Diagnostic · Research Phase
Gadopentetate Peptide Conjugates
No lawful US pathway
01 · Overview
Gadopentetate peptide conjugates are experimental agents in which a gadolinium chelate is chemically linked to a targeting peptide so that MRI contrast is concentrated at tissues expressing a chosen receptor. Gadopentetate dimeglumine itself is an approved non-targeted MRI contrast agent marketed as Magnevist, while the peptide-conjugated versions are laboratory constructs.
Targeting motifs explored in this area include RGD peptides, which bind integrins on angiogenic vessels and tumor cells, and somatostatin analogues. Most published conjugates use macrocyclic chelators such as Gd-DOTA rather than the gadopentetate DTPA chelate.
02 · Research summary & key findings
Preclinical studies have shown that Gd-DOTA conjugates of cyclic RGD peptides bind integrin receptors with higher affinity than reference cyclic RGD peptides and show high relaxivity and serum stability, with tumor targeting evaluated in cells and in mice (PMID 25449282). This is animal and cell-based evidence only. No gadolinium-peptide conjugate has reached clinical use, and as of a 2022 review there is no FDA-approved targeted contrast agent for magnetic resonance molecular imaging of cancer, in large part because MRI lacks the sensitivity to detect the low concentrations of most molecular targets (PMID 36121350). Development attention has shifted toward higher-relaxivity and nanoparticle platforms.
03 · Regulatory status
Gadopentetate Peptide Conjugates is in the research phase with limited clinical data in humans. Current evidence is primarily derived from preclinical (animal or in vitro) studies.
No lawful pathway today
Gadopentetate Peptide Conjugates is not FDA-approved and does not currently have a lawful prescription or compounding pathway in the United States, so we do not sell it and will not book a consultation for it. That can change: in 2026 FDA began reviewing several peptides for compounding.
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04 · Administration routes
- Intravenous
References
- [1]Improved tumor-targeting MRI contrast agents: Gd(DOTA) conjugates of a cycloalkane-based RGD peptide Biochem Biophys Res Commun, 2014. PMID 25449282
- [2]Targeted Contrast Agents for Magnetic Resonance Molecular Imaging of Cancer Acc Chem Res, 2022. PMID 36121350
Primary literature
- PubMed: "Gadopentetate Peptide Conjugates"
Peer-reviewed literature indexed by the National Library of Medicine.
- ClinicalTrials.gov: "Gadopentetate Peptide Conjugates"
Registered interventional and observational studies, including status and phase.
- PubChem: "Gadopentetate Peptide Conjugates"
Chemical structure, molecular properties, and bioactivity data.
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