Peptide PET/SPECT probes specific to oncoproteins in tumor extracellular matrix
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Publication Number
US-12576168-B2
Publication Date
2026-03-17
Expiration Date
Abstract
A PET/SPECT probe includes the following formula: P-L-C wherein P is a EDB-FN targeting peptide, C is a PET/SPECT contrast agent; and L is an optional linker that covalently links the peptide to the contrast agent.
Core Innovation
A PET/SPECT probe is described with a P-L-C construct in which P is a peptide that binds to extradomain-B fibronectin (EDB-FN) or extradomain-A fibronectin (EDA-FN) and includes an amino acid sequence selected from SEQ ID NO: 1-9, SEQ ID NO: 19-24, or retro-inverso amino acid sequences thereof. C is a PET/SPECT contrast agent, and L is an optional linker covalently linking the peptide to the PET/SPECT contrast agent.
The contrast agent is a metal chelating agent comprising at least one selected from DTPA, DOTA, DO3A, EDTA, TRITA, TETA, DOTMA, DO3MA, DOTP, DOTMP, DOTPP, N,N′-ethylenedi-L-cysteine, and salts or esters thereof. The probe concept combines an EDB-FN/EDA-FN binding peptide sequence set with a metal chelator class for use as a PET/SPECT contrast agent in the P-L-C formula.
The disclosed probe is positioned for detecting cancer cells by contacting tissue with the PET/SPECT probe and detecting a location and/or distribution of cancer cells in the tissue. The partial document further states example probe formulations such as ZD2-DA-(64Cu-DOTA) and ZD2-(68Ga-NOTA)/ZD2-(68Ga-HBED-CC), together with reported expression specificity to EDB-FN and PET imaging contrast differences between aggressive versus less aggressive tumors.
Claims Coverage
The partial content provides two independent claims, covering a structural PET/SPECT probe defined by a P-L-C formula and a method of detecting cancer cells in tissue by contacting with that PET/SPECT probe and detecting the probe’s location/distribution. Across the independent claims, the inventive features focus on EDB-FN/EDA-FN binding peptide sequence selection, the P-L-C construct with an optional covalent linker, and the PET/SPECT contrast agent being a metal chelating agent comprising specified chelators.
PET/SPECT probe defined by P-L-C targeting EDB-FN or EDA-FN with a metal chelating contrast agent
A PET/SPECT probe comprising P-L-C, wherein P is a peptide that binds to extradomain-B fibronectin (EDB-FN) or extradomain-A fibronectin (EDA-FN) and includes an amino acid sequence selected from SEQ ID NO: 1-9 and SEQ ID NO: 19-24, and retro-inverso amino acid sequences thereof; C is a PET/SPECT contrast agent; and L is an optional linker that covalently links the peptide to the PET/SPECT contrast agent; wherein the contrast agent is a metal chelating agent comprising at least one of DTPA, DOTA, DO3A, EDTA, TRITA, TETA, DOTMA, DO3MA, DOTP, DOTMP, DOTPP, N,N′-ethylenedi-L-cysteine, and salts or esters thereof.
Detecting cancer cells by contacting tissue with the EDB-FN/EDA-FN PET/SPECT probe and detecting probe distribution
A method of detecting cancer cells in tissue of a subject comprising contacting the tissue with a PET/SPECT probe defined by P-L-C, wherein P binds to extradomain-B fibronectin (EDB-FN) or extradomain-A fibronectin (EDA-FN) and includes an amino acid sequence selected from SEQ ID NO: 1-9 and SEQ ID NO: 19-24, and retro-inverso amino acid sequences thereof; C is a PET/SPECT contrast agent; and L is an optional linker covalently linking the peptide to the PET/SPECT contrast agent; wherein the contrast agent is a metal chelating agent comprising at least one of DTPA, DOTA, DO3A, EDTA, TRITA, TETA, DOTMA, DO3MA, DOTP, DOTMP, DOTPP, N,N′-ethylenedi-L-cysteine, and salts or esters thereof; and detecting a location and/or distribution of cancer cells in the tissue by detecting the PET/SPECT probe in the tissue of the subject.
Across the independent claims, the coverage centers on a PET/SPECT probe defined by a P-L-C construct that targets EDB-FN or EDA-FN using peptide sequences selected from listed SEQ ID NOs and retro-inverso sequences, optionally linked covalently via L, and coupled to a metal chelating agent PET/SPECT contrast agent selected from specified chelators and salts/esters. The method claim applies the same probe definition to contacting tissue and detecting the probe’s location and/or distribution to detect cancer cells.
Stated Advantages
Enables cancer detection/risk stratification and assessment of therapeutic efficacy.
Supports potential intra-operative surgical margin guidance.
Documented Applications
Systemic in vivo cancer imaging using the described PET/SPECT peptide probe.
Cancer detection and risk stratification, including aggressiveness/malignancy.
Assessment of therapeutic efficacy.
Potential intra-operative surgical margin guidance.
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