Compositions and methods for topical delivery of prostaglandins to subcutaneous fat

Inventors

Singer, Michael S. • Kalayoglu, Murat V.

Assignees

Topokine Therapeutics Inc

Abstract

Described herein are compositions comprising a prostaglandin FP receptor agonist (PFPRA) compound and a fatty acid ester (e.g., isopropyl myristate), optionally comprising an ointment base such as a hydrocarbon base (e.g., petroleum jelly) and/or an organic alcohol (e.g., propylene glycol), that, when topically applied to the skin, locally delivers a therapeutically effective amount of the PFPRA compound to subcutaneous fat under the skin, and methods of preparation. 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.

Core Innovation

The invention relates to topical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, together with isopropyl myristate. Formula (I) is defined by extensive structural variability through variables A, B, X, and Z, including optionally substituted alkylene, alkenylene, or alkynylene groups that can be interrupted by one or more —O— or —S— groups and bond configurations that can be cis or trans.

The structural definitions further specify X as —OR4, —SR4, or —N(R4)2 and Z as O, S, or NRZ, with defined substituent classes for R4 and RZ, and the compound definition includes relationships among R1, R2, R6, and R7. The disclosure also encompasses pharmaceutically acceptable forms and variants including salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, and prodrug.

The invention identifies specific PFPRA active agents and derivatives associated with the described Formula (I) embodiments, including latanoprost, tafluprost, travoprost, bimatoprost, CAY10509, and AL-12182, together with free acid and ester prodrug forms. The compositions are further described with topical formulation embodiments including an ointment base and organic alcohols, and are related to topical administration for reducing subcutaneous fat and body fat, including submental fat, periorbital fat, eyelids, and steatoblepharon.

Claims Coverage

The document includes one independent claim directed to a composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, formulated with isopropyl myristate. The claim covers a broad family of Formula (I) members defined by extensive structural variability, bond configuration, and substituent group definitions, with dependent narrowing claims also referenced in the provided material.

Coverage is anchored on a composition that includes a Formula (I) compound or pharmaceutically acceptable salt, defined by extensive structural variability, together with isopropyl myristate. Dependent refinements include Formula (I-a), sterile status, preservative and formulation component additions, and a use claim tied to reducing body fat in a subject.

Stated Advantages

Documented Applications