IP Library Granted Patent US 9,532,944
Granted Patent B2
US 9,532,944 · App. 14/887,253 · Granted Jan 3, 2017

Methods of improving ocular discomfort

Inventors: Douglas Michael Ackermann, Jr. (San Francisco, CA); James Loudin (Houston, TX); Kenneth J. Mandell (Arlington, MA)
Assignee: OYSTER POINT PHARMA, INC.
A61K9/0043A61K9/007A61K31/439A61K31/4427A61K31/4439A61K31/4985A61K31/4995A61K45/06
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Quick Facts
Patent No.
US 9,532,944
App. No.
14/887,253
Granted
Jan 3, 2017
Kind
B2
Abstract

Described herein are methods and pharmaceutical formulations for improving ocular discomfort.

Claims (15)

1. A method of improving ocular discomfort, comprising the local administration of a therapeutically effective amount of a nicotinic acetylcholine receptor agonist into the nasal cavity of an individual in need thereof, wherein the agonist selectively binds to the peripheral nicotinic acetylcholine receptor, is administered in a non-systemically bioavailable dose between 5 micrograms and 50 micrograms per dose, and does not cross the blood-brain barrier in a pharmacologically relevant concentration; and wherein the nicotinic acetylcholine receptor agonist is varenicline.

2. The method of claim 1 , wherein the agonist selectively binds to at least one of the peripheral nicotinic acetylcholine receptor subtypes selected from alpha3beta4, alpha4beta2, and alpha7.

3. The method of claim 1 , wherein the agonist selectively binds to the peripheral nicotinic acetylcholine receptor in an amount that does not result in undesired psychoactive side effects.

4. The method of claim 1 , wherein the agonist selectively binds to the peripheral nicotinic acetylcholine receptor in an amount that does not result in undesired systemic side effects.

5. The method of claim 1 , further comprising the local administration of one or more substances that prevent the entry or reduce the entry of the nicotinic acetylcholine receptor into the desensitized state, or facilitate the recovery of the nicotinic acetylcholine receptor from the desensitized state.

6. The method of claim 5 , 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.

7. The method of claim 6 , wherein the calcineurin inhibitor is selected from cyclosporine, pimecrolimus, and tacrolimus.

8. The method of claim 1 , wherein the nicotinic acetylcholine receptor agonist is administered at least once daily.

9. The method of claim 1 , wherein the nicotinic acetylcholine receptor agonist is administered at least twice daily.

10. The method of claim 1 , wherein the nicotinic acetylcholine receptor agonist is administered at least once weekly.

11. The method of claim 1 , wherein the nicotinic acetylcholine receptor agonist is administered into the nasal cavity as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm.

12. The method of claim 1 , wherein the nicotinic acetylcholine receptor agonist is administered into the nasal cavity by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid.

13. The method of claim 1 , wherein the trigeminal nerve is activated.

14. The method of claim 13 , wherein the anterior ethmoidal nerve is activated.

15. The method of claim 1 , wherein the nasolacrimal reflex is activated.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Feb 3, 2023
From: ORBIMED ROYALTY & CREDIT OPPORTUNITIES III, LP
To: OYSTER POINT PHARMA INC.
Reel/Frame 062582/0873 →
PATENT SECURITY AGREEMENT Recorded Aug 5, 2021
From: OYSTER POINT PHARMA, INC.
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES III, LP
Reel/Frame 057104/0189 →
CORRECTIVE ASSIGNMENT TO CORRECT THE MISSPELLING OF FIRST ASSIGNOR'S LAST NAME FROM ACKERMAN TO ACKERMANN AS PREVIOUSLY RECORDED ON REEL 042141 FRAME 0415. ASSIGNOR(S) HEREBY CONFIRMS THE CORRECTIVE ASSIGNMENT. Recorded May 5, 2020
From: ACKERMANN, DOUGLAS MICHAEL, JR.; LOUDIN, JAMES; MANDELL, KENNETH J.
To: OYSTER POINT PHARMA, INC.
Reel/Frame 052594/0910 →
CORRECTIVE ASSIGNMENT TO CORRECT THE MISSPELLING OF FIRST ASSIGNOR'S LAST NAME AND OUTDATED ASSIGNEE ADDRESS PREVIOUSLY RECORDED ON REEL 037059 FRAME 0288. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Apr 3, 2017
From: ACKERMANN, DOUGLAS MICHAEL, JR.; LOUDIN, JAMES; MANDELL, KENNETH J.
To: OYSTER POINT PHARMA, INC.
Reel/Frame 042141/0415 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2015
From: ACKERMANN, DOUGLAS MICHAEL, JR; LOUDIN, JAMES; MANDELL, KENNETH J.
To: OYSTER POINT PHARMA, INC.
Reel/Frame 037059/0288 →
Continuity (3)
Provisional Application 62066280 · Oct 20, 2014
Provisional Application 62100844 · Jan 7, 2015
Related Publication 20160106665A1 · Apr 21, 2016