{"entity":{"id":"rgd-integrin-radioligands","kind":"technology","name":"RGD integrin radioligands","aka":["RGD peptides","radiolabelled RGD peptides","integrin alphavbeta3 PET","Galacto-RGD","RGD PET"],"tldr":"Small radioactive peptides that stick to a protein called integrin alpha-v beta-3, found on new blood vessels growing into tumours and on some cancer cells. On a PET scan they show where a tumour is building blood vessels.","summary":"The tripeptide motif arginine-glycine-aspartate (RGD) binds integrins, and cyclic RGD peptides are selective for integrin alphavbeta3, which is expressed on activated endothelium in tumour neovasculature and on some tumour cells. Haubner and colleagues (Technical University of Munich, PLoS Medicine 2005) showed with [18F]Galacto-RGD that PET can assess alphavbeta3 expression non-invasively in patients with cancer, with tumour uptake correlating with expression measured afterwards, and proposed it for planning and monitoring anti-angiogenic therapy. Later studies imaged the neovasculature of head and neck squamous cell carcinoma and of malignant glioma.\n\nSeveral RGD tracers have been studied in people, but none is approved, and therapeutic RGD radioconjugates have remained largely preclinical. Uptake reflects both vessels and tumour cells, which makes the signal hard to interpret.","status":"emerging","asOf":"2026-11-03","links":[{"label":"Haubner et al. 2005, PLoS Medicine: non-invasive visualisation of the activated alphavbeta3 integrin in cancer patients by PET and [18F]Galacto-RGD","url":"https://doi.org/10.1371/journal.pmed.0020070"},{"label":"Beer et al. 2007, Clinical Cancer Research: [18F]Galacto-RGD PET of alphavbeta3 on the neovasculature in head and neck squamous cell carcinoma","url":"https://doi.org/10.1158/1078-0432.CCR-07-0528"},{"label":"Schnell et al. 2009, Neuro-Oncology: imaging of integrin alphavbeta3 expression in malignant glioma by [18F]Galacto-RGD PET","url":"https://doi.org/10.1215/15228517-2009-024"}],"tags":[],"related":[],"cancers":["glioblastoma"],"sections":["radiopharma","imaging"],"technologies":["radioligand-therapy","antiangiogenic","fapi-pet"],"targets":["itgav","itgb3"],"drugs":[],"companies":[],"institutions":["tum-munich"],"pathways":[],"terms":["angiogenesis"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"principle":"A cyclic RGD peptide or peptidomimetic, labelled with 18F, 68Ga or 64Cu (or a therapeutic radiometal), binds integrin alphavbeta3 on angiogenic endothelium and tumour cells and is imaged by PET.","strengths":["Images angiogenesis rather than metabolism","Small peptide with fast clearance","Studied in patients across several cancers"],"limitations":["No approved product","Signal mixes vessel and tumour-cell binding","Therapeutic versions largely preclinical"],"since":2005},"route":"/technologies/rgd-integrin-radioligands/","neighbours":{"cancer":[{"id":"glioblastoma","kind":"cancer","name":"Glioma & glioblastoma","route":"/cancers/glioblastoma/"}],"section":[{"id":"imaging","kind":"section","name":"Imaging","route":"/fronts/imaging/"},{"id":"radiopharma","kind":"section","name":"Radiopharmaceuticals & Theranostics","route":"/fronts/radiopharma/"}],"technology":[{"id":"antiangiogenic","kind":"technology","name":"Anti-angiogenic therapy","route":"/technologies/antiangiogenic/"},{"id":"fapi-pet","kind":"technology","name":"FAPI PET","route":"/technologies/fapi-pet/"},{"id":"radioligand-therapy","kind":"technology","name":"Radioligand therapy (beta emitters)","route":"/technologies/radioligand-therapy/"}],"target":[{"id":"itgav","kind":"target","name":"ITGAV","route":"/targets/itgav/"},{"id":"itgb3","kind":"target","name":"ITGB3","route":"/targets/itgb3/"}],"institution":[{"id":"tum-munich","kind":"institution","name":"TUM Klinikum rechts der Isar / CCC München","route":"/institutions/tum-munich/"}],"term":[{"id":"angiogenesis","kind":"term","name":"Angiogenesis","route":"/terms/angiogenesis/"}]}}