DOTATOC: A powerful new tool for receptor-mediated radionuclide therapy

Otte, Andreas; Jermann, Eduard; Béhé, Martin; Goetze, M; Bucher, Heiner C.; Roser, H.W.; Heppeler, A.; Müeller-Brand, Jan; Maecke, Helmut R.

doi:10.1007/bf00879669

Cited by 101 publications

(89 citation statements)

References 3 publications

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“…These findings suggest that the GRP receptor can be used as a molecular basis for diagnosing and treating prostate tumours with, for example, GRP receptor-targeted scintigraphy, radionuclide therapy and cytotoxic therapy [14,22]. It has been proposed that GRP receptor-expressing tumours can be visualised and treated using radiolabelled BN analogues in a manner similar to what has been found for somatostatin receptor-expressing tumours, which have been successfully imaged and treated using radiolabelled somatostatin analogues [23][24][25].…”

mentioning

confidence: 89%

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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Purpose It has been shown that some primary human tumours and their metastases, including prostate and breast tumours, overexpress gastrin-releasing peptide (GRP) (5-14)), was tested in vivo in biodistribution studies using rats bearing GRP receptor-expressing CA20948 tumours, and nude mice bearing human PC3 xenografts. Injection of 111In-labelled Cmp 3 in these animals showed high, receptor-mediated uptake in receptor-positive organs and tumours which could be visualised using planar gamma camera and microSPECT/CT imaging. Conclusion With their enhanced receptor affinity and their rapid receptor-mediated internalisation in vitro and in vivo, the new BN analogues, and especially Cmp 3, are promising candidates for use in diagnostic molecular imaging and targeted radionuclide therapy of GRP receptor-expressing cancers.

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mentioning

confidence: 89%

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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“…Several studies using 90 111 In-DTPA-octreotide. The kidney-to-tumor ratio was 1.9 times lower for 90 Y/ 111 In-DOTATOC than for 111 In-DTPA-octreotide (43). One year later, the same group reported results for 10 patients.…”

Section: Prrt Of Nets With Somatostatin-based Analogsmentioning

confidence: 49%

Radiopeptide Imaging and Therapy in Europe

Ambrosini¹,

Fani²,

Fanti³

et al. 2011

J Nucl Med

183

116

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Receptor targeting with radiolabeled peptides has become an important topic, particularly in nuclear oncology. Strong research efforts are under way in radiopharmaceutical science laboratories and in nuclear medicine departments in Europe. The target receptors belong to the large family of G-proteincoupled receptors. The prototypes of these radiopeptides are based on analogs of somatostatin targeting somatostatin receptor-positive tumors, particularly well-differentiated neuroendocrine tumors. These radiopeptides have an important impact not only on diagnosis but also on targeted radionuclide therapy of these tumors. Besides the registered radiopeptide 111 In-pentetreotide, efficient SPECT tracers labeled with 99m Tc and PET agents based on generator-produced 68 Ga have been developed and used in the clinic. In parallel to the development of diagnostic agents, radiopeptides labeled with the b 2 emitters 90 Y and 177 Lu are also widely used. Because the same chelators and therefore the same conjugates can be used in diagnosis and therapy, they constitute ideal theranostic pairs. This progress is driven not only by scientists and clinicians but also by patient interest groups. New radiopeptides targeting other G-protein-coupled receptors are entering the clinic, among them glucagon-like peptide 1 receptor-targeting molecules. This receptor is overexpressed on literally all benign insulinomas. 111 In-labeled derivatives of the insulinotropic 39-mer peptide exendin-4 were beneficial in the pre-and perioperative localization of these benign lesions. In contrast, lack of localization may indicate malignant insulinoma. The bombesin-and gastrin-releasing peptide receptor family is potentially important because these receptors are overexpressed on major human tumors such as prostate tumors, breast tumors, gastrointestinal stromal tumors, and vessels of ovarian cancer. 99m Tc-labeled peptides for SPECT and 68 Ga-, as well as 64 Cu-labeled agonists or antagonists, have been studied in breast tumors, prostate tumors, gastrointestinal stromal tumors, and gliomas with considerable success. A phase I therapeutic study with a 177 Lu-labeled agonist has been completed. There are not enough clinical data available to reveal the significance of these new modalities in patient care, but several phase I studies are under way in larger patient cohorts using PET agents. Another G-protein-coupled receptor with high overexpression on human tumors is the gastrin/ cholecystokinin-2 receptor. It is overexpressed in more than 90% of cases of medullary thyroid cancer, in small cell lung cancer, and in a subgroup of neuroendocrine tumors. Correlating with in vitro receptor localization using autoradiography of 27 patients with metastasized medullary thyroid cancer, SPECT or planar imaging of these patients resulted in a 95% sensitivity of tumor localization. Finally, another G-protein-coupled receptor is found in brain tumors and peritumoral vessels. Literally all cases of glioblastoma multiforme overexpress the neurokinin type 1 receptor; th...

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“…In the late 1990s and early 2000s, "early adopters" of PRRT were successfully using 90 Y coupled to various somatostatin analogs (13,(24)(25)(26)(27) The primary observed disadvantage of 90 Y PRRT was renal toxicity. 90 Y PRRT resulted in renal failure in patients when performed without kidney protection, although some renal toxicity was still observed even with the administration of amino acids for kidney protection (30)(31)(32).…”

Section: Y Prrt Continues To Thrivementioning

confidence: 99%

“…2) (11), it became clear that other radionuclides might be better suited for the regimen than 111 In because its short tissue range resulted in relatively modest tumor shrinkage (based on anatomic imaging with CT/MRI). In addition, DOTA-chelated peptides, which could be more easily labeled with radioactive metals, also started becoming available (12)(13)(14).…”

Section: Next Steps For Prrtmentioning

confidence: 99%

Clinical History of the Theranostic Radionuclide Approach to Neuroendocrine Tumors and Other Types of Cancer: Historical Review Based on an Interview of Eric P. Krenning by Rachel Levine

Levine

Krenning

2017

J Nucl Med

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In nuclear medicine, the term theranostics describes the combination of therapy and diagnostic imaging. In practice, this concept dates back more than 50 years; however, among the most successful examples of theranostics are peptide receptor scintigraphy and peptide receptor radionuclide therapy of neuroendocrine tumors. The development of these modalities through the radiolabeling of somatostatin analogs with various radionuclides has led to a revolution in patient management and established a foundation for expansion of the theranostic principle into other oncology indications. This article provides a review of the evolution and development of the theranostic radionuclide approach to the management of neuroendocrine tumors, as described by the inventor of this technique, Eric P. Krenning, in an interview with Rachel Levine.

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DOTATOC: A powerful new tool for receptor-mediated radionuclide therapy

Cited by 101 publications

References 3 publications

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Radiopeptide Imaging and Therapy in Europe

Clinical History of the Theranostic Radionuclide Approach to Neuroendocrine Tumors and Other Types of Cancer: Historical Review Based on an Interview of Eric P. Krenning by Rachel Levine

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