Pharmacokinetic properties of peptidic radiopharmaceuticals: Reduced uptake of (EH)3-conjugates in important organs

Journal of Nuclear Medicine

Volumn 54, Issue 8, 2013, Pages 1327-1330

  Eder, Matthias ^a   Löhr, Thomas ^a   Bauder Wüst, Ulrike ^a   Reber, Markus ^a   Mier, Walter ^b   Schäfer, Martin ^a   Haberkorn, Uwe ^b   Eisenhut, Michael ^a  

^a GERMAN CANCER RESEARCH CENTER DKFZ   (Germany)

^b UNIVERSITY OF HEIDELBERG   (Germany)

Author keywords

68Ga; Peptides; Pharmacokinetic properties; Radiopharmaceuticals

Indexed keywords

DICHLOROMETHANE; GALLIUM 68; GLUTAMINE UREA LYSINE N,N' BIS [2 HYDROXY 5 (CARBOXYETHYL)BENZYL] ETHYLENEDIAMINE; OCTREOTATE 8 AMINO 3,6 DIOXAOCTANOIC ACID N,N' BIS [2 HYDROXY 5 (CARBOXYETHYL)BENZYL] ETHYLENEDIAMINE; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG;

ARTICLE; CANCER DIAGNOSIS; CELL CULTURE; CHEMICAL STRUCTURE; COMPLEX FORMATION; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG PURIFICATION; DRUG SCREENING; DRUG SYNTHESIS; DRUG UPTAKE; HUMAN; HUMAN CELL; IN VITRO STUDY; INTERNALIZATION; ISOTOPE LABELING; PRIORITY JOURNAL; REVERSED PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; SCINTISCANNING;

68GA; PEPTIDES; PHARMACOKINETIC PROPERTIES; RADIOPHARMACEUTICALS;

ANIMALS; ANTIGENS, SURFACE; CAPRYLATES; CELL LINE, TUMOR; FEMALE; GALLIUM RADIOISOTOPES; GLUTAMATE CARBOXYPEPTIDASE II; MALE; MICE; PEPTIDES; PEPTIDOMIMETICS; RADIOPHARMACEUTICALS; RECEPTORS, SOMATOSTATIN;

EID: 84881406607     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.112.114512     Document Type: Article

References (17)

1. Akizawa H, Arano Y, Uezono T, et al. Renal metabolism of 111In-DTPA-D-Phe1-octreotide in vivo. Bioconjug Chem. 1998;9:662-670.
2. Akizawa H, Uehara T, Arano Y. Renal uptake and metabolism of radiopharmaceuticals derived from peptides and proteins. Adv Drug Deliv Rev. 2008;60:1319-1328.
3. Béhé M, Kluge G, Becker W, Gotthardt M, Behr TM. Use of polyglutamic acids to reduce uptake of radiometal-labeled minigastrin in the kidneys. J Nucl Med. 2005;46:1012-1015.
4. Gotthardt M, van Eerd-Vismale J, Oyen WJ, et al. Indication for different mechanisms of kidney uptake of radiolabeled peptides. J Nucl Med. 2007;48:596-601.
5. 99mTc, 111In, and 125I. J Med Chem. 2011;54:3817-3826.
6. Klaassen CD, Aleksunes LM. Xenobiotic, bile acid, and cholesterol transporters: function and regulation. Pharmacol Rev. 2010;62:1-96.
7. Hicks RJ. Use of molecular targeted agents for the diagnosis, staging and therapy of neuroendocrine malignancy. Cancer Imaging. 2010;10 Spec no A:S83-S91.
8. Eder M, Schafer M, Bauder-Wust U, et al. 68Ga-complex lipophilicity and the targeting property of a urea-based PSMA inhibitor for PET imaging. Bioconjug Chem. 2012;23:688-697.
9. Afshar-Oromieh A, Haberkorn U, Eder M, Eisenhut M, Zechmann C. [68Ga]galliumlabelled PSMA ligand as superior PET tracer for the diagnosis of prostate cancer: comparison with 18F-FECH. Eur J Nucl Med Mol Imaging. 2012;39:1085-1086.
10. Banerjee SR, Pullambhatla M, Byun Y, et al. 68Ga-labeled inhibitors of prostatespecific membrane antigen (PSMA) for imaging prostate cancer. J Med Chem. 2010;53:5333-5341.
11. Schuhmacher J, Maier-BorstW. A new Ge-68/Ga-68 radioisotope generator system for production of Ga-68 in dilute HCl. Int J Appl Radiat Isot. 1981;32:31-36.
12. Eder M, Wangler B, Knackmuss S, et al. Tetrafluorophenolate of HBED-CC: a versatile conjugation agent for 68Ga-labeled small recombinant antibodies. Eur J Nucl Med Mol Imaging. 2008;35:1878-1886.
13. Schäfer M, Bauder-Wust U, Leotta K, et al. A dimerized urea-based inhibitor of the prostate-specific membrane antigen for 68Ga-PET imaging of prostate cancer. EJNMMI Res.. 2012;2:23.
14. Liu T, Toriyabe Y, Kazak M, Berkman CE. Pseudoirreversible inhibition of prostate-specific membrane antigen by phosphoramidate peptidomimetics. Biochemistry. 2008;47:12658-12660.
15. Bacich DJ, Pinto JT, Tong WP, Heston WD. Cloning, expression, genomic localization, and enzymatic activities of the mouse homolog of prostate-specific membrane antigen/NAALADase/folate hydrolase. Mamm Genome. 2001;12:117-123.
16. Foss CA, Mease RC, Fan H, et al. Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer. Clin Cancer Res. 2005;11:4022-4028.
17. 3 targeted radiotracers for tumor imaging. Mol Pharm. 2006;3:472-487.