IP Library Granted Patent US 12,161,629
Granted Patent B2
US 12,161,629 · App. 17/283,038 · Granted Dec 10, 2024

Methods and compositions for treatment of glaucoma and related conditions

Inventors: William H. Pitlick (Seattle, WA); Alan R. Meyer (North Riverside, IL); Mina Sooch (Bloomfield, MI); Konstantinos Charizanis (Ypsilanti, MI)
Assignee: Opus Genetics, Inc.
A61K31/417A61K9/0048A61K31/138A61K31/222A61K31/27A61K31/382A61K31/4045A61K31/4164A61K31/4168A61K31/4178A61K31/439A61K31/444A61K31/4704A61K31/472A61K31/475A61K31/496A61K31/498A61K31/517A61K31/5377A61K31/55A61K31/551A61K31/5575A61K31/558A61K31/683A61K31/7076A61K45/06A61P27/06
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Quick Facts
Patent No.
US 12,161,629
App. No.
17/283,038
Granted
Dec 10, 2024
Kind
B2
Abstract

Methods, compositions and kits comprising alpha-adrenergic antagonists, such as phentolamine, for the treatment of glaucoma, ocular hypertension, and/or other ocular disorders, such as non-arteritic anterior ischemic optic neuropathy or keratoconus, are provided. Said methods, compositions and kits may further comprise additional therapeutic agents, including prostaglandin analogues such as latanoprost, beta-adrenergic antagonists, alpha-adrenergic agonists, carbonic anhydrase inhibitors, cholinergic agonists, NMDA receptor antagonist, adenosine receptor antagonists, 5-HT2a receptor agonists, or Rho kinase inhibitors.

Claims (20)

1. A method of treating a condition selected from the group consisting of glaucoma and ocular hypertension in a human patient while minimizing eye redness during the patient's waking hours, comprising topically administering in the form of an eye drop to an eye of the patient in need thereof at or near the bedtime of the patient a once daily dosage of phentolamine mesylate in the amount of from about 0.3 mg to about 0.7 mg to thereby treat the condition.

2. The method of claim 1 , further comprising administering to the eye of the patient a second therapeutic agent selected from the group consisting of a prostaglandin analog, a beta blocker, an alpha adrenergic agonist, a carbonic anhydrase inhibitor, a cholinergic agonist, NMDA receptor antagonist, adenosine receptor agonist, 5-HT 2A receptor agonist, and a Rho kinase inhibitor.

3. The method of claim 1 , further comprising administering to the eye of the patient a second therapeutic agent selected from the group consisting of latanoprost, bimatoprost, travoprost, tafluprost, latanoprostene bunod, timolol, brimonidine, dorzolamide, brinzolamide, acetazolamide, methazolamide, pilocarpine, netarsudil, ripasudil, AMA0076, trabodenoson, BOL-303259-X, ONO-9054, carbachol, aceclidine, and oxotremorine, or a pharmaceutically acceptable salt of any one of the foregoing.

4. The method of claim 3 , wherein the second therapeutic agent is latanoprost.

5. The method of claim 3 , wherein the second therapeutic agent is latanoprost administered at a daily dose of about 1.5 micrograms.

6. The method of claim 1 , wherein the dosage contains about 0.5 mg of phentolamine mesylate.

7. The method of claim 1 , wherein the patient experiences at least a 10% reduction in intraocular pressure in the eye due to the administering.

8. The method of claim 7 , wherein the reduction lasts for a duration of at least 12 hours.

9. The method of claim 7 , wherein the patient to begin treatment is characterized as having an intraocular pressure less than 26 mmHg.

10. The method of claim 1 , wherein the patient experiences at least a 2 mmHg reduction in intraocular pressure in the eye due to the administering.

11. The method of claim 1 , wherein the patient experiences at least a 4 mmHg reduction in intraocular pressure in the eye due to the administering.

12. The method of claim 1 , wherein the condition is glaucoma.

13. The method of claim 12 , wherein the glaucoma is closed-angle glaucoma.

14. The method of claim 12 , wherein the glaucoma is normal tension glaucoma.

15. The method of claim 1 , wherein the condition is ocular hypertension.

16. The method of claim 1 , wherein the patient to begin treatment is characterized as having an intraocular pressure less than 26 mmHg.

17. A method of treating a condition selected from the group consisting of glaucoma and ocular hypertension in a human patient according to a monotherapy treatment regimen, comprising topically administering in the form of an eye drop to an eye of the patient in need thereof a dosage of a single therapeutic agent in an amount of from about 0.3 mg to about 0.7 mg, wherein the single therapeutic agent is phentolamine mesylate.

18. A method of treating a condition selected from the group consisting of glaucoma and ocular hypertension in a human patient, comprising topically administering to an eye of the patient in need thereof (i) phentolamine mesylate in the amount of from about 0.3 mg to about 0.7 mg and (ii) a therapeutically effective dosage of a second therapeutic agent selected from the group consisting of a prostaglandin analog, a beta blocker, an alpha adrenergic agonist, a carbonic anhydrase inhibitor, a cholinergic agonist, NMDA receptor antagonist, adenosine receptor agonist, 5-HT 2A receptor agonist, and a Rho kinase inhibitor, to thereby treat the condition.

19. The method of claim 18 , wherein the second therapeutic agent is latanoprost.

20. The method of claim 18 , wherein the second therapeutic agent is latanoprost administered at a daily dose of about 1.5 micrograms.

Assignments (3)
SECURITY INTEREST Recorded Apr 21, 2026
From: OPUS GENETICS, INC.
To: OPCM SA LLC, AS PURCHASER AGENT FOR THE SECURED PARTIES
Reel/Frame 075478/0138 →
CHANGE OF NAME Recorded Nov 1, 2024
From: OCUPHIRE PHARMA, INC.
To: OPUS GENETICS, INC.
Reel/Frame 069291/0350 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 29, 2021
From: PITLICK, WILLIAM H.; MEYER, ALAN R.; SOOCH, MINA; CHARIZANIS, KONSTANTINOS
To: OCUPHIRE PHARMA, INC.
Reel/Frame 057644/0277 →
Continuity (3)
Provisional Application 62752088 · Oct 29, 2018
Provisional Application 62745806 · Oct 15, 2018
Related Publication 20210346350A1 · Nov 11, 2021