Methods and compositions for treating dry eye disease and other eye disorders
Inventors
Jain, Sandeep • Kompella, Uday Bhaskar • Musunuri, Shankar
Assignees
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Publication Number
US-9877964-B2
Publication Date
2018-01-30
Expiration Date
Abstract
The present invention relates to a method for treating a dry eye syndrome using an alpha 2 adrenergic agonist, pharmaceutically acceptable salt thereof or a mixture thereof. In particular, the alpha 2 adrenergic agonist of the invention has a higher alpha 2A agonist activity compared to alpha 2B agonist activity. This invention also relates to an ophthalmic composition comprising a therapeutically effective amount of an alpha 2 adrenergic agonist, a pharmaceutically acceptable salt thereof or a combination thereof as an active ingredient for treating a dry eye syndrome.
Core Innovation
The invention relates to methods of treating a patient suffering from dry eye syndrome by administering to an eye of the patient an ophthalmological pharmaceutical formulation comprising an active ingredient for treatment of dry eye syndrome. The active ingredient consists essentially of a therapeutically effective amount of an alpha 2 adrenergic agonist, or a pharmaceutically acceptable salt, having higher alpha 2A agonist activity compared to alpha 2B agonist activity.
The invention further provides application to Meibomian gland dysfunction by applying an ophthalmic solution having an active ingredient for treating MGD. The methods encompass treatment applied to selected ocular tissues or glands including the margin of the eyelid, the ocular surface, the Meibomian gland, and the lacrimal gland.
In addition to the therapeutic methods, the invention includes an aqueous ophthalmic solution for treating dry eye syndrome. The aqueous ophthalmic solution consists essentially of a therapeutically effective amount of an alpha 2 adrenergic agonist, a pharmaceutically acceptable excipient, and water, and brimonidine, or a pharmaceutically acceptable salt, is identified as a specific alpha 2 adrenergic agonist option.
The invention is directed to treating dry eye conditions including aqueous tear-deficient dry eye, evaporative dry eye, mixed mechanism dry eye, ocular graft-versus-host disease, Sjogren and non-Sjogren dry eye, and dry eye as a complication of LASIK refractive surgery using an alpha 2 adrenergic agonist selected to have higher alpha 2A agonist activity than alpha 2B agonist activity.
Claims Coverage
The independent claims cover three main treatment modalities using an alpha 2 adrenergic agonist with higher alpha 2A agonist activity than alpha 2B agonist activity. The inventive features are the alpha 2A over alpha 2B activity selectivity and the claimed formulation or solution construction for ocular delivery.
Alpha 2A-selective alpha 2 adrenergic agonist for dry eye syndrome
Administering an ophthalmological pharmaceutical formulation comprising an active ingredient for treatment of dry eye syndrome, wherein the active ingredient consists essentially of a therapeutically effective amount of an alpha 2 adrenergic agonist or a pharmaceutically acceptable salt thereof to treat dry eye syndrome, and wherein the alpha 2 adrenergic agonist has higher alpha 2A agonist activity compared to alpha 2B agonist activity.
Alpha 2A-selective alpha 2 adrenergic agonist ophthalmic solution for MGD
Applying an ophthalmic solution having an active ingredient for treating Meibomian gland dysfunction to each eye of the subject, wherein the active ingredient consists essentially of a therapeutically effective amount of an alpha 2 adrenergic agonist, and wherein the alpha 2 adrenergic agonist has higher alpha 2A agonist activity compared to alpha 2B agonist activity.
Aqueous ophthalmic solution with alpha 2A-selective alpha 2 adrenergic agonist
Providing an aqueous ophthalmic solution for treating a patient suffering from dry eye syndrome, wherein the aqueous ophthalmic solution consists essentially of a therapeutically effective amount of an alpha 2 adrenergic agonist, a pharmaceutically acceptable salt thereof or a combination thereof, a pharmaceutically acceptable excipient, and water, and wherein the alpha 2 adrenergic agonist has higher alpha 2A agonist activity compared to alpha 2B agonist activity.
Across the independent claims, coverage centers on ocular treatment of dry eye syndrome and MGD using an alpha 2 adrenergic agonist selected for higher alpha 2A agonist activity than alpha 2B agonist activity, delivered as an ophthalmological pharmaceutical formulation, an ophthalmic solution applied to each eye, or an aqueous ophthalmic solution consisting essentially of an active ingredient, excipient, and water.
Stated Advantages
Reduced redness/discomfort and improved MGD signs in working clinical examples.
Improved MGD signs in dry eye examples including ocular GVHD-related MGD, Sjogren and non-Sjogren dry eye, and LASIK-attributable evaporative dry eye.
Documented Applications
Treatment of dry eye syndrome including mixed mechanism dry eye, aqueous tear-deficient dry eye, and evaporative dry eye.
Treatment of Meibomian gland dysfunction (MGD).
Treatment of ocular graft-versus-host disease (oGVHD)-related MGD.
Treatment of Sjogren dry eye syndrome and non-Sjogren dry eye syndrome.
Treatment of LASIK-attributable evaporative dry eye as a complication of LASIK refractive surgery.
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