Peptide receptor radionuclide therapy
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Publication Number
US-12649008-B2
Publication Date
2026-06-09
Expiration Date
Abstract
The present disclosure provides methods and related compositions that incorporate a molecularly targeted approach via the integrin subtype αvβ6 using Peptide Receptor Radionuclide Therapy (PRRT) and a theranostic approach.
Core Innovation
The disclosed invention relates to pharmaceutical compositions and therapeutic and diagnostic conjugates based on a specific peptide having the amino acid sequence GNGVPNLRGDLQVLGQRVGRT (SEQ ID NO.: 1). The compositions and conjugates include a PEGylated peptide structure with a first PEG moiety covalently attached to the N-terminus and a second PEG moiety covalently attached to the C-terminus, provided as a therapeutic conjugate of Formula I and a diagnostic conjugate of Formula II.
The invention relates to an αvβ6 integrin-targeted peptide receptor radionuclide therapy (PRRT) theranostic approach using the PEGylated RGD peptide. The therapeutic conjugate of Formula I and the diagnostic conjugate of Formula II are administered in a theranostic workflow that includes diagnostic imaging followed by therapeutic administration, with radionuclides such as 68Ga for diagnostic imaging and 177Lu for therapy.
The disclosed content addresses αvβ6 integrin-related cancers by providing a specific PEGylated peptide conjugate architecture suitable for imaging and therapy. The content includes application to pancreatic ductal adenocarcinoma (PDAC) and other epithelial-derived cancers enumerated in the claims.
Claims Coverage
The independent claims cover three core inventive feature groups: a defined peptide sequence, a PEGylated conjugate architecture with first and second PEG moieties covalently attached to the N- and C-termini, and use of Formula I/Formula II conjugates for treatment or imaging respectively.
Defined peptide (SEQ ID NO.: 1) in a pharmaceutical composition
A pharmaceutical composition comprising a peptide having the amino acid sequence GNGVPNLRGDLQVLGQRVGRT (SEQ ID NO.: 1).
Therapeutic conjugate of Formula I with N- and C-terminus PEG moieties
A method for treating an αvβ6 integrin-related cancer comprising administering a dose of a therapeutic conjugate of Formula I to a subject in need of treatment, wherein 5G is a PEGylated peptide having an N-terminus, a C-terminus, and the amino acid sequence GNGVPNLRGDLQVLGQRVGRT (SEQ ID NO.: 1), and wherein a first PEG moiety is covalently attached to the N-terminus of the peptide and a second PEG moiety is covalently attached to the C-terminus of the peptide.
Diagnostic conjugate of Formula II for imaging with N- and C-terminus PEG moieties
A method for imaging a tumor, a cancerous lesion, or a cancer cell comprising administering a diagnostic conjugate comprising Formula II and a pharmaceutically acceptable excipient to a subject, wherein 5G is a PEGylated peptide having an N-terminus, a C-terminus, and the amino acid sequence GNGVPNLRGDLQVLGQRVGRT (SEQ ID NO.: 1), and wherein a first PEG moiety is covalently attached to the N-terminus of the peptide and a second PEG moiety is covalently attached to the C-terminus of the peptide.
Overall, the claim coverage centers on using the specific peptide sequence GNGVPNLRGDLQVLGQRVGRT (SEQ ID NO.: 1) as a PEGylated construct with covalently attached N- and C-terminus PEG moieties, implemented in Formula I for therapeutic administration to subjects with αvβ6 integrin-related cancer and in Formula II for imaging a tumor, cancerous lesion, or cancer cell.
Stated Advantages
Supports αvβ6-targeted PET imaging and radionuclide therapy outcomes as documented in vitro, in vivo, and clinical evidence.
Supports albumin-binding benefits for the PEGylated conjugates.
Provides quantitative targeting and pharmacokinetic/biodistribution performance metrics such as serum stability and albumin binding, including biodistribution values (%ID/g), tumor uptake, blood circulation, and kidney elimination.
Provides first-in-human pilot study support for the diagnostic and therapeutic conjugates.
Documented Applications
Treating an αvβ6 integrin-related cancer by administering a therapeutic conjugate of Formula I to a subject.
Imaging a tumor, a cancerous lesion, or a cancer cell by administering a diagnostic conjugate comprising Formula II to a subject.
αvβ6 integrin-related cancer imaging and therapy using 68Ga PET/CT and 177Lu therapy within a first-in-human pilot study workflow.
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