Tomatidine, analogs thereof, compositions comprising same, and uses for same

Inventors

Adams, Christopher M.DYLE, Michael C.Welsh, Michael

Assignees

University of Iowa Research Foundation UIRFUS Department of Veterans Affairs

Publication Number

US-10022386-B2

Publication Date

2018-07-17

Expiration Date

2033-08-02

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Abstract

In one aspect, the invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by providing to an animal in need thereof an effective amount of a compound. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Core Innovation

The invention relates to methods for promoting muscle hypertrophy or decreasing adiposity by administering an effective amount of a compound, specifically tomatidine or analogs thereof, to an animal in need thereof. The compounds disclosed can promote muscle hypertrophy, decrease adiposity, inhibit muscle atrophy, promote muscle health, normal muscle function, and healthy aging muscles.

The background identifies skeletal muscle atrophy as a characteristic of aging, starvation, and a consequence of various severe human illnesses, with no existing medical therapies to prevent or reverse it. Additionally, obesity associated with high adiposity is highlighted as a major societal problem leading to diseases and substantial treatment costs. Thus, there is a need for potent, efficacious, and selective compounds that promote muscle hypertrophy and decrease adiposity.

Claims Coverage

The patent contains multiple independent claims directed to methods of increasing muscle formation, muscle protein synthesis, reducing skeletal muscle atrophy, increasing the muscle to fat ratio, and decreasing adiposity using specific compounds including tomatidine and its analogs.

Method of increasing muscle formation, muscle protein synthesis, reducing skeletal muscle atrophy, increasing the ratio of skeletal muscle to fat, or decreasing adiposity

Administering an effective amount of a compound, including tomatidine or analogs thereof, to an animal in need thereof to achieve one or more of: promoting muscle formation, increasing muscle protein synthesis, reducing muscle atrophy, increasing muscle to fat ratio, or decreasing adiposity.

Use of compounds with specific structural features for muscle and adiposity modulation

Employing compounds having a structure represented by formula E1, with R51 selected from H and C1-C6 alkyl, for the therapeutic effects on muscle and adiposity.

Pharmaceutical or nutraceutical compositions comprising effective amounts of tomatidine compounds

Compositions containing at least 0.14% or 0.28% by weight of tomatidine or pharmaceutically acceptable salts thereof, provided as solutions, dispersions, suspensions, emulsions, or formulated in animal chow, medicinal food, energy or protein bars, drinks, teas, milks, cereals, infant formulas, or supplements.

Dosage regimens for administration of tomatidine compounds

Administration of said compounds in amounts greater than 5 mg, with dosing in the range of 0.1 to 250 mg/kg per day, preferably 0.5 to 100 mg/kg per day, delivered orally, including in capsules or tablets, with optional further additives such as preservatives, flavoring agents, colorants, or binders.

Treatment of various animals including livestock and pets

Application of the methods and compositions to a range of animals including non-human primates, horses, pigs, rabbits, dogs, sheep, goats, cows, cats, guinea pigs, fish, birds, and livestock such as pigs, cows, horses, goats, bison, and sheep.

The independent claims cover methods and compositions based on administration of tomatidine and related compounds or analogs to promote muscle hypertrophy, reduce muscle atrophy and adiposity, with defined structural features, dosages, and formulations applicable to various animals including humans and domesticated species.

Stated Advantages

Tomatidine promotes skeletal muscle hypertrophy and increases muscle strength and mass.

Tomatidine decreases adiposity, reducing fat mass in animals.

The compounds have favorable safety profiles based on consumption studies and animal models.

Tomatidine enhances exercise capacity and muscle function.

Documented Applications

Treatment of muscle atrophy in conditions including malnutrition, aging, immobilization, chronic diseases such as cancer, congestive heart failure, chronic pulmonary and renal diseases, diabetes, genetic and autoimmune muscle diseases, burns, sepsis, mechanical ventilation, spaceflight, and sarcopenia.

Promotion of muscle hypertrophy and increased muscle mass and strength in mammals, including humans, rodents, fish, and birds.

Decreasing adiposity and reducing obesity and related metabolic disorders such as type 2 diabetes and fatty liver disease in mammals, including diet-induced obesity models.

Manufacture of pharmaceutical and nutraceutical compositions and medicaments containing tomatidine and analogs for prevention and treatment of disorders involving muscle atrophy, adiposity, and related conditions.

Use as pharmacological tools for developing in vitro and in vivo test systems evaluating muscle atrophy inhibitors and promoters of muscle health.

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