Treatment of advanced neuroendocrine tumours with radiolabelled somatostatin analogues

Kaltsas, Gregory; Papadogias, Dimitrios; Makras, Polyzois; Grossman, Ashley

doi:10.1677/erc.1.01116

Cited by 139 publications

(131 citation statements)

References 43 publications

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“…Imaging probes currently being developed for these receptors include somatostatin analogs, cholecystokinin/gastrin and GLP-1 analogs for neuroendocrine tumors, bombesin and neuropeptide-Y analogs for prostate or breast cancers, and Arg-Gly-Asp peptides for neoangiogenesis labeling (2,24). The first and most successful Food and Drug Administrationapproved peptide-based radiopharmaceutical is the somatostatin analog (25) 111 In-DTPA-octreotide ( 111 In-OctreoScan, 111 In-pentetreotide) (2,26,27). It is being used for imaging somatostatin receptor-positive lesions, such as neuroendocrine tumors, mammary cancer, and small cell lung cancer (25)(26)(27).…”

Section: Discussionmentioning

confidence: 99%

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

et al. 2016

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Cancer-specific targeting sparing normal tissues would significantly enhance cancer therapy outcomes and reduce cancer-related mortality. One approach is to target receptors or molecules that are specifically expressed on cancer cells. Peptides as cancer-specific targeting agents offer advantages such as ease of synthesis, low antigenicity, and enhanced diffusion into tissues. Glucose-regulated protein 78 (GRP78) is an endoplasmic reticulum stress chaperone that regulates the unfolded protein response and is overexpressed in various cancers. In this study, we evaluated GIRLRG peptide that specifically targets GRP78 for cancer-specific binding (in vitro) and noninvasive tumor imaging (in vivo). Methods: GIRLRG peptide was modeled into the GRP78 ATPase domain using computational modeling. Surface plasmon resonance studies were performed to determine the affinity of GIRLRG peptide to GRP78 protein. GIRLRG was conjugated with PEG to prolong its circulation in mice. Tumor binding efficacy of PEG-GIRLRG peptide was evaluated in nude mice bearing heterotopic cervical (HT3), esophageal (OE33), pancreatic (BXPC3), lung (A549), and glioma (D54) tumors. Nano-SPECT/CT imaging of the mice was performed 48 and 72 h after injection with 111 In-labeled PEG-GIRLRG or PEG-control peptide. Post-SPECT biodistribution studies were performed 96 h after injection of the radiolabeled peptides. Results: Using molecular modeling and surface plasmon resonance, we identified that GIRLRG was binding with an affinity constant of 2.16 · 10 −3 M in the ATPase domain of GRP78. GIRLRG peptide specifically bound to cervical, lung, esophageal, and glioma cells. SPECT imaging revealed that 111 In-PEG-GIRLRG specifically bound to cervical, esophageal, pancreatic, lung, and brain tumors. Post-SPECT biodistribution data also validated the SPECT imaging results. Conclusion: GIRLRG peptide specifically binds to the ATPase domain of GRP78. Radiolabeled PEG-GIRLRG could be used to target various cancers. Further studies would be required to translate PEG-GIRLRG peptide into the clinic.

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Section: Discussionmentioning

confidence: 99%

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

et al. 2016

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“…[18][19][20] In patients with high-grade metastatic NET there is often limited somatostatin receptor expression and systemic chemotherapy may be favored over radionuclide therapy. 21 It is speculated that as a prelude to therapy dual imaging with 18 F-FIGURE 1.…”

Section: Discussionmentioning

confidence: 99%

Functional imaging of neuroendocrine tumors with combined PET/CT using ⁶⁸Ga‐DOTATATE (DOTA‐DPhe¹,Tyr³‐octreotate) and ¹⁸F‐FDG

Kayani¹,

Bomanji²,

Groves³

et al. 2008

Cancer

433

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BACKGROUND. The aim was to assess the relevant distribution of the novel PET tracer 68Ga‐DOTATATE in neuroendocrine tumors (NETs) with combined positron emission tomography / computed tomography (PET/CT) and compare its performance with that of 18F‐FDG PET/CT. METHODS. The imaging findings with 68Ga‐DOTATATE and 18F‐FDG on 38 consecutive patients with a diagnosis of primary or recurrent NET were compared and correlated with tumor grade on histology based on ki67 and mitotic index. RESULTS. The sensitivity of 68Ga‐DOTATATE PET/CT was 82% (31 of 38) and that of 18F‐FDG PET/CT was 66% (25 of 38). The sensitivity of combined 68Ga‐DOTATATE and 18F‐FDG PET/CT was 92% (35 of 38). There was greater uptake of 68Ga‐DOTATATE than 18F‐FDG in low‐grade NET (median SUV 29 vs 2.9, P < .001). In high‐grade NET there was higher uptake of 18F‐FDG over 68Ga‐DOTATATE (median SUV 11.7 vs 4.4, P = .03). There was a significant correlation with predominant tumor uptake of 68Ga‐DOTATATE or 18F‐FDG and tumor grade on histology (P < .0001). CONCLUSIONS. 68Ga‐DOTATATE PET/CT is a useful novel imaging modality for NETs and is superior to 18F‐FDG for imaging well‐differentiated NET. Functional imaging with both 68Ga‐DOTATATE and 18F‐FDG has potential for a more comprehensive tumor assessment in intermediate‐ and high‐grade tumors. Cancer 2008. ©2008 American Cancer Society.

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“…A reduction in catecholamine secretion is seen in up to 45% of patients [146]. The radiolabeled somatostatin analogues 111 In-pentetreotide/ 111 In-DOTA-octreotide, 90 Y-DOTA-octreotide, 177 Lu-DOTA-octreotide, and 90 Y-DOTA-lanreotide have also been used with a similar tumor response in patients with tumors demonstrating uptake of the somatostatin radionuclide [147,148].…”

Section: Management Of Malignant Diseasementioning

confidence: 99%

Pheochromocytoma: Current Approaches and Future Directions

et al. 2008

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After completing this course, the reader should be able to:1. Use current practice methods in the diagnosis of pheochromocytomas.2. Employ current practice methods in the treatment of pheochromocytomas.3. Evaluate the current molecular research that contributes to the treatment of pheochromocytomas.This article is available for continuing medical education credit at CME.TheOncologist.com. CME CME ABSTRACTPheochromocytomas are rare catecholamine-secreting tumors that arise from chromaffin tissue within the adrenal medulla and extra-adrenal sites. Because of the excess secretion of hormones, these tumors often cause debilitating symptoms and a poor quality of life. While medical management plays a significant role in the treatment of pheochromocytoma patients, surgical excision remains the only cure. Improved medical management and surgical techniques and an increased understanding of hereditary disease have improved the outcome of pheochromocytoma patients with benign disease; however, the outcome of patients with malignant disease remains poor. In this review, we discuss the presentation, diagnosis, management, and future directions in the management of this disease. The Oncologist

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Treatment of advanced neuroendocrine tumours with radiolabelled somatostatin analogues

Cited by 139 publications

References 43 publications

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

Functional imaging of neuroendocrine tumors with combined PET/CT using ⁶⁸Ga‐DOTATATE (DOTA‐DPhe¹,Tyr³‐octreotate) and ¹⁸F‐FDG

Pheochromocytoma: Current Approaches and Future Directions

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Treatment of advanced neuroendocrine tumours with radiolabelled somatostatin analogues

Cited by 139 publications

References 43 publications

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers

Functional imaging of neuroendocrine tumors with combined PET/CT using 68Ga‐DOTATATE (DOTA‐DPhe1,Tyr3‐octreotate) and 18F‐FDG

Pheochromocytoma: Current Approaches and Future Directions

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Functional imaging of neuroendocrine tumors with combined PET/CT using ⁶⁸Ga‐DOTATATE (DOTA‐DPhe¹,Tyr³‐octreotate) and ¹⁸F‐FDG