The method of claim 1, wherein the amount of varenicline so administered does not result in clinically significant vomiting. 14. The method of claim 1, wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer. 15. The method of claim 1, wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4. 16. The method of claim 15, wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4. 17. A method of increasing tear production in an individual in need thereof comprising administering a therapeutically effective amount of varenicline to the individual, wherein said administration is by locally administering a pharmaceutical formulation comprising 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, and wherein the therapeutically effective amount of varenicline administered into the nasal cavity is between 5 micrograms and 1000 micrograms. 18. The method of claim 17, wherein the amount of varenicline so administered selectively binds to peripheral nicotinic acetylcholine receptors. 19. The method of claim 17, wherein the amount of varenicline so administered is between 5 micrograms and 100 micrograms. 20. The method of claim 17, wherein the amount of varenicline so administered is between 25 micrograms and 500 micrograms. 21. The method of claim 17, wherein the amount of varenicline so administered is between 5 micrograms and 500 micrograms. 22. The method of claim 17, wherein the pharmaceutical formulation is a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 23. The method of claim 22, wherein the pharmaceutical formulation comprises a solution of the varenicline or varenicline salt. 24. The method of claim 23, wherein the pharmaceutical formulation is a liquid administered as a nasal spray. 25. The method of claim 17, wherein the tear production increases in an amount measurable by a Jones Schirmer test. 26. The method of claim 17, wherein the pharmaceutical formulation comprises a phosphate buffer or a phosphate citrate buffer. 27. The method of claim 17, wherein the pharmaceutical formulation comprises a buffer with a pH of from around 5.0 to around 7.4. 28. The method of claim 27, wherein the pharmaceutical formulation comprises a buffer with a pH of around 5.0, around 6.0, around 7.0 or around 7.4. 29. The method of claim 1, wherein the ocular discomfort is associated with symptoms of dry eye disease, and wherein the method comprises increasing tear production in the individual. 30. The method of claim 29, wherein the tear production increases in an amount measurable by a Jones Schirmer test.