Best Practice & Research Clinical Endocrinology & Metabolism
Volume 21, Issue 1 , Pages 111-129 , March 2007

Peptide receptor radionuclide therapy

  • Flavio Forrer, MD (PhD-Student)

      Affiliations

    • Corresponding Author InformationCorresponding author. Tel.: +31 10 463 48 89; Fax: +31 10 463 59 97.

References 

  1. Reubi JC. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocrine Reviews. 2003;24(4):389–427
  2. Reubi JC, Waser B, Schaer JC, Laissue JA. Somatostatin receptor sst1-sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands. European Journal of Nuclear Medicine. 2001;28:836–846
  3. Reubi JC, Waser B, Liu Q, et al. Subcellular distribution of somatostatin sst2A receptors in human tumors of the nervous and neuroendocrine systems: membranous versus intracellular location. The Journal of Clinical Endocrinology and Metabolism. 2000;85:3882–3891
  4. Krenning EP, Kwekkeboom DJ, Bakker WH, et al. Somatostatin receptor scintigraphy with [111In-DTPA-d-Phe1]- and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients. European Journal of Nuclear Medicine. 1993;20:716–731
  5. Kwekkeboom DJ, Krenning EP, de Jong M. Peptide receptor imaging and therapy. Journal of Nuclear Medicine. 2000;41:1704–1713
  6. Hofmann M, Maecke H, Borner R, et al. Biokinetics and imaging with the somatostatin receptor PET radioligand (68)Ga-DOTATOC: preliminary data. European Journal of Nuclear Medicine. 2001;28:1751–1757
  7. Maecke HR, Hofmann M, Haberkorn U. (68)Ga-labeled peptides in tumor imaging. J Nucl Med. 2005;46(supplement 1):172S–178S
  8. Wester HJ, Schottelius M, Scheidhauer K, et al. PET imaging of somatostatin receptors: design, synthesis and preclinical evaluation of a novel 18F-labelled, carbohydrated analogue of octreotide. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30:117–122
  9. Valkema R, De Jong M, Bakker WH, et al. Phase I study of peptide receptor radionuclide therapy with [In-DTPA]octreotide: the Rotterdam experience. Seminars in Nuclear Medicine. 2002;32:110–122
  10. McCarthy KE, Woltering EA, Anthony LB. In situ radiotherapy with 111In-pentetreotid. State of the art and perspectives. The Quarterly Journal of Nuclear Medicine. 2000;44:88–95
  11. Anthony LB, Woltering EA, Espenan GD, et al. Indium-111-pentetreotide prolongs survival in gastroenteropancreatic malignancies. Seminars in Nuclear Medicine. 2002;32:123–132
  12. Buscombe JR, Caplin ME, Hilson AJ. Long-term efficacy of high-activity 111In-pentetreotide therapy in patients with disseminated neuroendocrine tumors. Journal of Nuclear Medicine. 2003;44:1–6
  13. Otte A, Herrmann R, Heppeler A, et al. Yttrium-90 DOTATOC: first clinical results. European Journal of Nuclear Medicine. 1999;26:1439–1447
  14. Waldherr C, Pless M, Maecke HR, et al. The clinical value of [90Y-DOTA]-dPhe1-Tyr3-octreotide (90Y-DOTATOC) in the treatment of neuroendocrine tumours: a clinical phase II study. Annals of Oncology. 2001;12:941–945
  15. Waldherr C, Pless M, Maecke HR, et al. Tumor response and clinical benefit in neuroendocrine tumors after 7.4 GBq (90)Y-DOTATOC. Journal of Nuclear Medicine. 2002;43:610–616
  16. Forrer F, Waldherr C, Maecke HR, Mueller-Brand J. Targeted radionuclide therapy with 90Y-DOTATOC in patients with neuroendocrine tumors. Anticancer Research. 2006;26:703–707
  17. Bodei L, Cremonesi M, Zoboli S, et al. Receptor-mediated radionuclide therapy with 90Y-DOTATOC in association with amino acid infusion: a phase I study. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30:207–216
  18. Virgolini I, Britton K, Buscombe J, et al. In- and Y-DOTA-lanreotide: results and implications of the MAURITIUS trial. Seminars in Nuclear Medicine. 2002;32:148–155
  19. Baum RP, Söldner J, Schmücking M, Niesen A. Peptidrezeptorvermittelte Radiotherapie (PRRT) neuroendokriner Tumoren Klinischen Indikationen und Erfahrung mit 90Yttrium-markierten Somatostatinanaloga. Der Onkologe. 2004;10:1098–1110
  20. Kwekkeboom DJ, Bakker WH, Kam BL, et al. Treatment of patients with gastro-entero-pancreatic (GEP) tumours with the novel radiolabelled somatostatin analogue [(177)Lu-DOTA(0),Tyr(3)]octreotate. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30:417–422
  21. Kwekkeboom DJ, Bakker WH, Teunissen JJ, et al. Treatment with Lu-177-DOTA-Tyr3-octreotate in patients with neuroendocrine tumors: interim results. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30(supplement 2):S231;(abstract)
  22. Kwekkeboom DJ, Teunissen JJ, Bakker WH, et al. Radiolabelled somatostatin analog [177Lu-DOTAO,Tyr3]octreotate in patients with endocrine gastro entero pancreatic tumors. Journal of Clinical Oncology. 2005;23:2754–2762
  23. Forrer F, Uusijarvi H, Storch D, et al. Treatment with 177Lu-DOTATOC of patients with relapse of neuroendocrine tumors after treatment with 90Y-DOTATOC. Journal of Nuclear Medicine. 2005;46:1310–1316
  24. Krenning EP, Kooij PP, Bakker WH, et al. Radiotherapy with a radiolabeled somatostatin analogue, [111In-DTPA-d-Phe1]-octreotide. A case history. Annals of the New York Academy of Sciences. 1994;733:496–506
  25. Konijnenberg MW, Bijster M, Krenning EP, De Jong M. A stylized computational model of the rat for organ dosimetry in support of preclinical evaluations of peptide receptor radionuclide therapy with (90)Y, (111)In, or (177)Lu. Journal of Nuclear Medicine. 2004;45:1260–1269
  26. Scarpignato C, Pelosini I. Somatostatin analogs for cancer treatment and diagnosis: an overview. Chemotherapy. 2001;47(supplement 2):1–29
  27. Lamberts SW, van der Lely AJ, de Herder WW, Hofland LJ. Octreotide. The New England Journal of Medicine. 1996;334:246–254
  28. Reubi JC, Schaer JC, Laissue JA, Waser B. Somatostatin receptors and their subtypes in human tumors and in peritumoral vessels. Metabolism. 1996;45(supplement 1):39–41
  29. Reubi JC, Schar JC, Waser B, et al. Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use. European Journal of Nuclear Medicine. 2000;27:273–282
  30. Bruno JF, Berelowitz M. Somatostatin receptors: orphan that found family and function. Molecular and Cellular Neurosciences. 1993;4:307–309(abstract)
  31. Yamada Y, Kagimoto S, Kubota A, et al. Cloning, functional expression and pharmacological characterization of a fourth (hSSTR4) and a fifth (hSSTR5) human somatostatin receptor subtype. Biochemical and Biophysical Research Communications. 1993;195:844–852
  32. Oberg K, Eriksson B. Endocrine tumours of the pancreas. Best Practice and Research. Clinical Gastroenterology. 2005;19:753–781
  33. Slooter GD, Breeman WA, Marquet RL, et al. Anti-proliferative effect of radiolabelled octreotide in a metastases model in rat liver. International Journal of Cancer. 1999;81:767–771
  34. Mardirossian G, Wu C, Hnatowich DJ. The stability in liver homogenates of indium-111 and yttrium-90 attached to antibody via two popular chelators. Nuclear Medicine and Biology. 1993;20:65–74
  35. Liu S. The role of coordination chemistry in the development of target-specific radiopharmaceuticals. Chemical Society Reviews. 2004;33:445–461
  36. Otte A, Jermann E, Behe M, et al. DOTATOC: a powerful new tool for receptor-mediated radionuclide therapy. European Journal of Nuclear Medicine. 1997;24:792–795
  37. Chinol M, Bodei L, Cremonesi M, Paganelli G. Receptor-mediated radiotherapy with Y-DOTA-DPhe-Tyr-octreotide: the experience of the European Institute of Oncology Group. Seminars in Nuclear Medicine. 2002;32:141–147
  38. Paganelli G, Bodei L, Handkiewicz Junak D, et al. 90Y-DOTA-d-Phe1-Try3-octreotide in therapy of neuroendocrine malignancies. Biopolymers. 2002;66:393–398
  39. Paganelli G, Zoboli S, Cremonesi M, et al. Receptor-mediated radiotherapy with 90Y-DOTA-d-Phe1-Tyr3-octreotide. European Journal of Nuclear Medicine. 2001;28:426–434
  40. Bodei L, Cremonesi M, Grana C, et al. Receptor radionuclide therapy with (90)Y-[DOTA](0)-Tyr(3)-octreotide ((90)Y-DOTATOC) in neuroendocrine tumours. European Journal of Nuclear Medicine and Molecular Imaging. 2004;31:1038–1046
  41. Valkema R, Pauwels S, Kvols L, et al. Long-term follow-up of a phase 1 study of peptide receptor radionuclide therapy (PRRT) with (90Y-DOTA0,Tyr3)octreotide in patients with somatostatin receptor positive tumours. European Journal of Nuclear Medicine. 2003;30(supplement 2):232;(abstract)
  42. de Jong M, Valkema R, Jamar F, et al. Somatostatin receptor-targeted radionuclide therapy of tumors: preclinical and clinical findings. Seminars in Nuclear Medicine. 2002;32:133–140
  43. Smith MC, Liu J, Chen T, et al. OctreoTher: ongoing early clinical development of a somatostatin-receptor-targeted radionuclide antineoplastic therapy. Digestion. 2000;62(supplement 1):69–72
  44. Baum RP, Soldner J, Schmucking M, Niesen A. Intravenous and intra-arterial peptide receptor radionuclide therapy (PRRT) using Y-90-DOTA-Tyr3-octreotate (Y-90-DOTA-TATE) in patients with metastatic neuroendocrine tumors. European Journal of Nuclear Medicine. 2004;31(supplement 2):S238;(abstract)
  45. Valkema R, Pauwels S, Kvols LK, et al. Survival and response after peptide receptor radionuclide therapy with [90Y-DOTA0,Tyr3]octreotide in patients with advanced gastroenteropancreatic neuroendocrine tumors. Seminars in Nuclear Medicine. 2006;36:147–156
  46. Oberg K, Norheim I, Lundqvist G, et al. Cytotoxic treatment in patients with malignant carcinoid tumors. Response to streptozocin – alone or in combination with 5–FU. Acta Oncologica (Stockholm, Sweden). 1987;26:429–432
  47. Engstrom PF, Lavin PT, Moertel CG. Streptozocin plus fluorouracil versus doxorubicin therapy for metastatic carcinoid tumor. Journal of Clinical Oncology. 1984;2:1255–1259
  48. Moertel CG, Hanley JA. Combination chemotherapy trials in metastatic crcinoid tumor and the malignant carcinoid syndrome. Cancer Clinical Trials. 1979;2:327–334
  49. Cremonesi M, Ferrari M, Zoboli S, et al. Biokinetics and dosimetry in patients administered with (111)In-DOTA-Tyr(3)-octreotide: implications for internal radiotherapy with (90)Y-DOTATOC. European Journal of Nuclear Medicine. 1999;26:877–886
  50. Forrer F, Uusijarvi H, Waldherr C, et al. A comparison of 111In-DOTATOC and 111In-DOTATATE: biodistribution and dosimetry in the same patients with metastatic neuroendocrine tumours. European Journal of Nuclear Medicine and Molecular Imaging. 2004;31:1257–1262
  51. De Jong M, Valkema R, Van Gameren A, et al. Inhomogeneous localization of radioactivity in the human kidney after injection of [(111)In-DTPA]octreotide. Journal of Nuclear Medicine. 2004;45:1168–1171
  52. de Jong M, Barone R, Krenning E, et al. Megalin is essential for renal proximal tubule reabsorption of (111)In-DTPA-octreotide. Journal of Nuclear Medicine. 2005;46:1696–1700
  53. Behr TM, Sharkey RM, Sgouros G, et al. Overcoming the nephrotoxicity of radiometal-labeled immunoconjugates: improved cancer therapy administered to a nude mouse model in relation to the internal radiation dosimetry. Cancer. 1997;80(12 supplement):2591–2610
  54. Rolleman EJ, Valkema R, de Jong M, et al. Safe and effective inhibition of renal uptake of radiolabelled octreotide by a combination of lysine and arginine. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30:9–15
  55. van Eerd JE, Vegt E, Wetzels JF, et al. Gelatin-based plasma expander effectively reduces renal uptake of 111In-octreotide in mice and rats. Journal of Nuclear Medicine. 2006;47:528–533
  56. Vegt E, Wetzels JF, Russel FG, et al. Renal uptake of radiolabeled octreotide in human subjects is efficiently inhibited by succinylated gelatin. Journal of Nuclear Medicine. 2006;47:432–436
  57. Forrer F, Rolleman E, Valkema R, et al. Amifostine is most promising in protecting renal function during radionuclide therapy with [Lu-177-DOTA0,Tyr3]octreotate. Journal of Nuclear Medicine. 2006;47(supplement 1):43;(abstract)
  58. Rolleman EJ, Forrer F Bernard B, Bijster M, et al. Amifostine protects rat kidneys in peptide receptor radionuclide therapy with [177Lu-DOTA0,Tyr3]octreotate. European Journal of Nuclear Medicine and Molecular Imaging 2006 Dec 5 [Epub ahead of print].
  59. Moll S, Nickeleit V, Mueller-Brand J, et al. A new cause of renal thrombotic microangiopathy: yttrium 90-DOTATOC internal radiotherapy. American Journal of Kidney Diseases. 2001;37:847–851
  60. Cybulla M, Weiner SM, Otte A. End-stage renal disease after treatment with 90Y-DOTATOC. European Journal of Nuclear Medicine. 2001;28:1552–1554
  61. Stoffel MP, Pollok M, Fries J, Baldamus CA. Radiation nephropathy after radiotherapy in metastatic medullary thyroid carcinoma. Nephrology, Dialysis, Transplantation. 2001;16:1082–1083
  62. Barone R, Borson-Chazot F, Valkema R, et al. Patient-specific dosimetry in predicting renal toxicity with 90Y-DOTATOC: relevance of kidney volume and dose rate in finding a dose–effect relationship. Journal of Nuclear Medicine. 2005;46:99S–106S
  63. Otte A, Mueller-Brand J, Dellas S, et al. Yttrium-90-labelled somatostatin-analogue for cancer treatment. Lancet. 1998;351:417–418
  64. Emami B, Lyman J, Brown A, et al. Tolerance of normal tissue to therapeutic irradiation. International Journal of Radiation Oncology, Biology, Physics. 1991;21:109–122
  65. Valkema R, Pauwels SA, Kvols LK, et al. Long-term follow-up of renal function after peptide receptor radiation therapy with 90Y-DOTA0,Tyr3-octreotide and 177Lu-DOTA0,Tyr3-octreotate. Journal of Nuclear Medicine. 2005;46(supplement 1):83S–91S
  66. Pauwels S, Barone R, Walrand S, et al. Practical dosimetry of peptide receptor radionuclide therapy with (90)Y-labeled somatostatin analogs. Journal of Nuclear Medicine. 2005;46(supplement 1):92S–98S
  67. Bushnell D, Menda Y, Madsen M, et al. Assessment of hepatic toxicity from treatment with 90Y-SMT 487 (OctreoTher(TM)) in patients with diffuse somatostatin receptor positive liver metastases. Cancer Biotherapy and Radiopharmaceuticals. 2003;18:581–588
  68. Raut C, Kulke M, Glickman J, et al. Carcinoid tumors. Current Problems in Surgery. 2006;43:383–450
  69. Berber E, Flesher N, Siperstein AE. Laparoscopic radiofrequency ablation of neuroendocrine liver metastases. World Journal of Surgery. 2002;26:985–990
  70. Hellman P, Ladjevardi S, Skogseid B, et al. Radiofrequency tissue ablation using cooled tip for liver metastases of endocrine tumors. World Journal of Surgery. 2002;26:1052–1056
  71. Modlin IM, Latich I, Kidd M, et al. Therapeutic options for gastrointestinal carcinoids. Clinical Gastroenterology and Hepatology. 2006;4:526–547
  72. Krenning EP, de Jong M, Kooij PP, et al. Radiolabelled somatostatin analogue(s) for peptide receptor scintigraphy and radionuclide therapy. Annals of Oncology. 1999;10(supplement 2):S23–S29
  73. Toth-Fejel S, Pommier RF. Relationships among delay of diagnosis, extent of disease, and survival in patients with abdominal carcinoid tumors. American Journal of Surgery. 2004;187:575–579
  74. Teunissen JJ, Kwekkeboom DJ, Krenning EP. Quality of life in patients with gastroenteropancreatic tumors treated with [177Lu-DOTA0,Tyr3]octreotate. Journal of Clinical Oncology. 2004;22:2724–2729
  75. Ginj M, Chen J, Walter MA, et al. Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy. Clinical Cancer Research. 2005;11:1136–1145
  76. Breeman WA, De Jong M, Visser TJ, et al. Optimising conditions for radiolabelling of DOTA-peptides with 90Y, 111In and 177Lu at high specific activities. European Journal of Nuclear Medicine and Molecular Imaging. 2003;30:917–920
  77. Froidevaux S, Hintermann E, Torok M, et al. Differential regulation of somatostatin receptor type 2 (sst 2) expression in AR4-2J tumor cells implanted into mice during octreotide treatment. Cancer Research. 1999;59:3652–3657
  78. de Jong M, Breeman WAP, Valkema R, et al. Combination Radionuclide Therapy Using 177Lu- and 90Y-Labeled Somatostatin Analogs. Journal of Nuclear Medicine. 2005;46(supplement 1):13S–17S
  79. Uusijarvi H, Bernhardt P, Rosch F, et al. Electron- and positron-emitting radiolanthanides for therapy: aspects of dosimetry and production. Journal of Nuclear Medicine. 2006;47:807–814
  80. Norenberg JP, Krenning BJ, Konings IR, et al. 213Bi-[DOTA0,Tyr3]octreotide peptide receptor radionuclide therapy of pancreatic tumors in a preclinical animal model. Clinical Cancer Research. 2006;12:897–903
  81. van Putten JW, Price A, van der Leest AH, et al. A phase I study of gemcitabine with concurrent radiotherapy in stage III, locally advanced non-small cell lung cancer. Clinical Cancer Research. 2003;9:2472–2477
  82. Joiner MC, Marples B, Lambin P, et al. Low-dose hypersensitivity: current status and possible mechanisms. International Journal of Radiation Oncology, Biology, Physics. 2001;49:379–389
  83. Collis SJ, Schwaninger JM, Ntambi AJ, et al. Evasion of early cellular response mechanisms following low level radiation-induced DNA damage. The Journal of Biological Chemistry. 2004;279:49624–49632
  84. Reubi JC, Macke HR, Krenning EP. Candidates for peptide receptor radiotherapy today and in the future. Journal of Nuclear Medicine. 2005;46(supplement 1):67S–75S
  85. Smith CJ, Volkert WA, Hoffman TJ. Gastrin releasing peptide (GRP) receptor targeted radiopharmaceuticals: a concise update. Nuclear Medicine and Biology. 2003;30:861–868
  86. Behe M, Behr TM. Cholecystokinin-B (CCK-B)/gastrin receptor targeting peptides for staging and therapy of medullary thyroid cancer and other CCK-B receptor expressing malignancies. Biopolymers. 2002;66:399–418

PII: S1521-690X(07)00008-5

doi: 10.1016/j.beem.2007.01.007

Best Practice & Research Clinical Endocrinology & Metabolism
Volume 21, Issue 1 , Pages 111-129 , March 2007