Methods 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 treating and preventing ocular Demodex-related conditions, including blepharitis, ocular rosacea, and inflammation associated with Demodex mites. It provides topical ophthalmic formulations for direct ocular-local delivery to the ocular surface, eyelid margins, eyelashes, and meibomian gland orifices, using eye drops and related ophthalmic dosage forms.

The ophthalmic composition contains parasiticidal actives, primarily isoxazoline parasiticides including lotilaner, fluralaner, sarolaner, afoxolaner, and fluxametamide, and alternatively formamidine parasiticides including amitraz, DPMF, and 2,4-dimethylanaline. The formulation is described as sterile and non-irritating, with excipient strategies such as polysorbate for solubility and buffering or pH stability to support ocular contact and residence time.

The document emphasizes targeted delivery concepts in which the formulation is delivered directly to ocular surface components and associated anatomical areas, including contacting meibomian orifices and areas outside eyelid margins. It also discusses diagnostic approaches for Demodex quantification without epilation, including diagnostic hydrogel contact lens approaches and tear or lens sampling for Demodex DNA or PCR and other biomarkers.

Claims Coverage

The independent claims cover three treatment outcomes: treating blepharitis caused by Demodex mites, treating eyelid margin redness caused by Demodex mites, and eradicating Demodex mites. Each is implemented by topically administering an eye-drop ophthalmic composition directly to the ocular surface and/or adjacent eyelid or eyelash anatomy, with the core inventive structure repeated as lotilaner with a pharmaceutically acceptable vehicle in eye-drop form.

All independent claims are grounded in topical delivery of an eye-drop ophthalmic composition containing lotilaner and a pharmaceutically acceptable vehicle, directed to the ocular surface and, for eyelid margin redness, also eye, eyelids, or eyelashes, to achieve treatment or eradication of Demodex-associated conditions.

Stated Advantages

Documented Applications

No documented applications found