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Assignees
Member
Vascular BioSciencesVascular Biosciences (VBS) is an innovative biomedical company developing breakthrough solutions to critical military and civilian medical challenges including: Military Infectious Diseases, Sepsis, Combat Casualty Care, Acute High Altitude Pulmonary Edema, and CBRN medical countermeasures. Our inflammation homing peptide, CARSKNKDC (CAR), enables increased localized concentrations of drugs to dramatically improve therapeutic outcomes with reduced side-effects. CAR converts systemically administered drugs into precision medicines. CAR peptide, by itself, also dramatically speeds up wound healing.
Vascular Biosciences (VBS) is an innovative biomedical company developing breakthrough solutions to critical military and civilian medical challenges including: Military Infectious Diseases, Sepsis, Combat Casualty Care, Acute High Altitude Pulmonary Edema, and CBRN medical countermeasures. Our inflammation homing peptide, CARSKNKDC (CAR), enables increased localized concentrations of drugs to dramatically improve therapeutic outcomes with reduced side-effects. CAR converts systemically administered drugs into precision medicines. CAR peptide, by itself, also dramatically speeds up wound healing.
Publication Number
US-11524077-B2
Publication Date
2022-12-13
Expiration Date
Abstract
Disclosed are compositions and methods useful for oral delivery of targeted therapies for pulmonary diseases, fibrotic disorders and cancer. The compositions and methods are based on peptide sequences that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. The disclosed targeting is useful for oral delivery of therapeutic and detectable agents to diseased tissue in an animal.
Core Innovation
The invention concerns an orally active targeting peptide (CAR) and variants for homing to diseased tissue, including hypertensive pulmonary vasculature, acutely injured lungs, and fibrotic pulmonary tissue. The disclosed peptides are defined by sequences selected from SEQ ID NOs: 2, 3, 4, 5, 6, and 7 and additionally SEQ ID NOs: 8 through 12. The peptides include linear and cyclic forms, including variants such as AKNKDCCAR, GKNKDCCAR, MKNKDCCAR, SKNKDCCAR, TKNKDCCAR, VKNKDCCAR and cyclic variants including CARAKNKDC, CARGKNKDC, CARMKNKDC, CARTKNKDC, and CARVKNKDC.
The disclosed approach provides a treatment that yields a measurable, disease-selective benefit while using an orally active targeting peptide. The background and disclosure emphasize co-administration with a therapeutic compound to achieve a bystander effect, enabling benefit in the diseased target region rather than relying on direct peptide activity alone. The therapeutic compound conveys a measurable therapeutic benefit to an individual suffering from a disease, in combination with the orally active composition.
The document also provides experimental support for orally active delivery and target-selective outcome in pulmonary settings, including pulmonary hypotensive activity and a measurable reduction in right ventricular systolic pressure (RVSP) without a corresponding systemic arterial pressure (SAP) change. In addition, trypsin proteolysis stability data support an oral availability rationale, including that cyclic CAR yields a predominant SKNKDCCAR (SEQ ID NO:5) and that this cyclic peptide is more resistant to further trypsin degradation than cyclic or linear CAR.
Claims Coverage
The independent claim covers a method of treating a disease using an orally active targeting peptide selected from specified SEQ ID NOs, co-administered with at least one therapeutic compound that provides a measurable therapeutic benefit, with therapeutic benefit measured in the individual. This independent claim is supported by dependent claim sets that narrow peptide origin, enumerate the disease set, impose disease-specificity on the therapeutic compound, restrict the therapeutic compound to a listed panel, and optionally narrow the therapeutic compound class to vasodilators.
Orally active targeting peptide selected from specified SEQ ID NOs
Providing an orally active targeting peptide comprising a sequence, where the sequence consists of at least one member selected from SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11 and SEQ ID NO: 12.
Therapeutic compound conveying measurable therapeutic benefit
Providing at least one therapeutic compound which conveys a measurable therapeutic benefit to an individual suffering from a disease.
Co-administration of oral composition containing peptide and therapeutic compound
Co-administering an oral composition comprising the orally active targeting peptide and the at least one therapeutic compound to the individual in need thereof.
Measuring therapeutic benefit in the individual
Measuring the therapeutic benefit to the individual.
Overall claim coverage centers on an oral composition that includes an orally active targeting peptide defined by specified SEQ ID NOs and a therapeutic compound that provides a measurable therapeutic benefit, with benefit measured in the individual. Dependent refinements in the provided claim set specify peptide origin, limit the disease to enumerated conditions, require disease-specificity of the therapeutic compound, restrict the compound to a detailed list of therapeutic agents, and optionally narrow the compound to vasodilators.
Stated Advantages
Measurable, disease-selective therapeutic benefit is enabled by co-administration with an orally active targeting peptide (bystander effect).
Orally active delivery is presented to yield pulmonary hypotensive/adjuvant activity.
A measurable reduction in right ventricular systolic pressure (RVSP) is presented without a systemic arterial pressure (SAP) change.
Cyclic CAR is presented as more resistant to further trypsin degradation, supporting an oral availability rationale.
Documented Applications
Treatment of pulmonary hypertension and hypertensive pulmonary vasculature, including pulmonary hypotensive/adjuvant activity with disease-selective benefit.
Treatment associated with acutely injured lungs, including acute lung injury (ALI) and acute respiratory distress syndrome (ARDS).
Treatment associated with fibrotic pulmonary tissue and fibrotic disorders.
Use of co-administration with therapeutic compounds to achieve a bystander effect for disease-selective benefit.
Treatment across a stated set of diseases including pulmonary, systemic, cardiovascular, inflammatory, infectious, and other conditions as enumerated in the dependent claim set.
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