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Integrin α v β 3 is a molecular marker for the estimation of tumor angiogenesis and is an imaging target for radiolabeled Arg-Gly-Asp (RGD) peptides. In this study, the authors investigated the clinical efficacy and safety of a novel radiolabeled RGD peptide, 99m Tc-IDA-D-[c(RGDfK)] 2 , for the imaging of integrin α v β 3 expression, as a measure of tumor angiogenesis in lung cancers and brain tumors. Five patients with lung cancers and seven with brain tumors underwent 99m Tc-IDA-D-[c(RGDfK)] 2 single-photon emission computed tomography (SPECT) imaging. Tumors were also assessed using 18 F-fluorodeoxyglucose positron emission tomography/computed tomography. Uptake of the radiotracer was expressed as the tumor-to-normal uptake ratio (TNR). All the lung cancers and brain tumors were well visualized on 99m Tc-IDA-D-[c(RGDfK)] 2 SPECT. TNR for 99m Tc-IDA-D-[c(RGDfK)] 2 was significantly higher than that for 18 F-FDG in brain tumors (6.4 ± 4.1 vs. 0.9 ± 0.4). Proliferation index of brain tumors showed a significant positive correlation with TNR for 99m Tc-IDA-D-[c(RGDfK)] 2 and 18 F-FDG. No laboratory and clinical adverse events were reported after 99m Tc-IDA-D-[c(RGDfK)] 2 injection. Their results suggest that 99m Tc-IDA-D-[c(RGDfK)] 2 is an efficacious and safe radiotracer for imaging integrin α v β 3 expression with potential application to monitoring the clinical efficacy of antiangiogenic agents in malignant tumors. In addition, this is the first clinical application of radiolabeled RGD peptides for SPECT imaging of brain tumors.

cancer biotherapy and radiopharmaceuticals

Imaging of Integrin αvβ3 Expression in Lung Cancers and Brain Tumors Using Single-Photon Emission Computed Tomography with a Novel Radiotracer 99mTc-IDA-D-[c(RGDfK)]2