Compounds and methods for treating or preventing anterior segment ocular disorders and/or retinal degenerations
Inventors
Fields, Mark • Del Priore, Lucian • Cai, Huey • Hoyer, Denton
Assignees
Publication Number
US-12310970-B2
Publication Date
2025-05-27
Expiration Date
2039-01-08
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Abstract
The invention provides a method of treating retinal degenerations, such as but not limited to anterior segment ocular disorders and/or age-related macular degeneration (AMD), in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of a compound of formula (1) or formula (2). In a further aspect, the invention provides compounds of formula (2). In certain embodiments, the compounds of the invention prevent or minimize cellular assault, such as oxidative stress-related cellular assault, and/or promote cell viability.
Core Innovation
The invention provides methods and compositions for treating retinal degenerations—including but not limited to anterior segment ocular disorders and age-related macular degeneration (AMD)—in a subject by administering a pharmaceutical composition comprising an effective amount of a compound of formula (1) or formula (2). The invention also provides specified compounds of formula (2) and pharmaceutical compositions containing these compounds.
The compounds of the invention act to prevent or minimize cellular assault, including oxidative stress-related cellular assault, and/or promote cell viability. These compounds specifically protect retinal cells, such as retinal pigment epithelium (RPE) cells, from cell death caused by oxidative stress or damage and enhance the metabolic function of such cells, which is beneficial for maintaining vision and addressing degenerative processes in ocular tissues.
The problem being addressed is that retinal degenerations such as AMD and anterior segment ocular disorders (like Fuchs endothelial corneal dystrophy, cataracts, glaucoma, and keratoconus) are major causes of blindness and currently lack effective treatments, especially for forms such as 'dry' AMD. Oxidative stress is a significant contributing factor in the pathology of these diseases, causing cell damage and death. The compounds and methods disclosed aim to provide effective therapies to slow, retard, or prevent the development and progression of such ocular disorders.
Claims Coverage
There are two independent claims in this patent, each covering a separate inventive feature.
Ophthalmologically acceptable formulation comprising ciclopirox, cyclodextrin, and an analgesic agent
An ophthalmologically acceptable formulation suitable for topical administration to the eye of a subject, comprising: - A therapeutically effective amount of ciclopirox (6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone), or a salt or solvate thereof. - At least one compound selected from hydroxypropyl-alpha-cyclodextrin and hydroxypropyl-beta-cyclodextrin. - At least one analgesic agent. This formulation is tailored for ocular use and supports co-delivery of ciclopirox with specific cyclodextrins and analgesic agents to the eye.
Packaged pharmaceutical kit including ciclopirox formulation and instructions for ocular administration
A packaged pharmaceutical kit comprising: - A container holding an ophthalmologically acceptable formulation suitable for topical administration to the eye of a subject, wherein the formulation includes: - An effective amount of ciclopirox (6-cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone), or a salt or solvate thereof; - At least one compound selected from hydroxypropyl-alpha-cyclodextrin and hydroxypropyl-beta-cyclodextrin; - At least one analgesic agent. - Instructions for applying the ophthalmologically acceptable formulation topically to the eye of the subject. The claim also contemplates that the formulation may be used for treating retinal degeneration and related ocular disorders.
In summary, the independent claims cover an ophthalmically suitable ciclopirox formulation with specific cyclodextrins and analgesic agents, as well as a pharmaceutical kit that includes this formulation and detailed instructions for ocular administration.
Stated Advantages
The compounds and methods protect or rescue retinal pigment epithelial (RPE) cells and other ocular cells, which helps prevent disease progression in degenerative retinal and anterior segment ocular disorders.
The compounds mitigate risk of oxidative stress damage, thereby enhancing cell viability and promoting metabolic function (such as ATP production and mitochondrial respiration) in relevant cell types.
The formulations can be administered in various ocular delivery forms, including cyclodextrin-based solutions, suspensions, or lyophilized forms, providing flexibility for clinical use.
Documented Applications
Treatment or prevention of retinal degeneration, including age-related macular degeneration (AMD).
Treatment or prevention of anterior segment ocular disorders, including Fuchs Endothelial Corneal Dystrophy, cataracts, glaucoma, and keratoconus.
Promoting cell viability and preventing cell death (including oxidative stress-induced cell death) in ocular cells such as lens epithelial cells and corneal endothelial cells.
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