Abstract68 Ga-NODAGA-THERANOSTÔ is an a v b 3 integrin antagonist and the first radiolabeled peptidomimetic to reach clinical development for targeting integrin receptors. In this first-in-human study, the feasibility of integrin receptor peptidomimetic positron emission tomography/computed tomography (PET/CT) imaging was confirmed in patients with non-small-cell lung cancer and breast cancer. Ga-NODAGA-THERANOST revealed high tumor-to-background ratios (SUV max = 4.8) and uptake at neoangiogenesis sites. Reconstructed fused images distinguished cancers with high malignancy potential and enabled enhanced bone metastasis detection.18 F-FDG-positive lung and lymph node metastases did not show uptake, indicating the absence of neovascularization. Conclusions:68 Ga-NODAGA-THERANOST was found to be safe and effective, exhibiting in this study rapid blood clearance, stability, rapid renal excretion, favorable biodistribution and PK/PD, low irradiation burden (lSv/MBq/lg), and convenient radiolabeling. This radioligand might enable theranostics, that is, a combination of diagnostics followed by the appropriate therapeutics, namely antiangiogenic therapy, image-guided presurgical assessment, treatment response evaluation, prediction of pathologic response, neoadjuvantpeptidomimetic-radiochemotherapy, and personalized medicine strategies. Further clinical trials evaluating 68 Ga-NODAGA-THERANOST are warranted.