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Publication Number
US-10188661-B2
Publication Date
2019-01-29
Expiration Date
Abstract
Described herein is a novel dosage regimen, and related uses and methods, for a prostaglandin FP receptor agonist (PFPRA) compound topically administered to the skin. The dosage regimen is useful for reduction of subcutaneous fat, for example, in patients who suffer from local excesses of subcutaneous fat. A particular advantage of the dosage regimen is the ability to reduce composition exposure and thereby promote convenience and comfort, while maintaining the desired exposure and therapeutic effect in subcutaneous fat. Further provided are kits according to the novel dosage regimen, comprising a PFPRA composition and instructions for use.
Core Innovation
The disclosed invention relates to a topical dosage regimen for prostaglandin FP receptor agonists, including latanoprost and related analogs and/or prodrugs, to locally reduce body fat. The approach is based on experimentally discovered skin, dermis, and subcutaneous fat pharmacokinetics, focusing on where transcutaneous delivery occurs and how long the compound and/or an active metabolite persists after application.
The regimen emphasizes that most of the dermal delivery occurs within a time window of about 4 to 12 hours after administering to the skin surface. It further emphasizes that the compound or active metabolite persists in the dermis and/or subcutaneous fat for 24 hours or more.
To balance local fat reduction with patient comfort and convenience, the invention includes removing the topical composition or residue from the skin surface between about 4 and about 12 hours after the administering. In some instances, the removal occurs after the dermis is substantially loaded or after more than about 60% of the 24-hour flux has occurred, while maintaining delivery to deeper fat/dermis.
Claims Coverage
The provided material includes two independent claims, both directed to methods for locally reducing body fat using a latanoprost-containing composition applied to the skin surface and a removal step within a defined post-administration interval. Across the two independent claims, three main inventive constraints are explicitly set out.
Latanoprost topical administration with removal between 4 and 12 hours
Administering a composition comprising latanoprost to the skin surface and removing the composition or residue thereof from the skin surface between about 4 hours and about 12 hours, inclusive, after said administering.
Removal after a 24-hour flux threshold is reached
More than about 60 percent of the 24-hour flux of latanoprost or an active metabolite thereof occurs within 4 to 12 hours, inclusive, after the step of administering, and the step of removing is after more than about 60 percent of the 24-hour flux has occurred.
Latanoprost topical administration with dermis fully loaded within 4 to 12 hours
Administering a composition comprising latanoprost to the skin surface and removing the composition or residue thereof from the skin surface between about 4 hours and about 12 hours, inclusive, after said administering, wherein the dermis is fully loaded with latanoprost, an active metabolite thereof, or a combination thereof, within 4 to 12 hours, inclusive, after the administering.
Removal after dermis is fully loaded
The step of removing is after the dermis is fully loaded.
Both independent claims cover locally reducing body fat by applying a latanoprost-containing composition to the skin surface and removing the composition or residue between about 4 and about 12 hours. One claim ties removal to a 24-hour flux threshold, while the other ties removal to a dermis fully-loaded condition within 4 to 12 hours.
Stated Advantages
Improving comfort/convenience by reducing prolonged skin-surface exposure while maintaining delivery to deeper fat/dermis.
Documented Applications
Locally reducing body fat in a subject in need thereof.
Topical treatment of fat depots such as the submental area and eyelid fat/steatoblepharon.
Reducing body fat targeted as eyelid fat.
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