Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-8975224-B2
Publication Date
2015-03-10
Expiration Date
Abstract
We describe peptides and their uses for the treatment of autoimmune, inflammatory and metabolic diseases.
Core Innovation
The disclosed method treats an inflammatory condition in a human subject affected by it by administering an oral formulation comprising a peptide selected from a specified group of five peptides, in an amount that reduces serum TNF-α levels. The peptides are short C-terminal Serpin-derived peptides, particularly SP16 and alanine-substituted variants, described as anti-inflammatory and immunomodulatory agents. The description also includes peptide fusion formats and peptide modifications.
Reported supporting results include reduced inflammatory responses in mouse LPS/sepsis and arthritis models, including reduced arthritis paw-swelling scores after oral administration, and improved glycemic measures in diabetic mouse models. Additional results include reduced IL-6 secretion in cells, lower MMP1 secretion from primary human synoviocytes, and dose-dependent TLR2 activation. The supplied content does not directly show serum TNF-α reduction in humans, and the problem addressed is not explicitly described in patent.
Claims Coverage
There is one independent claim, directed to a method of treating an inflammatory condition in a human subject by oral administration of a specified peptide formulation to reduce serum TNF-α. The claim set presents five inventive features: the independent claim and four dependent refinements concerning the reduction level, peptide additions, D amino acids, and covered conditions.
Oral peptide formulation for reducing serum TNF-α
The independent claim covers treating an inflammatory condition in an affected human subject by administering an oral formulation comprising a peptide selected from five specified peptide sequences, in an amount that reduces serum TNF-α levels.
Quantified reduction relative to pretreatment TNF-α levels
A dependent claim specifies a reduction of at least 50% in TNF-α levels compared with levels before peptide administration.
Fusion peptide additions
Dependent claims specify attachment of at least one second peptide or protein to the peptide as a fusion peptide, including an epitope tag, a half-life extender, or both.
D amino acids
A dependent claim specifies that one or more amino acids of the peptide are D amino acids.
Specified inflammatory conditions
A dependent claim identifies type I and type II diabetes, lupus, graft versus host disease, uveitis, eczema, psoriasis, cystic fibrosis, rheumatoid arthritis, acute radiation syndrome, burn patients, and inflammatory bowel disease.
The claims center on oral administration of specified peptides to reduce serum TNF-α in a human subject with an inflammatory condition, with dependent claim elements addressing the reduction threshold, peptide fusion or modification, and the conditions treated.
Stated Advantages
The peptides are described as anti-inflammatory and immunomodulatory agents.
The method reduces serum TNF-α levels in a human subject affected by an inflammatory condition; a dependent claim specifies at least a 50% reduction relative to pretreatment levels, and embodiments with 50% or 75% reductions are reported.
Documented Applications
Treatment of inflammatory conditions in human subjects, including type I and type II diabetes, lupus, graft versus host disease, uveitis, eczema, psoriasis, cystic fibrosis, rheumatoid arthritis, acute radiation syndrome, burn patients, and inflammatory bowel disease.
Preclinical evaluation in models of inflammation, arthritis (including oral treatment), diabetes, and endotoxemia, including mouse LPS/sepsis models.
Interested in licensing this patent?