Isoxazoline parasiticide formulations and methods for treating blepharitis

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 topical ophthalmic treatment of Demodex blepharitis and ocular Demodex infestation in a human patient. It uses an ophthalmic composition formulated into an eye drop and includes an effective amount of an isoxazoline parasiticide, in some embodiments lotilaner, delivered directly to an ocular surface of one or more eyes using a pharmaceutically acceptable vehicle. The ophthalmic composition is described as sterile in at least one embodiment.

The treatment strategy specifies topically administering directly to the ocular surface, and in some embodiments to one or more of the eye, eyelids, or eyelashes. The delivery regimen includes repeated dosing, including twice daily for at least 4 weeks, and in certain embodiments twice daily for at least 6 weeks, with additional embodiments including at least one time daily for at least 4 weeks or other minimum duration thresholds. In some embodiments, the composition is applied when the eyes are closed to contact the Meibomian gland orifices outside the eyelid margins.

The ophthalmic composition is formulated with defined formulation constraints, including that the isoxazoline parasiticide can be the sole active ingredient. The composition may be described as not comprising tea tree oil in at least one method for ocular Demodex infestation. Formulation components include pharmaceutically acceptable vehicles, polysorbates, optional castor oil or hydrogenated castor oil, and thickeners described as HPMC, Pemulen TR, or similar polymers. A mechanistic rationale for miticidal action is described in terms of GABA-chloride antagonists and preferential abdominal absorption of Demodex mites.

Claims Coverage

The document includes four independent claims, each covering a topically administered ophthalmic eye-drop method using an isoxazoline parasiticide comprising lotilaner. Across these independent claims, the main inventive features focus on treating specific Demodex conditions, direct ocular-surface administration via an eye drop, formulation limitations such as sterile composition, absence of tea tree oil, and sole-active-ingredient status, and dosing frequency/duration and certain administration conditions.

Overall, the claim coverage centers on treating Demodex-related ocular conditions using a sterile or non-sterile ophthalmic eye-drop formulation with an effective amount of an isoxazoline parasiticide comprising lotilaner, including formulation limits such as sole active ingredient and, for at least one method, absence of tea tree oil. The independent claims also anchor treatment by topically administering to an ocular surface, or to eye, eyelids, or eyelashes, with defined dosing frequency and minimum duration requirements.

Stated Advantages

Documented Applications

No documented applications found