Influence of biological assay conditions on stability assessment of radiometal-labelled peptides exemplified using a 177Lu-DOTA-minigastrin derivative

Nuclear Medicine and Biology

Volumn 38, Issue 2, 2011, Pages 171-179

  Ocak, Meltem ^a,b   Helbok, Anna ^a   von Guggenberg, Elisabeth ^a   Ozsoy, Y ^b   Kabasakal, Levent ^b   Kremser, Leopold ^a   Decristoforo, Clemens ^a  

^a INNSBRUCK MEDICAL UNIVERSITY   (Austria)

^b ISTANBUL UNIVERSITY   (Turkey)

Author keywords

In vitro stability; In vivo stability; Radiometabolites; Radiopeptides

Indexed keywords

LUTETIUM 1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID HISTIDYLHISTIDYLGLUTAMYLALANYLTYROSYLGLYCYLTRYPTOPHANYLNORLEUCYLASPARTYLPHENYLALANINAMIDE LU 177; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BIOASSAY; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DEGRADATION; DRUG STABILITY; DRUG URINE LEVEL; FEMALE; HUMAN; IN VITRO STUDY; INTERMETHOD COMPARISON; ISOTOPE LABELING; MATRIX ASSISTED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; METABOLITE; MOUSE; NONHUMAN; PROTEIN CLEAVAGE; RAT; REVERSED PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; TISSUE HOMOGENATE; URINALYSIS;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; BIOLOGICAL ASSAY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CHROMATOGRAPHY, REVERSE-PHASE; FEMALE; GASTRINS; HETEROCYCLIC COMPOUNDS, 1-RING; HUMANS; ISOTOPE LABELING; LUTETIUM; MICE; MICE, INBRED BALB C; PEPTIDE HYDROLASES; PROTEIN STABILITY; RADIOISOTOPES; RATS; SPECTROMETRY, MASS, MATRIX-ASSISTED LASER DESORPTION-IONIZATION; TISSUE EXTRACTS;

EID: 79551680701     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2010.07.009     Document Type: Article

References (30)

1. Breeman W.A., Kwekkeboom D.J., de Blois E., de Jong M., Visser T.J., Krenning E.P. Radiolabelled regulatory peptides for imaging and therapy. Anticancer Agents Med Chem 2007, 7(3):345-357.
2. Reubi J.C., Maecke H.R. Peptide-based probes for cancer imaging. J Nucl Med 2008, 49(11):1735-1738.
3. Aloj L., Morelli G. Design, synthesis and preclinical evaluation of radiolabeled peptides for diagnosis and therapy. Curr Pharm Des 2004, 10(24):3009-3031.
4. Gotthardt M., Boermann O.C., Behr T.M., Behe M.P., Oyen W.J. Development and clinical application of peptide-based radiopharmaceuticals. Curr Pharm Des 2004, 10(24):2951-2963.
5. de Jong M., Verwijnen S.M., de Visser M., Kwekkeboom D.J., Valkema R., Krenning E.P. Peptides for radionuclide therapy. Targeted Radionuclide Tumor Therapy, Biological Aspects. Springer 2008, 117-144. T. Stigbrand, J. Carlsson, G.P. Adams (Eds.).
6. 177Lu for radioimmunotherapeutic applications. Nucl Med Biol 2002, 29(4):431-442.
7. 90Y from cyclic and acyclic ligand-antibody conjugated. Nucl Med Biol 1991, 18:469-476.
8. Liu S., Edwards D.S. Bifunctional chelators for therapeutic lanthanide radiopharmaceuticals. Bioconjug Chem 2001, 12:7-34.
9. Good S., Walter M.A., Waser B., Wang X., Müller-Brand J., Behe M.P., et al. Macrocyclic chelator-coupled gastrin based radiopharmaceuticals for targeting of gastrin receptor-expressing tumours. Eur J Nucl Med Mol Imaging 2008, 35(10):1868-1877.
10. Werle M., Bernkop-Schnürch A. Strategies to improve plasma half life time of peptide and protein drugs. Amino Acids 2006, 30(4):351-367.
11. Adessi C., Soto C. Converting a peptide into a drug: strategies to improve stability and bioavailability. Curr Med Chem 2002, 9(9):963-978.
12. Garcia-Garayoa E., Allemann-Tannahil L., Blaeuenstein P., Willmann M., Carrel-Rémy N., Tourwé D., et al. In vitro and in vivo evaluation of new radiolabelled neurotensin (8-13) analogues with high affinity for NT1 receptors. Nucl Med Biol 2001, 28(1):75-84.
13. 99mTc-labeled anti-VEGF peptide targeting neuropilin-1. Nucl Med Biol 2004, 31(5):575-581.
14. Behr T.M., Jenner N., Behe M., Angerstein C., Gratz S., Raue F., et al. Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors. J Nucl Med 1999, 40(6):1029-1044.
15. 99mTc-labeling and in vitro and in vivo evaluation of HYNIC-and (Nalpha-His)acetic acid-modified[D-Glu1]-minigastrin. Bioconjug Chem 2004, 15(4):864-871.
16. 99mTc-labelled HYNIC-minigastrin with reduced kidney uptake for targeting of CCK-2 receptor-positive tumours. Eur J Nucl Med Mol Imaging 2007, 34(8):1209-1218.
17. von Guggenberg E., Sallegger W., Helbok A., Ocak M., King R., Mather S.J., et al. Cyclic minigastrin analogues for gastrin receptor scintigraphy with technetium-99m: preclinical evaluation. J Med Chem 2009, 52(15):4786-4793.
18. Behr T.M., Jenner N., Radetzky S., Béhe M., Gratz S., Yücekent S., et al. Targeting of cholecystokinin-B/gastrin receptors in vivo: preclinical and initial clinical evaluation of diagnostic and therapeutic potential of radiolabelled gastrin. Eur J Nucl Med 1998, 25(4):424-430.
19. 111In-labeled nonsulfated CCK8 analog: a peptide for CCK-B receptor-targeted scintigraphy and radionuclide therapy. J Nucl Med 1999, 40(12):2081-2087.
20. 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging. J Nucl Med 2004, 45(3):485-494.
21. Nock B.A., Maina T., Béhé M., Nikolopoulou A., Gotthardt M., Schmitt J.S., et al. CCK-2/gastrin receptor targeting tumor imaging with (99m)Tc-labelled minigastrin analogs. J Nucl Med 2005, 46(10):1727-1736.
22. Mather S.J., McKenzie A.J., Sosabowski J.K., Morris T.M., Ellison D., Watson S.A. Selection of radiolabelled gastrin analogs for peptide receptor-targeted radionuclide therapy. J Nucl Med 2007, 48(4):615-622.
23. Roosenburg S., Laverman P., Joosten L., Eek A., Oyen W.J., de Jong M., et al. Stabilized (111)In-labeled sCCK8 analogues for targeting CCK2-receptor positive tumors: synthesis and evaluation. Bioconjug Chem 2010 Apr, 21(4):663-670.
24. Breeman W.A., Fröberg A.C., de Blois E., van Gameren A., Melis M., de Jong M., et al. Optimised labelling, preclinical and initial clinical aspects of CCK-2 receptor-targeting with 3 radiolabeled peptides. Nucl Med Biol 2008, 35(8):839-849.
25. Kwekkeboom D.J., Bakker W.H., Kooij P.P., Erion J., Srinivasan A., de Jong M., et al. Cholecystokinin receptor imaging using an octapeptide DTPA-CCK analogue in patients with medullary thyroid carcinoma. Eur J Nucl Med 2000, 27(9):1312-1317.
26. Behe M., Behr T.M. 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.
27. 99mTc-labeled small peptides as diagnostic radiopharmaceuticals. Chem Rev 1999, 99(9):2235-2268.
28. Smith-Jones P.M., Stolz B., Bruns C., Albert R., Reist H.W., Fridrich R., et al. Gallium-67/gallium-68-[DFO]-octreotide - a potential radiopharmaceutical for PET imaging of somatostatin receptor-positive tumors: synthesis and radiolabeling in vitro and preliminary in vivo studies. J Nucl Med 1994, 35:317-325.
29. Mather S. Preclinical development of therapeutic radiopharmaceuticals. IAEA Technical Reports Series No.458, Comparative evaluation of therapeutic radiopharmaceuticals 2007, 257-265.
30. Decristoforo C., Mather S.J. 99m-Technetium-labelled peptide-HYNIC conjugates: effects of lipophilicity and stability on biodistribution. Nucl Med Biol 1999, 26:389-396.