Ophthalmic composition for treatment of dry eye disease

Patent metadata

Field	Value
Publication number	US-12496326-B2
Application number	US-202217933471-A
Country	US
Kind code	B2
Filing date	Sep 19, 2022
Priority date	Dec 23, 2016
Publication date	Dec 16, 2025
Grant date	Dec 16, 2025

Abstract

The invention provides pharmaceutical compositions comprising about 0.05 to 0.1% (w/v) cyclosporine dissolved in 1-perfluorobutyl-pentane for use in the topical treatment of dry eye disease and provides for dosing and treatment methods thereof. The invention further provides kits comprising such compositions.

First claim

The invention claimed is:

1 . A method for reducing corneal and/or conjunctival inflammation, the method comprising the step of topically administering to a human patient in need thereof an ophthalmic composition consisting of cyclosporine, 1-perfluorobutylpentane, 2-perfluorobutylpentane, and ethanol; wherein the cyclosporine is present in an amount of 0.1% (w/v), the 1-perfluorobutylpentane is present in an amount of at least 97% (w/w), the 2-perfluorobutylpentane is present in an amount of up to 2% (w/w), and the ethanol is present in an amount of up to 1.0% (w/w); wherein the composition is administered twice per day per eye as a single drop having a volume of about 10 μl.

2 . The method according to claim 1 , further comprising measuring inflammation; wherein the corneal inflammation is measured by fluorescein staining and the conjunctival inflammation is measured by lissamine green staining.

3 . The method according to claim 1 , wherein the method is a method for reducing corneal inflammation in the patient in need thereof.

4 . The method according to claim 1 , wherein the method is a method for reducing conjunctival inflammation in a patient in need thereof.

5 . The method according to claim 1 , wherein the patient is not responsive to treatment with artificial tears.

6 . The method according to claim 1 , wherein the patient has at least one eye with:
a. a score of >40 on the dryness visual analogue scale (VAS); b. a total corneal fluorescein staining score of >6; c. a total lissamine green conjunctival staining score of >2; or d. a Schirmer's Test I score >2 mm and <8 mm.

7 . The method according to claim 3 , wherein the patient has at least one eye with:
a. a total corneal fluorescein staining score of at least 6; or b. a central corneal fluorescein staining score of at least 1.

8 . The method according to claim 4 , wherein the patient has at least one eye with a total lissamine green conjunctival staining score of at least 2.

9 . The method according to claim 1 , wherein the patient has dry eye disease.

10 . The method according to claim 1 , wherein the patient has moderate to severe dry eye disease.

11 . The method according to claim 1 , wherein the patient has moderate to severe dry eye disease characterized by at least one or a combination of the following:
a. a total corneal fluorescein staining score of >6; b. being symptomatic with a score of >40 on the dryness visual analogue scale (VAS); c. a score >20 on the Ocular Surface Disease Index (OSDI); or d. a Schirmer's Test I score of >2 mm and <8 mm.

12 . The method according to claim 1 , wherein the amount of cyclosporine administered in a single dose per eye is about 10 μg and wherein the total daily dosage of cyclosporine administered per eye is about 20 μg.

13 . The method according to claim 1 , wherein the 2-perfluorobutylpentane is present in an amount selected from the group consisting of up to 1% (w/w) and up to 0.5% (w/w).

14 . The method according to claim 7 , wherein the patient has dry eye disease.

15 . The method according to claim 8 , wherein the patient has dry eye disease.

16 . The method according to claim 13 , wherein the patient has dry eye disease.

Assignees

• Novaliq Gmbh

Inventors

• Beier Markus
• Haisser Jörg
• Meides Alice
• Krösser Sonja
• Voss Hartmut
• LÖSCHER Frank
• Günther Bernhard

Classifications

• A61P27/02

  Ophthalmic agents · CPC title

• A61J1/00

  Containers specially adapted for medical or pharmaceutical purposes (capsules or the like for oral use A61J3/07; specially adapted for surgical or diagnostic appliances or instruments A61B50/30; containers for radioactive substances G21F5/00) · CPC title

• A61K31/00

  Medicinal preparations containing organic active ingredients · CPC title

• A61K47/06

  Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite · CPC title

• A61K9/08 Primary

  Solutions {(composition of solutions A61K47/00)} · CPC title