In vivo biodistribution and pharmacokinetics of 18F-labelled Spiegelmers: A new class of oligonucleotidic radiopharmaceuticals

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 32, Issue 4, 2005, Pages 470-477

  Boisgard, Raphaël ^a   Kuhnast, Bertrand ^a   Vonhoff, Stefan ^b   Younes, Chéraz ^a   Hinnen, Françoise ^a   Verbavatz, Jean Marc ^a   Rousseau, Bernard ^a   Fürste, Jens Peter ^b,c   Wlotzka, Britta ^b   Dollé, Frédéric ^a   Klussmann, Sven ^b   Tavitian, Bertrand ^a  

^a DIF   (France)

^b NOXXON PHARMA AG   (Germany)

^c FREIE UNIVERSITÄT BERLIN   (Germany)

Author keywords

Aptamers; Fluorine 18; Mirror image oligonucleotides; Positron emission tomography; Spiegelmers

Indexed keywords

FLUORODEOXYGLUCOSE F 18; IODINE 125; OLIGONUCLEOTIDE; RADIOPHARMACEUTICAL AGENT; SELENIUM; SPIEGELMER; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG STABILITY; DRUG UPTAKE; EX VIVO STUDY; MALE; METABOLIC ACTIVATION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RAT; WHOLE BODY RADIATION;

ANIMALS; FLUORINE RADIOISOTOPES; IODINE RADIOISOTOPES; MALE; METABOLIC CLEARANCE RATE; OLIGONUCLEOTIDES; ORGAN SPECIFICITY; PAPIO; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; SPECIES SPECIFICITY; TISSUE DISTRIBUTION;

EID: 17844393983     PISSN: 16197070     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00259-004-1669-8     Document Type: Article

References (36)

1. Tuerk C, Gold L. Systematic evolution of ligands by exponential enrichment: RNA ligands to bacteriophage T4 DNA polymerase. Science 1990;249:505-10
2. Ellington AD, Szostak JW. In vitro selection of RNA molecules that bind specific ligands. Nature 1990;346:818-22
3. Brody EN, Gold L. Aptamers as therapeutic and diagnostic agents. J Biotechnol 2000;74:5-13
4. Tavitian B. In vivo imaging with oligonucleotides for diagnosis and drug development. Gut 2003;52:1-7
5. Ulrich H, Magdesian MH, Alves MJ, Colli W. In vitro selection of RNA aptamers that bind to cell adhesion receptors of Trypanosoma cruzi and inhibit cell invasion. J Biol Chem 2002;277:20756-62
6. Daniels DA, Chen H, Hicke BJ, Swiderek KM, Gold L. A tenascin-C aptamer identified by tumor cell SELEX: systematic evolution of ligands by exponential enrichment. Proc Natl Acad Sci USA 2003;100:15416-21
7. Hicke BJ, Stephens AW. Escort aptamers: a delivery service for diagnosis and therapy. J Clin Invest 2000;106:923-8
8. Blank M, Weinschenk T, Priemer M, Schluesener H. Systematic evolution of a DNA aptamer binding to rat brain tumor microvessels. Selective targeting of endothelial regulatory protein pigpen. J Biol Chem 2001;276:16464-8
9. Younes CK, Boisgard R, Tavitian B. Labelled oligonucleotides as radiopharmaceuticals: pitfalls, problems and perspectives. Curr Pharm Des 2002;8:1451-66
10. Cerchia L, Hamm J, Libri D, Tavitian B, de Franciscis V. Nucleic acid aptamers in cancer medicine. FEBS Lett 2002;528:12-6
11. Guhlke S, Famulok M, Biersack HJ. Aptamers: a novel class of radiopharmaceutical with diagnostic and therapeutic potential. Eur J Nucl Med Mol Imaging 2003;30:1441-3
12. Charlton J, Sennello J, Smith D. In vivo imaging of inflammation using an aptamer inhibitor of human neutrophil elastase. Chem Biol 1997;4:809-16
13. Klussmann S, Nolte A, Bald R, Erdmann VA, Furste JP. Mirror-image RNA that binds D-adenosine. Nat Biotechnol 1996;14:1112-5
14. Urata H, Ogura E, Shinohara K, Ueda Y, Akagi M. Synthesis and properties of mirror-image DNA. Nucleic Acids Res 1992;20:3325-32
15. Nolte A, Klussmann S, Bald R, Erdmann VA, Furste JP. Mirror-design of L-oligonucleotide ligands binding to L-arginine. Nat Biotechnol 1996;14:1116-9
16. Williams KP, Liu XH, Schumacher TN, Lin HY, Ausiello DA, Kim PS, et al. Bioactive and nuclease-resistant L-DNA ligand of vasopressin. Proc Natl Acad Sci U S A 1997;94:11285-90
17. Leva S, Lichte A, Burmeister J, Muhn P, Jahnke B, Fesser D, et al. GnRH binding RNA and DNA Spiegelmers: a novel approach toward GnRH antagonism. Chem Biol 2002;9:351-9
18. Vater A, Jarosch F, Buchner K, Klussmann S. Short bioactive Spiegelmers to migraine-associated calcitonin gene-related peptide rapidly identified by a novel approach: tailored-SELEX. Nucleic Acids Res 2003;31:e130
19. Purschke WG, Radtke F, Kleinjung F, Klussmann S. A DNA Spiegelmer to staphylococcal enterotoxin B. Nucleic Acids Res 2003;31:3027-32
20. Faulhammer D, Eschgfaller B, Stark S, Burgstaller P, Englberger W, Erfurth J, et al. Biostable aptamers with antagonistic properties to the neuropeptide nociceptin/orphanin FQ. RNA 2004;10:516-27
21. Wlotzka B, Leva S, Eschgfaller B, Burmeister J, Kleinjung F, Kaduk C, et al. In vivo properties of an anti-GnRH Spiegelmer: an example of an oligonucleotide-based therapeutic substance class. Proc Natl Acad Sci USA 2002;99:8898-902
22. Kuhnast B, Klussmann S, Hinnen F, Boisgard R. Rousseau B, Furste JP, et al. Fluorine-18- and iodine-125-labelling of spiegelmers. J Labelled Comp Radiopharm 2003;46:1205-19
23. Kuhnast B, Hinnen F, Boisgard R, Tavitian B, Dolle F. Fluorine-18 labelling of oligonucleotides: prosthetic labelling at the 5′-end using the N-(4-F-18 fluorobenzyl)-2-bromoacetamide reagent. J Labelled Comp Radiopharm 2003;46:1093-103
24. Agrawal S, Zhang X, Lu Z, Zhao H, Tamburin JM, Yan J, et al. Absorption, tissue distribution and in vivo stability in rats of a hybrid antisense oligonucleotide following oral administration. Biochem Pharmacol 1995;50:571-6
25. Wincott F, DiRenzo A, Shaffer C, Grimm S, Tracz D, Workman C, et al. Synthesis, deprotection, analysis and purification of RNA and ribozymes. Nucleic Acids Res 1995;23:2677-84
26. Tavitian B, Terrazzino S, Kuhnast B, Marzabal S, Stettler O, Dolle F, et al. In vivo imaging of oligonucleotides with positron emission tomography. Nat Med 1998;4:467-71
27. Aboagye EO, Price PM, Jones T. In vivo pharmacokinetics and pharmacodynamics in drug development using positron-emission tomography. Drug Discov Today 2001;6:293-302
28. Dolle F, Hinnen F, Vaufrey F, Tavitian B, Crouzel C. A general method for labeling oligodeoxynucleotides with F-18 for in vivo PET imaging. J Labelled Comp Radiopharm 1997;39:319-30
29. Kuhnast B, Dolle F, Terrazzino S, Rousseau B, Loc'h C, Vaufrey F, et al. General method to label antisense oligonucleotides with radioactive halogens for pharmacological and imaging studies. Bioconjug Chem 2000;11:627-36
30. Kuhnast B, Dolle F, Tavitian B. Fluorine-18 labeling of peptide nucleic acids. J Labelled Comp Radiopharm 2002;45:1-11
31. Agrawal S, Temsamani J, Tang JY. Pharmacokinetics, biodistribution, and stability of oligodeoxynucleotide phosphorothioates in mice. Proc Natl Acad Sci U S A 1991;88:7595-9
32. Hnatowich DJ, Mardirossian G, Fogarasi M, Sano T, Smith CL, Cantor CR, et al. Comparative properties of a technetium-99m-labeled single-stranded natural DNA and a phosphorothioate derivative in vitro and in mice. J Pharmacol Exp Ther 1996;276:326-34
33. Grindel JM, Musick TJ, Jiang Z, Roskey A, Agrawal S. Pharmacokinetics and metabolism of an oligodeoxynucleotide phosphorothioate (GEM91) in cynomolgus monkeys following intravenous infusion. Antisense Nucleic Acid Drug Dev 1998;8:43-52
34. Hermann T, Patel DJ. Adaptive recognition by nucleic acid aptamers. Science 2000;287:820-5
35. Tavitian B. In vivo antisense imaging. Q J Nucl Med 2000;44:236-55
36. Hnatowich DJ. Pharmacokinetic considerations in the development of oligomers as radiopharmaceuticals. Q J Nucl Med 1997;41:91-100