Methods for reducing body fat using tafluprost and analogs thereof
Inventors
Kalayoglu, Murat V. • Singer, Michael S.
Assignees
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Publication Number
US-9861641-B2
Publication Date
2018-01-09
Expiration Date
Abstract
Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7′, Z, Y, n, y, and x, are as defined herein.
Core Innovation
The invention relates to local administration methods for reducing body fat and/or adipocytes in a subject having an excess deposit of body fat. It administers prostaglandin FP receptor agonist compound, including tafluprost, to the skin to achieve reduction of body fat and adipocyte-associated endpoints such as adipose thickness and adipocyte size.
The invention provides a broad compound scope through Formula (I) with X substituents (—OR1, —SR2, —NR3R4), and includes compounds defined by Formula (II) as well as tafluprost free acid (with R1 hydrogen) and tafluprost (with R1 as an isopropyl ester). The document also includes tafluprost thioesters and tafluprost amides, and additionally mentions further compounds via Formula (V) for use as locally administered prostaglandin FP receptor agonists.
It also includes pharmaceutically acceptable salts, hydrates, solvates, stereoisomers, polymorphs, tautomers, isotopically enriched derivatives, and prodrugs, and defines variable substituents using R1/R2/R3/R4 with Formula (II), Formula (IV), and Formula (V) embodiments. The invention is linked to pharmaceutical compositions containing the compound embodiments and to administration routes involving skin, including topical, subcutaneous, intradermal, and intralesional.
Claims Coverage
The independent claim set contains one independent claim. It covers a method for reducing body fat by administering, to the skin, a compound of Formula (II) or a pharmaceutically acceptable salt or stereoisomer, with dependent claims refining the indication, skin location, administration mode, and formulation/composition constraints.
Skin administration of Formula (II) compound for body fat reduction
A method for reducing body fat in a subject having an excess deposit of body fat by administering to the skin a compound of Formula (II), or a pharmaceutically acceptable salt or stereoisomer, wherein R1 is hydrogen or C1-C6 alkyl.
R1 limited to hydrogen or C1-C6 alkyl in Formula (II)
In the Formula (II) compound used in the method, R1 is hydrogen or C1-C6 alkyl, including specified alkyl groups such as methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, isobutyl, and sec-butyl.
Routes include subcutaneous, intradermal, or intralesional administration
Administering the compound using a route selected from subcutaneous, intradermal, or intralesional administration, including application to facial skin.
Compound concentration in the pharmaceutical composition is 0.001% to 1% w/w
Providing the compound in a pharmaceutical composition where the compound concentration is between 0.001% and 1% w/w inclusive, and the composition may comprise isopropyl myristate.
Overall, the claims coverage centers on a skin-administration method using a Formula (II) compound with R1 limited to hydrogen or C1-C6 alkyl, and dependent claims refine this by selecting particular R1 alkyls, specifying administration routes and anatomical region, and by adding formulation constraints including a 0.001% to 1% w/w concentration range and inclusion of isopropyl myristate.
Stated Advantages
Reducing body fat in a subject having an excess deposit of body fat.
Local body fat reduction is supported in examples for indications such as HIV lipodystrophy and periorbital/orbital fat prolapse.
The document states tafluprost is more effective than bimatoprost for local administration.
Documented Applications
Reducing body fat or adipocytes in a subject having an excess deposit of body fat using skin administration of the defined compounds.
Treating or reducing fat-related conditions explicitly mentioned in the document, including chin fat, gynecomastia, orbital fat prolapse, buffalo hump, HIV lipodystrophy, and lipoma/lipomatosis/Madelung disease.
Local delivery use cases at skin or skin-associated sites described in the document, including topical, subcutaneous, intradermal, and intralesional administration, including facial and palpebral skin and related local sites.
HIV lipodystrophy involving local body fat reduction, including dorsocervical fat pad.
Periorbital/orbital fat prolapse, including local body fat reduction in the periorbital/orbital region.
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