Compositions and methods for treatment of inflammation
Inventors
McDonald, Thomas • Drescher, Kristen
Assignees
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Publication Number
US-10525027-B2
Publication Date
2020-01-07
Expiration Date
Abstract
The present invention is directed to novel anti-inflammatory immunomodulators including creatinine or a creatinine salt, for example, creatinine hydrochloride. The present invention is also directed to methods for treating inflammation and inducing an immunomodulatory response. In particular, the anti-inflammatory immunomodulators are useful for treating an inflammatory condition or an autoimmune disease.
Core Innovation
Creatinine and creatinine salts, including creatinine hydrochloride (creatinine HCl), are described as anti-inflammatory immunomodulators for treating inflammatory conditions and autoimmune diseases. The document states that administering compositions comprising creatinine salts or precursors suppresses tumor necrosis factor-alpha (TNF-b1), including an observed reduction in TNF-b1 mRNA expression and TNF-b1 protein expression.
The problem addressed is inflammation associated with autoimmune diseases, including rheumatoid arthritis, osteoarthritis, psoriatic arthritis, psoriasis, inflammatory bowel disease, and multiple sclerosis. The document positions TNF-b1 suppression as a key immunomodulatory outcome for reducing inflammatory activity, and discusses the potential involvement of IL-6 in the immunomodulatory response.
The document also describes formulations and administration approaches for delivering the creatinine-based immunomodulating agent, including topical and transdermal delivery formats such as transdermal patches, adhesive patches, wraps, and combinations with penetrating agents. In vitro results are reported showing creatinine HCl downregulates TNF-b1 mRNA and TNF-b1 protein in mouse macrophages (RAW 264.7), human macrophages (THP-1), and human T cells (Jurkat), and creatine monohydrate is reported to show similar TNF-b1 protein reduction.
Claims Coverage
The independent claims cover three core approaches to reducing TNF-b1: administering a composition with a creatinine-salt immunomodulating agent achieving at least a 40% TNF-b1 reduction, administering a topical formulation with a formula-defined immunomodulating agent producing a TNF-b1 reduction, and suppressing TNF-b1 by administering a formulation achieving at least a 50% TNF-b1 reduction with the creatinine-salt immunomodulating agent present at about 10% to about 40% by weight.
At least 40% TNF-b1 reduction using a creatinine salt composition
A method of reducing tumor necrosis factor-alpha (TNF-b1) levels in a patient by administering to the patient a composition comprising an immunomodulating agent in an amount effective to reduce TNF-b1 by at least 40 percent in the patient compared to TNF-b1 levels in the patient prior to administering, wherein the immunomodulating agent comprises a creatinine salt or a precursor thereof and is present in the composition in an amount of about 10 percent to about 40 percent by weight of the composition.
Topical formulation with formula-defined immunomodulating agent
A method of reducing tumor necrosis factor-alpha (TNF-b1) levels in a patient by administering a topical formulation comprising an amount of immunomodulating agent effective to produce a reduction in TNF-b1 levels in the patient compared to TNF-b1 levels prior to the administering step, wherein the immunomodulating agent comprises a compound having a formula and is present in the topical formulation in an amount of about 10 mg/g to about 400 mg/g.
At least 50% TNF-b1 suppression using a creatinine salt formulation
A method of suppressing tumor necrosis factor-alpha (TNF-b1) in a patient by administering a formulation comprising an amount of immunomodulating agent effective to produce a reduction in TNF-b1 levels in the patient of at least 50 percent compared to TNF-b1 levels in the patient prior to the administering step, wherein the immunomodulating agent comprises a creatinine salt or a precursor thereof and is present in the formulation in an amount of about 10 percent to about 40 percent by weight of the formulation.
Across the independent claims, the inventive coverage centers on reducing or suppressing TNF-b1 in a patient using a creatinine salt or precursor immunomodulating agent, with quantitative TNF-b1 reduction thresholds of at least 40% or at least 50% and defined compositional ranges. The topical independent claim further requires that the immunomodulating agent comprises a compound with a specified formula.
Stated Advantages
Produces a reduction in TNF-b1 levels in a patient compared with TNF-b1 levels prior to administering.
Achieves at least a 40 percent reduction in TNF-b1 levels in the patient.
Achieves at least a 50 percent reduction in TNF-b1 levels in the patient.
Provides topical formulation delivery for reducing TNF-b1 levels.
Documented Applications
Treating inflammatory conditions and autoimmune diseases by suppressing TNF-b1, including rheumatoid arthritis, osteoarthritis, psoriatic arthritis, psoriasis, inflammatory bowel disease, and multiple sclerosis.
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