In vivo enzyme inhibition improves the targeting of [177Lu]DOTA-GRP(13-27) in GRPR-positive tumors in mice

Cancer Biotherapy and Radiopharmaceuticals

Volumn 29, Issue 9, 2014, Pages 359-367

  Marsouvanidis, Panteleimon J ^a,b   Melis, Marleen ^b   De Blois, Erik ^b   Breeman, Wout A P ^b   Krenning, Eric P ^b   Maina, Theodosia ^a   Nock, Berthold A ^a   De Jong, Marion ^b  

^a INSTITUTE OF NANOSCIENCE AND NANOTECHNOLOGY   (Greece)

^b ERASMUS MEDICAL CENTER   (Netherlands)

Author keywords

Enzyme inhibition; In vivo stability; Lysine; Neutral endopeptidase; Phosphoramidon; Radiolabeled gastrin releasing peptide; Radionuclide therapy; Renal retention

Indexed keywords

DOTA GASTRIN RELEASING PEPTIDE (13-27) LUTETIUM LU 177; GASTRIN RELEASING PEPTIDE DERIVATIVE; GASTRIN RELEASING PEPTIDE RECEPTOR; LYSINE; MEMBRANE METALLOENDOPEPTIDASE; PHOSPHORAMIDON; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; BOMBESIN RECEPTOR; GASTRIN RELEASING PEPTIDE; GLYCOPEPTIDE; LUTETIUM; PEPTIDE FRAGMENT; PROTEINASE INHIBITOR; RADIOISOTOPE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; CONTROLLED STUDY; DRUG DOSE ESCALATION; DRUG STABILITY; DRUG TARGETING; DRUG UPTAKE; ENZYME DEGRADATION; ENZYME INHIBITION; EX VIVO STUDY; HUMAN; HUMAN CELL; IN VIVO STUDY; ISOTOPE LABELING; MALE; MOUSE; NMRI NUDE MOUSE; NONHUMAN; PROSTATE CANCER; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOSYNTHESIS; CHEMISTRY; DIAGNOSTIC USE; ENZYMOLOGY; METABOLISM; NUDE MOUSE; PROSTATE TUMOR; SCINTISCANNING; TISSUE DISTRIBUTION; TUMOR CELL LINE; XENOGRAFT;

ANIMALS; CELL LINE, TUMOR; GASTRIN-RELEASING PEPTIDE; GLYCOPEPTIDES; HETEROGRAFTS; HUMANS; LUTETIUM; MALE; MICE; MICE, NUDE; NEPRILYSIN; PEPTIDE FRAGMENTS; PROSTATIC NEOPLASMS; PROTEASE INHIBITORS; RADIOISOTOPES; RADIOPHARMACEUTICALS; RECEPTORS, BOMBESIN; TISSUE DISTRIBUTION;

EID: 84912074092     PISSN: 10849785     EISSN: 15578852     Source Type: Journal    
DOI: 10.1089/cbr.2014.1706     Document Type: Article

References (47)

1. Reubi JC. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr Rev 2003;24:389.
2. Fani M, Maecke HR. Radiopharmaceutical development of radiolabelled peptides. Eur J Nucl Med Mol Imaging 2012;39 Suppl 1:S11.
3. 3]-octreotide: The Rotterdam experience with more than 1000 patients. Eur J Nucl Med 1993;20:716.
4. Ginj M, Schmitt JS, Chen J, et al. Design, synthesis, and biological evaluation of somatostatin-based radiopeptides. Chem Biol 2006;13:1081.
5. Kwekkeboom DJ, Mueller-Brand J, Paganelli G, et al. Overview of results of peptide receptor radionuclide therapy with 3 radiolabeled somatostatin analogs. J Nucl Med 2005;46 Suppl 1:62S-66S.
6. Kwekkeboom DJ, de Herber WW, Kam BL, et al. Treatment with the radiolabeled somatostatin analog [177Lu- DOTA0,Tyr3]octreotate: Toxicity, efficacy and survival. J Clin Oncol 2008;26:2124.
7. Giovacchini G, Nicolas G, Forrer F. Peptide receptor radionuclide therapy with somatostatin analogues in neuroendocrine tumors. Anticancer Agents Med Chem 2012;12:526.
8. Gugger M, Reubi JC. Gastrin-releasing peptide receptors in non-neoplastic and neoplastic human breast. Am J Pathol 1999;155:2067.
9. Markwalder R, Reubi JC. Gastrin-releasing peptide receptors in the human prostate: Relation to neoplastic transformation. Cancer Res 1999;59:1152.
10. Sancho V, Di Florio A, Moody TW. Bombesin receptor-mediated imaging and cytotoxicity: Review and current status. Curr Drug Deliv 2011;8:79.
11. De Visser M, Bernard HF, Erion JL, et al. Novel 111In-labeled bombesin analogues for molecular imaging of prostate tumours. Eur J Nucl Med Mol Imaging 2007;34:1228.
12. Ananias HJ, de Jong IJ, Dierckx RA, et al. Nuclear imaging of prostate cancer with gastrin-releasing-peptide-receptor targeted radiopharmaceuticals. Curr Pharm Des 2008;14:3033.
13. Zhang H, Abiraj K, Thorek DL, et al. Evolution of bombesin conjugates for targeted PET imaging of tumors. PLoS One 2012;7:e44046.
14. 2 GRP receptor-targeted radiotherapy and chemotherapy in PC-3 human prostate tumor cell xenografted SCID mice. Cancer Biother Radiopharm 2006;21:155.
15. 177Lu-labeled GRP-R agonist for systemic radiotherapy of prostate cancer. J Nucl Med 2006;47:1144.
16. Zhang H, Schuhmacher J, Waser B, et al. DOTA-PESIN, a DOTA-conjugated bombesin derivative designed for the imaging and targeted radionuclide treatment of bombesin receptor-positive tumours. Eur J Nucl Med Mol Imaging 2007;34:1198.
17. Linder KE, Metcalfe E, Arunachalam T, et al. In vitro and in vivo metabolism of Lu-AMBA, a GRP-receptor binding compound, and the synthesis and characterization of its metabolites. Bioconjug Chem 2009;20:1171.
18. Marsouvanidis PJ, Maina T, Sallegger W, et al. Tumor diagnosis with new (111)In-radioligands based on truncated human gastrin releasing peptide sequences: Synthesis and preclinical comparison. J Med Chem 2013;56:8579.
19. 99mTc radiotracers based on human GRP(18-27): Synthesis and comparative evaluation. J Nucl Med 2013;54:1797.
20. Bunnett NW, Kobayashi R, Orloff MS, et al. Catabolism of gastrin releasing peptide and substance P by gastric membrane-bound peptidases. Peptides 1985;6:277.
21. Erdös EG, Skidgel RA. Neutral endopeptidase 24.11 (enkephalinase) and related regulators of peptide hormones. FASEB J 1989;3:145.
22. Shipp MA, Tarr GE, Chen CY, et al. CD10/neutral endopeptidase 24.11 hydrolyzes bombesin-like peptides and regulates the growth of small cell carcinomas of the lung. Proc Natl Acad Sci U S A 1991;88:10662.
23. Suda H, Aoyagi T, Takeuchi T, et al. Letter: A thermolysin inhibitor produced by Actinomycetes: Phosphoramidon. J Antibiot (Tokyo) 1973;26:621.
24. Komiyama T, Aoyagi T, Takeuchi T, et al. Inhibitory effects of phosphoramidon on neutral metalloendopeptidases and its application on affinity chromatography. Biochem Biophys Res Commun 1975;65:352.
25. Roques BP, Noble F, Dauqe V, et al. Neutral endopeptidase 24.11: Structure, inhibition, and experimental and clinical pharmacology. Pharmacol Rev 1993;45:87.
26. Nowak W, Errasti AE, Armesto AR, et al. Endothelial angiotensin-converting enzyme and neutral endopeptidase in isolated human umbilical vein: An effective bradykinin inactivation pathway. Eur J Pharmacol 2011;667:271.
27. Nock BA, Maina T, Krenning EP, et al. "To serve and protect": Enzyme inhibitors as radiopeptide escorts promote tumor targeting. J Nucl Med 2014;55:121.
28. Gotthardt M, van Eerd-Vismale J, Oyen WJ, et al. Indication for different mechanisms of kidney uptake of radiolabeled peptides. J Nucl Med 2007;48:596.
29. Moestrup SK, Cui S, Vorum H, et al. Evidence that epithelial glycoprotein 330/megalin mediates uptake of polybasic drugs. J Clin Invest 1995;96:1404.
30. Orlando RA, Exner M, Czekay RP, et al. Identification of the second cluster of ligand-binding repeats in megalin as a site for receptor-ligand interactions. Proc Natl Acad Sci U S A 1997;94:2368.
31. 111In-DTPA-octreotide. J Nucl Med 2005;46:1696.
32. Vegt E, Melis M, Eek A, et al. Renal uptake of different radiopeptides is mediated by megalin: SPECT and biodistribution studies in megalin-deficient mice. Eur J Nucl Med Mol Imaging 2011;38:623.
33. Behe M, Kluge G, Becker W, et al. Use of polyglutamic acids to reduce uptake of radiometal-labeled minigastrin in the kidneys. J Nucl Med 2005;46:1012.
34. Vegt E, Wetzels JF, Russel FG, et al. Renal uptake of radiolabeled octreotide in human subjects is efficiently inhibited by succinylated gelatin. J Nucl Med 2006;47:432.
35. Vegt E, van Eerd JE, Eek A, et al. Reducing renal uptake of radiolabeled peptides using albumin fragments. J Nucl Med 2008;49:1506.
36. Vegt E, de Jong M, Wetzels JF, et al. Renal toxicity of radiolabeled peptides and antibody fragments: Mechanisms, impact on radionuclide therapy, and strategies for prevention. J Nucl Med 2010;51:1049.
37. 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. Eur J Nucl Med Mol Imaging 2003;30:9-15.
38. 90Y-DOTATOC in association with amino acid infusion: A phase I study. Eur J Nucl Med Mol Imaging 2003;30:207.
39. Schroeder RPJ, de Blois E, de Ridder CMA, et al. Improving radiopeptides pharmacokinetics by adjusting experimental conditions for bombesin receptor-mediated imaging of prostate cancer. Q J Nucl Med Mol Imaging 2012;56:468.
40. 68Ga generator and aspects of radiolabelling DOTA-peptides. Appl Radiat Isot 2011;69:308.
41. Tokita K, Katsuno T, Hocart SJ, et al. Molecular basis for selectivity of high affinity peptide antagonists for the gastrinreleasing peptide receptor. J Biol Chem 2001;276:36652.
42. Uehara H, Gonzalez N, Sancho V, et al. Pharmacology and selectivity of various natural and synthetic bombesin related peptide agonists for human and rat bombesin receptors differs. Peptides 2011;32:1685.
43. Azay J, Nagain C, Llinares M, et al. Comparative study of in vitro and in vivo activities of bombesin pseudopeptide analogs modified on the C-terminal dipeptide fragment. Peptides 1998;19:57.
44. 99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging. Eur J Nucl Med Mol Imaging 2003;30:247.
45. De Visser M, Verwijnen SM, de Jong M. Update: Improvement strategies for peptide receptor scintigraphy and radionuclide therapy. Cancer Biother Radiopharm 2008;23:137.
46. Schroeder RP, De Blois E, De Ridder CM, et al. Improving radiopeptide pharmacokinetics by adjusting experimental conditions for bombesin receptor-targeted imaging of prostate cancer. Q J Nucl Med Mol Imaging 2012;56:468.
47. Breeman WAP, Kwekkeboom DJ, Kooij PM, et al. Effect of dose and specific activity on tissue distribution of Indium-111-pentetreotide in rats. J Nucl Med 1995;36:623.