Ophthalmic compositions for treating ocular Demodex using lotilaner formulations

Inventors

Azamian, Bobak Robert • Ackermann, Douglas Michael • Hickok, Shawn D. • Vehige, Joseph G.

Assignees

Tarsus Pharmaceuticals Inc

Abstract

Disclosed herein are methods for treating or preventing ophthalmic and dermatologic conditions in a patient, including ocular surface conditions such as blepharitis. The methods can include topically administering directly to an ocular surface of one or more eyes of a patient in need of treatment thereof an effective amount of an isoxazoline parasiticide, formamidine parasiticide, or other active ingredient, formulated into an ophthalmic composition, the ophthalmic composition further comprising a pharmaceutically acceptable vehicle. Compositions are also disclosed.

Core Innovation

The invention relates to ophthalmic compositions for treatment of ocular Demodex, including Demodex folliculorum and Demodex brevis, where the compositions are formulated as eye drops. The compositions include lotilaner together with a pharmaceutically acceptable vehicle, and the eye-drop formulations are described as sterile and nonirritating to the eye.

The document describes that the lotilaner concentration is present from about 0.10% to about 0.50% by weight with respect to the total weight of the composition. The formulations and administration concepts emphasize ocular-surface delivery as eye-drop form, and further embodiments relate to formulation choices within pharmaceutically acceptable vehicles.

The disclosed approach is directed to treating ocular Demodex infestation in a human patient and is associated with conditions such as blepharitis and ocular rosacea. The document also describes a proposed mechanism for mite paralysis/death involving GABA-chloride antagonism and preferential Demodex abdominal absorption of the drug.

In addition to isoxazoline parasiticides such as fluralaner, sarolaner, lotilaner, afoxolaner, and fluxametamide, the document identifies alternative active classes that may be used, including formamidine parasiticides, phenylpyrazoles, and certain Alzheimer’s drugs such as galantamine. The document further describes diagnostic and assessment approaches for mite quantification, including methods referenced for evaluating Demodex infestation to guide therapy.

Claims Coverage

The disclosed claim set includes at least one independent claim directed to an ophthalmic eye-drop composition comprising lotilaner in a pharmaceutically acceptable vehicle, with sterility and nonirritating properties to the eye, and a specified lotilaner concentration range. Dependent claim coverage further narrows the composition and intended use to ocular Demodex infestation in a human patient, with additional refinements for formulation and administration parameters as stated.

Overall, the claim coverage centers on a sterile, nonirritating ophthalmic eye-drop composition containing lotilaner in a defined concentration range, with dependent refinements that further restrict formulation features, specify intended therapeutic use for ocular Demodex infestation in a human patient, and state administration parameters in certain dependent claims.

Stated Advantages

Documented Applications

No documented applications found