Dry powder formulation of caveolin-1 peptides and methods of use thereof
Inventors
Williams, III, Robert O. • Watts, Alan B. • Zhang, Yajie • SAHAKIJPIJARN, Sawittree • Christensen, Dale • Koleng, John J. • Shetty, Sreerama
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12280089-B2
Publication Date
2025-04-22
Expiration Date
Abstract
Provided herein are compositions comprising caveolin-1 (Cav-1) peptides. Further provided are methods of using the Cav-1 peptides for the treatment of lung infections or acute or chronic lung injury, particularly lung fibrosis.
Core Innovation
The invention provides dry powder formulations comprising caveolin-1 (Cav-1) scaffolding peptides, including an amino acid sequence of FTTFTVT (SEQ ID NO: 2) and peptide variants with 1-5 additional amino acids at the N- and/or C-terminus of SEQ ID NO: 2. The dry powder formulations are configured for inhaled treatment using a dry powder inhaler and are described as not comprising a pharmaceutically acceptable carrier or excipient, including essentially excipient-free formulations.
The peptides and dry powder composition are described with particle and solid-state characteristics, including particle size and respirable fractions, median particle diameter, and measurements such as MMAD, fine particle fraction (FPF), and emitted fraction (EF). The document further describes formulation processing options to produce the inhalable dry powder, including milling and drying approaches such as spray-drying and thin film freezing, and characterization methods for crystallinity, amorphous behavior, and moisture.
In vivo data in a mouse bleomycin fibrosis model are described, where inhaled CSP7 is reported to reduce collagen content and Ashcroft fibrosis scores.
Claims Coverage
The partial content provides two independent method claims. Across these claims, the coverage centers on treating a subject using an inhaled, carrier- or excipient-free dry powder formulation comprising specific Cav-1 scaffolding peptide sequences or particles containing those peptides, with additional particle-size and inhaler performance constraints defined in the second independent claim.
Dry powder inhaler treatment of COPD using Cav-1 scaffolding peptide without carrier or excipient
Administering to a subject having chronic obstructive pulmonary disease (COPD) a dry powder formulation comprising a peptide or a pharmaceutically acceptable salt, where the dry powder formulation does not comprise a pharmaceutically acceptable carrier or excipient, the peptide is FTTFTVT (SEQ ID NO: 2) or a variant with 1-5 additional amino acids at the N- and/or C-terminus, and administering is by a dry powder inhaler.
Carrier/excipient-free dry powder composition with specific peptide particles for inhaler administration
Administering to a subject an effective amount of a dry powder composition comprising particles comprising a peptide consisting of FTTFTVT (SEQ ID NO: 2) or a pharmaceutically acceptable salt thereof, where the particles have a median particle diameter of less than 5 μm, the dry powder composition does not comprise a pharmaceutically acceptable carrier or excipient, and the dry powder composition is administered using a dry powder inhaler.
Overall, the claim coverage is directed to inhaled, essentially excipient-free dry powder formulations featuring the Cav-1 scaffolding peptide sequence FTTFTVT (SEQ ID NO: 2) or defined N/C-terminal variants, with the second independent claim further requiring sub-5 μm median particle diameter and inhaler administration.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Inhaled treatment of lung infections and acute/chronic lung injury, especially lung fibrosis and pulmonary inflammatory/fibrotic disorders [procedural detail omitted for safety].
Treatment of chronic obstructive pulmonary disease (COPD) using a dry powder inhaler and carrier/excipient-free dry powder formulations.
Mouse bleomycin-induced lung fibrosis model, where inhaled CSP7 is reported to reduce collagen content and Ashcroft fibrosis scores.
Interested in licensing this patent?