Methods and compositions for topical delivery of prostaglandins to subcutaneous fat
Inventors
Singer, Michael S. • Kalayoglu, Murat V.
Assignees
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Publication Number
US-10869874-B2
Publication Date
2020-12-22
Expiration Date
Abstract
Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid, e.g., oleic acid, that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound or active metabolite thereof to subcutaneous fat under the skin. The therapeutic effect is, for example, reduction of the subcutaneous fat under the skin. Further provided are methods of reducing body fat in a subject comprising topically administering the composition to the subject. The present invention also provides kits comprising the composition and instructions for use.
Core Innovation
The invention relates to a method for reducing subcutaneous fat in a subject by topically administering a composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof. The composition further comprises a fatty acid, and the Formula (I) compound is defined with structural variable options including single or double bonds with cis/trans configuration and substituent definitions for A, B, X, Z, and R1/R2.
The disclosed compounds include prostaglandin F2α-related compounds and prostaglandin FP receptor agonist scope, including named compounds such as bimatoprost, bimatoprost isopropyl ester, bimatoprost free acid, travoprost, travoprost free acid, latanoprost, latanoprost free acid, tafluprost, and tafluprost free acid. The formulas further specify pharmaceutically acceptable salts, hydrates, solvates, stereoisomers, polymorphs, tautomers, isotopically enriched derivatives, and prodrugs.
The described formulation combines the Formula (I) compound with the fatty acid in a topical composition for delivery through skin toward subcutaneous tissue. The disclosure includes reference to skin-to-adipose delivery through skin barrier components and experimentally observed improved skin-to-adipose delivery and subcutaneous fat reduction associated with the formulation.
Claims Coverage
The consolidated claim coverage centers on one independent topical method for reducing subcutaneous fat. The inventive package includes a Formula (I) compound or pharmaceutically acceptable salt thereof, detailed structural definitions for Formula (I), and the requirement that the composition further comprises a fatty acid.
Topical administration for subcutaneous fat reduction with Formula (I) compound and fatty acid
A method for reducing subcutaneous fat in a subject by topically administering a composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein the composition further comprises a fatty acid.
Formula (I) structural scope with cis/trans configuration and substituent variables
The compound of Formula (I) is defined such that each instance of a bond which can be in the cis or trans configuration is independently cis or trans, with structural variables including A, B, X, Z, and R1/R2, together with related variables R4, R5, R6, R7, and m.
Prostaglandin F2α-related and prostaglandin FP receptor agonist scope
The disclosed Formula (I) compounds include prostaglandin F2α-related compounds and prostaglandin FP receptor agonist scope, including named compounds such as bimatoprost, travoprost, latanoprost, and tafluprost, together with their free acid forms and related variants.
Across the independent claim, the inventive coverage is the combination of a Formula (I) compound with a fatty acid in a topical composition for reducing subcutaneous fat, with the Formula (I) compound constrained by cis/trans configuration and defined substituent classes. The claims also identify prostaglandin F2α-related and prostaglandin FP receptor agonist compounds within the Formula (I) scope.
Stated Advantages
Improved skin-to-adipose delivery.
Subcutaneous fat reduction.
Documented Applications
Topically administering a composition for reducing subcutaneous fat in a subject.
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