Claims for Patent: 10,456,396

Summary for Patent: 10,456,396

Title:	Dry eye treatments
Abstract:	Described herein are methods and pharmaceutical formulations for treating dry eye disease.
Inventor(s):	Ackermann, Jr.; Douglas Michael (Reno, NV), Loudin; James (Houston, TX), Mandell; Kenneth J. (Lexington, MA)
Assignee:	Oyster Point Pharma, Inc. (Princeton, NJ)
Application Number:	15/422,382
Patent Claims:	1. A method of treating dry eye in an individual in need thereof, comprising administering between 5 micrograms and 600 micrograms of varenicline in alternating nostrils of the individual. 2. The method of claim 1, comprising administering between 5 micrograms and 100 micrograms of varenicline in alternating nostrils of the individual. 3. The method of claim 1, wherein varenicline selectively binds to a peripheral nicotinic acetylcholine receptor in an amount that does not result in undesired psychoactive side effects. 4. The method of claim 1, further comprising administering one or more substances that prevent the entry or reduce the entry of a nicotinic acetylcholine receptor into the desensitized state, or facilitate the recovery of the nicotinic acetylcholine receptor from the desensitized state. 5. The method of claim 1, wherein the one or more substances are selected from protein kinase C (PKC) or factors that upregulate or up-modulate PKC, cAMP-dependent protein kinase (PKA) or factors that upregulate or up-modulate PKA, and calcineurin inhibitors. 6. The method of claim 5, wherein the calcineurin inhibitor is selected from cyclosporine, pimecrolimus, and tacrolimus. 7. The method of claim 1, wherein varenicline is administered at least once daily. 8. The method of claim 1, wherein varenicline is administered at least twice daily. 9. The method of claim 1, wherein varenicline is administered at least once weekly. 10. The method of claim 1, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 11. The method of claim 1, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 12. The method of claim 1, wherein a trigeminal nerve is activated. 13. The method of claim 12, wherein an anterior ethmoidal nerve is activated. 14. The method of claim 1, wherein a nasolacrimal reflex is activated. 15. The method of claim 1, wherein varenicline is administered with a medical device. 16. The method of claim 15, wherein varenicline is administered with a punctal plug. 17. The method of claim 1, comprising administering about 0.5 mg/mL of varenicline. 18. The method of claim 2, wherein varenicline is administered at least once daily. 19. The method of claim 2, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 20. The method of claim 2, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 21. The method of claim 2, wherein varenicline is administered with a medical device. 22. A method of treating dry eye in an individual in need thereof, comprising administering between 100 micrograms and 750 micrograms of varenicline in alternating nostrils of the individual. 23. The method of claim 22, comprising administering between 150 micrograms and 600 micrograms of varenicline in alternating nostrils of the individual. 24. The method of claim 22, wherein varenicline selectively binds to a peripheral nicotinic acetylcholine receptor in an amount that does not result in undesired psychoactive side effects. 25. The method of claim 22, further comprising administering one or more substances that prevent the entry or reduce the entry of a nicotinic acetylcholine receptor into the desensitized state, or facilitate the recovery of the nicotinic acetylcholine receptor from the desensitized state. 26. The method of claim 25, wherein the one or more substances are selected from protein kinase C (PKC) or factors that upregulate or up-modulate PKC, cAMP-dependent protein kinase (PKA) or factors that upregulate or up-modulate PKA, and calcineurin inhibitors. 27. The method of claim 22, wherein the calcineurin inhibitor is selected from cyclosporine, pimecrolimus, and tacrolimus. 28. The method of claim 22, wherein varenicline is administered at least once daily. 29. The method of claim 22, wherein varenicline is administered at least twice daily. 30. The method of claim 22, wherein varenicline is administered at least once weekly. 31. The method of claim 22, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 32. The method of claim 22, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 33. The method of claim 22, wherein a trigeminal nerve is activated. 34. The method of claim 22, wherein an anterior ethmoidal nerve is activated. 35. The method of claim 22, wherein a nasolacrimal reflex is activated. 36. The method of claim 22, wherein varenicline is administered with a medical device. 37. The method of claim 36, wherein varenicline is administered with a punctal plug. 38. A method of treating ocular discomfort in an individual in need thereof, comprising administering between 5 micrograms and 600 micrograms of varenicline in alternating of the individual. 39. The method of claim 38, comprising administering between 5 micrograms and 100 micrograms of varenicline in alternating of the individual. 40. The method of claim 38, wherein varenicline is administered prior to or after Lasik surgery. 41. The method of claim 38, wherein varenicline is administered at least once daily. 42. The method of claim 38, wherein varenicline is administered at least twice daily. 43. The method of claim 38, wherein varenicline is administered at least once weekly. 44. The method of claim 38, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 45. The method of claim 38, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 46. The method of claim 38, wherein varenicline is administered with a medical device. 47. The method of claim 38, comprising about 0.5 mg/mL of varenicline. 48. The method of claim 39, wherein varenicline is administered at least once daily. 49. The method of claim 39, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 50. The method of claim 39, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 51. The method of claim 39, wherein varenicline is administered with a medical device. 52. A method of treating ocular discomfort in an individual in need thereof, comprising administering between 100 micrograms and 750 micrograms of varenicline in alternating of the individual. 53. The method of claim 52, comprising administering between 150 micrograms and 600 micrograms of varenicline in alternating of the individual. 54. The method of claim 52, wherein varenicline is administered prior to or after Lasik surgery. 55. The method of claim 52, wherein varenicline is administered at least once daily. 56. The method of claim 52, wherein varenicline is administered at least twice daily. 57. The method of claim 52, wherein varenicline is administered at least once weekly. 58. The method of claim 52, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 59. The method of claim 52, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 60. The method of claim 52, wherein varenicline is administered with a medical device. 61. A method of increasing tear production in an individual in need thereof, comprising administering between 5 micrograms and 600 micrograms of varenicline in alternating nostrils of the individual. 62. The method of claim 61, comprising administering between 5 micrograms and 100 micrograms of varenicline in alternating of the individual. 63. The method of claim 61, wherein varenicline is administered prior to or after Lasik surgery. 64. The method of claim 61, wherein prior to administering varenicline, the individual has a Schirmer tear test score of .ltoreq.10 mm/5 minutes in at least one eye. 65. The method of claim 64, wherein the Schirmer tear test is performed with topical anesthetic. 66. The method of claim 64, wherein the Schirmer tear test is performed without nasal stimulation. 67. The method of claim 64, wherein the Schirmer tear test is performed with nasal stimulation. 68. The method of claim 61, wherein varenicline is administered at least once daily. 69. The method of claim 61, wherein varenicline is administered at least twice daily. 70. The method of claim 61, wherein varenicline is administered at least once weekly. 71. The method of claim 61, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 72. The method of claim 61, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 73. The method of claim 61, wherein varenicline is administered with a medical device. 74. The method of claim 62, wherein varenicline is administered at least once daily. 75. The method of claim 62, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 76. The method of claim 62, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 77. The method of claim 62, wherein varenicline is administered with a medical device. 78. The method of claim 61, comprising administering about 0.5 mg/mL of varenicline. 79. A method of increasing tear production in an individual in need thereof, comprising administering between 100 micrograms and 750 micrograms of varenicline in alternating nostrils of the individual. 80. The method of claim 79, comprising administering between 150 micrograms and 600 micrograms of varenicline in alternating of the individual. 81. The method of claim 79, wherein varenicline is administered prior to or after Lasik surgery. 82. The method of claim 79, wherein prior to administering varenicline, the individual has a Schirmer tear test score of .ltoreq.10 mm/5 minutes in at least one eye. 83. The method of claim 82, wherein the Schirmer tear test is performed with topical anesthetic. 84. The method of claim 82, wherein the Schirmer tear test is performed without nasal stimulation. 85. The method of claim 82, wherein the Schirmer tear test is performed with nasal stimulation. 86. The method of claim 79, wherein varenicline is administered at least once daily. 87. The method of claim 79, wherein varenicline is administered at least twice daily. 88. The method of claim 79, wherein varenicline is administered at least once weekly. 89. The method of claim 79, wherein varenicline is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 90. The method of claim 79, wherein varenicline is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 91. The method of claim 79, wherein varenicline is administered with a medical device. 92. A pharmaceutical formulation formulated for administration in alternating nostrils of an individual in need thereof, comprising between 5 micrograms and 600 micrograms of varenicline, per dose. 93. The pharmaceutical formulation of claim 92 comprising between 5 micrograms and 100 micrograms of varenicline, per dose. 94. The pharmaceutical formulation of claim 92, wherein the pharmaceutical formulation is formulated as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 95. The pharmaceutical formulation of claim 92, wherein the pharmaceutical formulation is formulated for administration by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 96. The pharmaceutical formulation of claim 92, comprising about 0.5 mg/mL of varenicline. 97. A pharmaceutical formulation formulated for administration in alternating nostrils of an individual in need thereof, comprising between 100 micrograms and 750 micrograms of varenicline, per dose. 98. The pharmaceutical formulation of claim 97 comprising between 150 micrograms and 600 micrograms of varenicline, per dose. 99. The pharmaceutical formulation of claim 97, wherein the pharmaceutical formulation is formulated as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 100. The pharmaceutical formulation of claim 97, wherein the pharmaceutical formulation is formulated for administration by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid.