Compositions and methods for treating diabetes, hypertension and hypercholesterolemia
Inventors
THAI, NGOC • POLLETT, JONATHAN
Assignees
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Publication Number
US-10548941-B2
Publication Date
2020-02-04
Expiration Date
Abstract
The present invention provides a composition comprising a therapeutically effective amount of a polypeptide, peptide, or analog corresponding to one or more of SEQ ID NO(s) 1, 2, 3 or 4, and or more of a pharmaceutically acceptable carrier, pharmaceutically acceptable diluent, and/or pharmaceutically acceptable excipient. The polypeptide therapeutic of the present invention may be formulated for administration to a subject in need of treatment as an oral formulation, a parenteral formulation, a topical formulation, an aqueous formulation, a solid formulation, a lyophilized formulation, or a trans-dermal formulation. Also disclosed is a method for treating at least one of diabetes, and/or hyperglycemia, and/or hypercholesterolemia, and/or hypertension in a subject, comprising: administering to the subject a polypeptide of the invention or formulation of the invention.
Core Innovation
The disclosed invention relates to RPS2-derived polypeptides and peptide analogs, including fragments and sequence-identity variants, defined by SEQ ID NOs 1-4. The polypeptides are formulated with pharmaceutically acceptable carriers and administered to treat diabetes and hyperglycemia.
The invention addresses the treatment of diabetes and hyperglycemia, including in subjects with comorbid hypercholesterolemia and hypertension. The disclosed polypeptide compositions are reported to lower blood glucose to less than 200 mg/dL, and to reduce insulin resistance, hepatic glucose production, and glucagon.
The disclosed compositions are also reported to reduce systolic and diastolic blood pressure and cholesterol levels. The described example data include ZDF type 2 and STZ type 1 animal models, together with toxicology and pharmacokinetic findings and mechanistic findings indicating activity of C-terminal fragments relative to N-terminal fragments in an endothelial MTT assay.
Claims Coverage
The independent claim covers a pharmaceutical composition comprising a therapeutically-effective amount of a polypeptide of SEQ ID NO: 1 sufficient to lower blood glucose to less than 200 mg/dL. Dependent claims further define administration routes, formulation components, dosage form, and additional physiological effects, and include a related mammal glycemic-control method.
Blood glucose lowering to less than 200 mg/dL with SEQ ID NO: 1 polypeptide composition
A pharmaceutical composition comprising a therapeutically-effective amount of a polypeptide of SEQ ID NO: 1, wherein the therapeutically effective amount is sufficient to lower blood glucose level in a subject to less than 200 mg/dL.
Oral or parenteral administration of the SEQ ID NO: 1 composition
The pharmaceutical composition is suitable for oral or parenteral administration.
Formulation with pharmaceutically acceptable carrier, diluent, and/or excipient
The pharmaceutical composition further comprises one or more pharmaceutically acceptable carrier, diluent, and/or excipient.
Solid dose pharmaceutical formulation
The composition is a solid dose pharmaceutical formulation.
Additional reductions in hepatic glucose production, cholesterol, glucagon, and blood pressure
When administered to a subject in need thereof, the composition reduces hepatic glucose production, cholesterol levels, glucagon levels, and blood pressure.
Glycemic control method in a mammal using SEQ ID NO: 1 composition
A method of achieving glycemic control in a mammal by administering the pharmaceutical composition of claim 1, with a dose sufficient to lower blood glucose to less than 200 mg/dL.
Overall, the claim set centers on a SEQ ID NO: 1 polypeptide pharmaceutical composition that lowers subject blood glucose to less than 200 mg/dL, with dependent claim refinements addressing administration, formulation components, solid dosage, additional target reductions, and a corresponding mammal glycemic-control method.
Stated Advantages
Lowering blood glucose levels in a subject to less than 200 mg/dL.
Reducing hepatic glucose production.
Reducing cholesterol levels.
Reducing glucagon levels.
Reducing blood pressure.
Documented Applications
Treating diabetes and hyperglycemia, including reduction of blood glucose to less than 200 mg/dL, in animal models (ZDF type 2 and STZ type 1) with reported pharmacokinetic and toxicology findings.
Use of RPS2-derived polypeptide/peptide analog compositions in subjects with comorbid hypercholesterolemia and hypertension, with reported reductions in cholesterol and systolic/diastolic blood pressure.
Formulation and administration described for multiple routes including oral, parenteral, topical, transdermal, and solid or lyophilized formulations.
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