Diagnostic · In Clinical Trials
RGD Peptide Tracers
No lawful US pathway
01 · Overview
RGD peptide tracers are short synthetic peptides containing the arginine-glycine-aspartic acid sequence, which binds integrin receptors, in particular alphavbeta3, coupled to positron- or gamma-emitting radionuclides. Alphavbeta3 integrin is upregulated on angiogenic endothelium and on some tumor cells, so these tracers are studied for imaging tumor angiogenesis and, more recently, cardiovascular disease.
Cyclic and multimeric RGD constructs have been developed to improve binding affinity and tumor retention. The fluorine-18 labeled tracer fluciclatide binds both alphavbeta3 and alphavbeta5 integrins (PMID 26383153).
02 · Research summary & key findings
In 11 patients with head and neck squamous cell carcinoma, fluorine-18 galacto-RGD PET identified 10 of 12 tumors with good contrast, missing two lesions under 5 mm, and immunohistochemistry confirmed alphavbeta3 expression chiefly on tumor microvessels (PMID 18006761). A multicenter test-retest study in 39 patients with solid tumors found fluorine-18 fluciclatide uptake reproducible between sessions, an important step toward its use as a response biomarker but not a demonstration of clinical benefit (PMID 26383153). No RGD tracer has achieved FDA approval, and current trials listed on ClinicalTrials.gov are largely exploratory or combine RGD with other targeting motifs such as somatostatin or FAP ligands.
03 · Regulatory status
RGD Peptide Tracers is currently undergoing clinical trials. It is not yet FDA-approved and is available only through clinical research settings or investigational protocols.
No lawful pathway today
RGD Peptide Tracers 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.
See the 2 FDA-approved compounds in Diagnostic
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04 · Administration routes
- Intravenous
References
- [1][18F]galacto-RGD positron emission tomography for imaging of alphavbeta3 expression on the neovasculature in patients with squamous cell carcinoma of the head and neck Clin Cancer Res, 2007. PMID 18006761
- [2]Multicenter Reproducibility of 18F-Fluciclatide PET Imaging in Subjects with Solid Tumors J Nucl Med, 2015. PMID 26383153
Primary literature
- PubMed: "RGD Peptide Tracers"
Peer-reviewed literature indexed by the National Library of Medicine.
- ClinicalTrials.gov: "RGD Peptide Tracers"
Registered interventional and observational studies, including status and phase.
- PubChem: "RGD Peptide Tracers"
Chemical structure, molecular properties, and bioactivity data.
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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol. See our editorial policy for how this content is produced and reviewed. Clinicians: join the network.