Peptide saporin conjugate for the treatment of cancer
Inventors
Brown, Kathlynn C. • Allred, Curtis • McGuire, Michael
Assignees
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Publication Number
US-12576157-B2
Publication Date
2026-03-17
Expiration Date
Abstract
Disclosed herein, are compositions comprising one or more a molecular guidance system (MGS) peptides and a cytotoxic agent. Also described herein, are methods of administering the compositions to patients with cancer.
Core Innovation
The invention relates to targeted cancer therapies using molecular guidance system (MGS) peptides conjugated to the cytotoxic plant toxin saporin. Saporin acts as a ribosome-inactivating protein, providing a cytotoxic payload, while the MGS peptide provides molecular guidance to promote binding and internalization into cancer cells with reduced effects on normal tissues.
The described conjugates include membrane-permeable forms and intracellular targeting concepts, including targeting to intracellular compartments such as the lysosome. The MGS peptide sequences are provided as specified amino acid sequences, including PEGylated conjugate variants that use PEG linkers, with examples including PEG11 linker concepts and chemically modified MGS peptide forms.
The invention further describes therapeutic compositions including one or more cytotoxic agents conjugated to one or more MGS peptides, including PEG-linked MGS peptide-saporin conjugates and multivalent display architectures. Documented variants include covalent multimerization such as dimeric and tetrameric structures, as well as additional MGS peptide variants used for intracellular trafficking effects.
Claims Coverage
The provided independent claims cover two inventive features: defined MGS peptide sequences, including PEG11-linked variants, and compositions in which one or more cytotoxic agents are conjugated to one or more specified MGS peptides. Dependent features add multivalent conjugate architectures and pharmaceutically acceptable carrier formulation.
Peg11-linked MGS peptide sequence
A molecular guidance system (MGS) peptide selected from CH3CO-FHAVPQSFYT-PEG11-C-NH2 (SEQ ID No: 76) and FHAVPQSFY (SEQ ID NO: 78).
Cytotoxic-agent conjugate composition with specified MGS peptides
A composition comprising one or more cytotoxic agents conjugated to one or more molecular guidance system (MGS) peptides selected from LQWRRNFGVWARYRL (SEQ ID NO: 31), CH3CO-LQWRRNFGVWARYRL, CH3CO-LQWRRNFGVWARYRL-PEG11-C-NH2 (SEQ ID NO: 72), CH3CO-FHAVPQSFYT-PEG11-C-NH2 (SEQ ID NO: 76), FHAVPQSFY (SEQ ID NO: 78), and CH3CO-YAAWPASGAWT-PEG11-C-NH2 (SEQ ID NO: 71).
The claim coverage centers on defined MGS peptide sequences, including PEG11-linked variants, and on compositions containing cytotoxic agents conjugated to those specified MGS peptides. The dependent features further define covalent attachment, PEG linker inclusion, and multivalent dimeric or tetrameric conjugate architectures.
Stated Advantages
Promotes intracellular delivery of the cytotoxic payload.
Supports cancer-specific uptake with reduced effects on normal tissues.
Maintains activity in non-dividing cells.
Reduces the likelihood of resistance.
Uses small and economical peptide targeting.
Documented Applications
Treatment across multiple carcinoma types is described, including lung cancer, breast cancer, colorectal cancer, ovarian cancer, and pancreatic cancer.
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