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Current Radiopharmaceuticals

Author(s): Fateme Badipa, Behrouz Alirezapour and Hassan Yousefnia*

DOI: 10.2174/1874471016666221207122731

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An Overview of Radiolabeled RGD Peptides for Theranostic Applications

Page: [107 - 122] Pages: 16

  • * (Excluding Mailing and Handling)

Abstract

Angiogenesis phenomenon, as a highly affecting factor on the growth and spread of cancer cells, depends on specific molecular interactions between components of the extracellular matrix and vascular cells. αv integrin acts as a cell adhesive molecule involved in tumor invasion and angiogenesis. Among the various combinations of integrin subunits expressed on the surface of cells, αvβ3 integrin has a particularly interesting expression pattern during angiogenesis. The αvβ3 integrin is a vital receptor affecting tumor growth, tumor invasiveness, metastasis, and angiogenesis overexpressed on various human tumors, leading to the development of different theranostics probes and radiopharmaceuticals. The αvβ3 integrin can recognize several extracellular matrix molecules in the base of the RGD adhesive sequence. This review provides an overview of the status, trends and future of the most studied αvβ3 integrin-binding ligand, RGD tripeptides, labeled with various radioisotopes. An overview of the pre-clinical models for radiolabeled RGD peptides and clinical aspects of the RGD- based radiopharmaceuticals is provided with some new considerations and ways forward.

Graphical Abstract

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Dual SSTR2 and Integrin αvβ3 Targeting PET/CT Imaging. ClinicalTrials. gov Identifier: NCT02817945. Available from: https://ClinicalTrials.gov/show/NCT02817945
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Multimodal Imaging Assessment of the Inflammatory Atheromatous Plaque. ClinicalTrials.gov Identifier: NCT01608516. Available from: https://ClinicalTrials.gov/show/NCT01608516
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A Study of 99mTc-3PRGD2 Injection in Healthy Volunteers. ClinicalTrials. gov Identifier: NCT03974685. Available from: https://ClinicalTrials.gov/show/NCT03974685
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A Study of 99mTc-3PRGD2 Injection in Lung Cancer Patient. ClinicalTrials.gov Identifier: NCT04233476. Available from: https://ClinicalTrials.gov/show/NCT04233476
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Virus DNX2401 and Temozolomide in Recurrent Glioblastoma(D24GBM). ClinicalTrials.gov Identifier: NCT01956734. Available from: https://ClinicalTrials.gov/show/NCT01956734
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Safety Study of a Genetically Modified Adenovirus in Ovarian Cancer Patients (Ad5Delta24RGD). ClinicalTrials.gov Identifier: NCT00562003. Available from: https://ClinicalTrials.gov/show/NCT00562003
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A Study of an Infectivity Enhanced Suicide Gene Expressing Adenovirus for Ovarian Cancer in Patients With Recurrent Ovarian and Other Selected Gynecologic Cancers. ClinicalTrials.gov Identifier: NCT00964756. Available from:https://ClinicalTrials.gov/show/NCT00964756
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Study of the Angiogenesis by PET/CT in Patients With Lymphoma (RGDLymphome). ClinicalTrials.gov Identifier: NCT02490891. Available from:https://ClinicalTrials.gov/show/NCT02490891
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TRACER [F-18] RDG-K5 Carotid Plaque Imaging Study (K5- C200). ClinicalTrials.gov Identifier: NCT03364270. Available from: https://ClinicalTrials.gov/show/NCT03364270
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The Use of 18F-ALF-NOTA-PRGD2 PET/CT Scan to Predict the Efficacy and Adverse Events of Apatinib in Malignancies. ClinicalTrials. gov Identifier: NCT03384511. Available from: https://ClinicalTrials.gov/show/NCT03384511
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68Ga-AlfatideII for the Differential Diagnosis of of Lung Cancer and Lung Tuberculosis by PET/CT. ClinicalTrials.gov Identifier: NCT02481726. Available from: https://ClinicalTrials.gov/show/NCT02481726
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PET/CT Imaging of Angiogenesis in Lung or Head and Neck Cancers Prior or During Chemotherapy With Antiangiogenic Agents (MLAPOCHI). ClinicalTrials.gov Identifier: NCT02325349. Available from: https://ClinicalTrials.gov/show/NCT02325349
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Combination Adenovirus + Pembrolizumab to Trigger Immune Virus Effects (CAPTIVE). ClinicalTrials.gov Identifier: NCT02798406. Available from: https://ClinicalTrials.gov/show/NCT02798406
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DNX-2401 With Interferon Gamma (IFN-γ) for Recurrent Glioblastoma or Gliosarcoma Brain Tumors (TARGET-I). ClinicalTrials. gov Identifier: NCT02197169. Available from: https://ClinicalTrials.gov/show/NCT02197169
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Targeted PET/CT and PET/MRI Imaging of Vascular Inflammation. ClinicalTrials.gov Identifier: NCT02995642. Available from: https://ClinicalTrials.gov/show/NCT02995642