Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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FIG. 10.18. EPC pattern of 90 Y sample. 10.4.4. Conclusion In these experiments, 90 Sr in equilibrium with 90 Y with a relatively low activity (~1.85 GBq) was used. The efficiency of the 90 Sr/ 90 Y generator was ~96% of the theoretical value. The initial results confirmed the efficiency of the 90 Sr/ 90 Y electrochemical generator and allowed development of the electrochemical separation technique as a quality control method for 90 Y. The next step will involve production of higher levels of activity from the 90 Sr/ 90 Y generator for labelling and supply of 90 Y to the national nuclear medicine community of Serbia. REFERENCES TO CHAPTER 10 [10.1] MAUSNER, L.F., SRIVASTAVA, S.C., Selection of radionuclides for radioimmunotherapy, Med. Phys. 20 (1993) 503. [10.2] BRANS, B., LINDEN, O., GIAMMARILE, F., TENNVALL, J., PUNT, C., Clinical application of newer radionuclide therapies, Eur. J. Cancer 42 (2006) 994. [10.3] INTERNATIONAL ATOMIC ENERGY AGENCY, Comparative Evaluation of Therapeutic Radiopharmaceuticals, Technical Reports Series No. 458, IAEA, Vienna (2007). [10.4] KOTHARI, K., et al., “Preparation of 186 Re complexes of dimercaptosuccinic acid and hydroxy ethylidine diphosphonate”, Modern Trends in Radiopharmaceuticals for Diagnosis and Therapy, IAEA-TECDOC-1029, IAEA, Vienna (1998) 539. 204
[10.5] DJOKIĆ, D.J., JANKOVIĆ, D.L., NIKOLIĆ, N.S., Labeling, characterization, and in vivo localization of a new Y-90-based phosphonate chelate 2,3-dicarboxypropane- 1,1-diphosphonic acid for the treatment of bone metastases: Comparison with Tc-99m-DPD complex, Bioorga. Med. Chem. 16 (2008) 4457. [10.6] DJOKIĆ, D., JANKOVIĆ, D., NIKOLIĆ, N., Preparation and in vivo evaluation of 90 Y-meso-dimercaptosuccinic acid ( 90 Y-DMSA) for possible therapeutic use: Comparison with 99m Tc-DMSA, Canc. Biother. Radiopharm. 24 (2009) 129. [10.7] JANKOVIĆ, D., et al., Particle sizes analysis: 90 Y and 99m Tc-labelled colloids, J. Microsc. 232 (2008) 601. [10.8] JANKOVIĆ, D.L., et al., 90 Y-labeled tin fluoride colloid as a promising therapeutic agent: Preparation, characterization, and biological study in rats, J. Pharm. Sci. 101 (2012) 2194. [10.9] ECKELMAN, W., KARESH, S., REBA, R., New compounds: Fatty acid and long chain hydrocarbon derivatives containing a strong chelating agent, J. Pharm. Sci. 64 (1975) 704. [10.10] OKARVI, S.M., Recent developments in 99m Tc-labelled peptide-based radiopharmaceuticals: An overview, Nucl. Med. Comm. 20 (1999) 1093. [10.11] KWEKKEBOOM, D.J., KRENNING, P.E., DE JONG, M., Peptide imaging and therapy, J. Nucl. Med. 41 (2000) 1704. [10.12] DE JONG, M., KRENNING, E., New advances in peptide receptor therapy, J. Nucl. Med. 43 (2002) 617. [10.13] BREEMAN, W.A.P., DE JONG, M., VISSER, T.J., ERION, J.L., KRENNING, E.P., Optimising conditions for radiolabelling of DOTA-peptides with 90 Y, 111 In and 177 Lu at high specific activities, Eur. J. Nucl. Med. Mol. Imaging 30 (2003) 917. [10.14] REISCHL, G., ROSCH, F., MACHULLA, H.J., Electrochemical separation and purification of yttrium-86, Radiochim. Acta 90 (2002) 225. [10.15] YOO, J., et al., Preparation of high specific activity 86Y using a small medical cyclotron, Nucl. Med. Biol. 32 (2005) 891. [10.16] INTERNATIONAL ATOMIC ENERGY AGENCY, Cyclotron Produced Radionuclides: Physical Characteristics and Production Methods, Technical Reports Series No. 468, IAEA, Vienna (2009) 244. [10.17] CHINOL, M., HNATOWICH, D.J., Generator produced yttrium-90 for radioimmunotherapy, J. Nucl. Med. 28 (1987) 1465. [10.18] CHAKRAVARTY, R., et al., Development of an electrochemical 90 Sr– 90 Y generator for separation of 90 Y suitable for targeted therapy, Nucl. Med. Biol. 35 (2008) 245. [10.19] INTERNATIONAL ATOMIC ENERGY AGENCY, Therapeutic Radionuclide Generators: 90 Sr/ 90 Y and 188 W/ 188 Re Generators, Technical Reports Series No. 470, IAEA, Vienna (2009) 73. [10.20] PANDEY, U., DHAMI, P.S., JAGESIA, P., VENKATESH, M., PILLAI, M.R.A., A novel extraction paper chromatography (EPC) technique for the radionuclidic purity evaluation of 90 Y for clinical use, Anal. Chem. 80 (2008) 801. 205
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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YTTRIUM-90 AND RHENIUM-188 RADIOPHA
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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FOREWORD The IAEA helps to promote
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CONTENTS CHAPTER 1. INTRODUCTION ..
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7.4. Discussion ...................
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CHAPTER 12. DEVELOPMENT OF 90 Sr/ 9
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Chapter 1 INTRODUCTION 1.1. BACKGRO
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devices were designed to improve th
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etention of the antibody’s target
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Binding affinity of these derivativ
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Chapter 2 FUNDAMENTAL CONCEPTS IN R
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A special characteristic of radioph
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β particles emitted by 90 Y. Numer
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2.3.1. Exploitation of certain meta
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2.3.3. Antibodies The high specific
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cell cultures, presents one example
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Another very promising form of radi
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destructive processes within the jo
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esearch efforts, since then. Howeve
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[2.18] HAMILTON, J.G., The metaboli
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[2.52] GOLDENBERG, D.M., et al., Mu
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Chapter 3 DEVELOPMENT OF RADIOPHARM
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FIG. 3.3. Elution efficiencies for
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FIG. 3.5. Electrodeposition of yttr
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The results of the experiments of r
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TABLE 3.3. RESULTS FOR 90 Sr/ 90 Y
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FIG. 3.11. Elution yield of a 90 Sr
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According to Fig. 3.12, there is a
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eagent (Sigma). The mean recovery o
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FIG. 3.18. Variation of RCP (%) of
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(20 and 30 min) and volume of 188 R
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FIG. 3.24. Variation of labelling y
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(c) Clodronate: 20 mg of clodronate
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Chapter 4 EVALUATION OF THE 90 Sr/
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Kamadhenu consists of five main com
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Quality control of radiolabelling w
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The electrochemical deposition of 9
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FIG. 4.5. Typical pattern of the wh
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FIG. 4.6. Elution profile from the
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FIG. 4.8. CD20 recognition in Ramos
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4.5. RECOMMENDATIONS AND FUTURE WOR
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adioiodine labelled anti-NCAM antib
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FIG. 5.1. Comparison of biodistribu
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FIG. 5.3. Three step strategy. Biot
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TABLE 5.1. THREE STEP PRETARGETING:
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5.1.4. Therapeutic experiments with
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5.1.4.4. Conclusion The radioiodine
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control procedure for detection of
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6.1.3. Recovery of doped 85/89 Sr 2
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6.2. PREPARATION AND BIOEVALUATION
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(a) (b) (c) FIG. 6.5. PD-10 column
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FIG. 6.7. SDS PAGE pattern of ritux
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FIG. 6.10. HPLC pattern of pure 90
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FIG. 6.13. Cell binding studies wit
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6.2.1.6. Conclusion The procedure f
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FIG. 6.17. Elution profile of 90 Y
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form NADH, which, in turn, causes t
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FIG. 6.19. In vivo distribution pat
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ACKNOWLEDGEMENTS The authors of thi
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Chapter 7 DEVELOPMENT OF THERAPEUTI
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the residual breast tissue becoming
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7.2.5.2. Automatic procedure The la
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FIG. 7.2. RCP values of 90 Y r-BHD
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FIG. 7.3. Pyrogen test shows result
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to avidin at the 1:4 avidin:r-BHD m
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[7.9] SU, F.M., GUSTAVSON, L.M., AX
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8.1. INTRODUCTION In past years, th
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(a) FIG. 8.1. (a) Schematic illustr
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Preliminary synthesis of the biotin
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(a) (b) FIG. 8.4. (a) PEGylated and
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TABLE 8.2. BIODISTRIBUTION IN RATS
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A specific binding to avidin was ev
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[8.13] BOSCHI, A., DUATTI, A., UCCE
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90 Y solution obtained from a 90 Sr
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From each fraction, a ~1 g aliquot
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FIG. 9.2. Relationship between 90 S
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with 188 Re obtained from the 188 W
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9.3.2. Labelling of DPA ale DPA ale
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FIG. 9.8. TLC radiochromatogram of
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(-) 188 Re(CO) 3 (+) (-) 99m Tc(CO)
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the HSA solution containing sodium
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TABLE 9.3. RESULTS OF 99m Tc LABELL
Page 167 and 168: 9.4.4. Yttrium-90 and 177 Lu labell
Page 169 and 170: FIG. 9.14. In vitro stability of 90
Page 171 and 172: (a) (b) (c) (d) (e) (f) (g) (h) (i)
Page 173 and 174: TABLE 9.8. YTTRIUM-90 CITRATE COLLO
Page 175 and 176: (a) (b) FIG. 9.17. Grain size distr
Page 177 and 178: TABLE 9.10. BIODISTRIBUTION AFTER A
Page 179 and 180: FIG. 9.19. Structure of DOTA biotin
Page 181 and 182: [9.8] WESTERA, G., GADZE, A., HORST
Page 183 and 184: Chapter 10 DEVELOPMENT, PREPARATION
Page 185 and 186: acidic pH) and the vial heated for
Page 187 and 188: 10.2.2.1. Materials and methods (a)
Page 189 and 190: Using a semiquantitative method, th
Page 191 and 192: FIG. 10.3. Whole body, SPECT and ta
Page 193 and 194: TABLE 10.4. ORGAN DISTRIBUTION STUD
Page 195 and 196: was assessed by measuring the relea
Page 197 and 198: —— Biological studies: The whol
Page 199 and 200: or liver) (see Fig. 10.7). The resu
Page 201 and 202: (b) Results and discussion Healthy
Page 203 and 204: and the pellet (particles of HA lab
Page 205 and 206: FIG. 10.11. Organ distribution stud
Page 207 and 208: The procedure was as follows: —
Page 209 and 210: TABLE 10.5. INFLUENCE OF CHEMICAL I
Page 211 and 212: analysed using ICP OES was within t
Page 213 and 214: suggested for separation of pure 86
Page 215 and 216: adionuclidic purity of the 90 Y sol
Page 217: FIG. 10.16. (a) Strontium-90/yttriu
Page 221 and 222: Yttrium-90 is one of the radionucli
Page 223 and 224: (a) (b) (c) The generator was prepa
Page 225 and 226: —— Development of EPC: The EPC
Page 227 and 228: FIG. 11.4. Elution curve of 90 Sr e
Page 229 and 230: 11.4. YTTRIUM-90 MAbs The use of th
Page 231 and 232: FIG. 11.6. RCP measured using ITLC
Page 233 and 234: FIG. 11.9. Biodistribution of 90 Y
Page 235 and 236: 11.5. YTTRIUM-90 EDTMP Bone metasta
Page 237 and 238: FIG. 11.14. Electrophoresis of 90 Y
Page 239 and 240: FIG. 11.15. Particle size distribut
Page 241 and 242: 11.7. CONCLUSION During this CRP, a
Page 243 and 244: Chapter 12 DEVELOPMENT OF 90 Sr/ 90
Page 245 and 246: 12.1.1.4. Acid vapour trap and radi
Page 247 and 248: 12.1.8. Yttrium-90 peptide labellin
Page 249 and 250: (a) FIG. 12.3. Yttrium-90 elution p
Page 251 and 252: FIG. 12.6. HPLC of 90 Y DOTATATE. 1
Page 253 and 254: Chapter 13 BIFUNCTIONAL BISPHOSPHON
Page 255 and 256: latter requirement [13.10]. When th
Page 257 and 258: whether the organometallic core sel
Page 259 and 260: The fate of a targeted imaging prob
Page 261 and 262: FIG. 13.7. SPECT/CT images showing
Page 263 and 264: FIG. 13.9. TLC SG analyses of [ 188
Page 265 and 266: FIG. 13.11. Stability study (toward
Page 267 and 268: Ex vivo biodistribution studies at
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was in the form of either pertechne
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FIG. 13.19. Absolute uptake of 99m
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[13.2] ZHANG, S., GANGAL, G., ULUDA
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[13.31] DE ROSALES, R.T.M., et al.,
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The activity due to 90 Sr should be
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14.3.1.2. Operation of the 90 Sr/ 9
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antibody were taken, to which 90 Y
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operation, radiopharmaceutical grad
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14.4.1.3. Operation of the stage II
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A typical EPC pattern for a 90 Y pr
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FIG. 14.10. Decay curve of carrier
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FIG. 14.12. ITLC of 90 Y rituximab.
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FIG. 14.13. Reaction scheme for lab
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TABLE 14.6. STABILITY (%) OF 90 Y D
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FIG. 14.18. Microsphere albumin siz
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[14.3] PANDEY, U., DHAMI, P.S., JAG
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naphthalene and 1.2 g of 2,5-diphen
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A-2.2. Materials The method for sep
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out using a Wallac 1411 spectromete
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A-5.3. Procedure The technique was
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Although acyclic chelators offer ma
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(b) (c) and 90 Y colloids, both ser
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CONTRIBUTORS TO DRAFTING AND REVIEW
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INDIA Allied Publishers 1 st Floor,
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A key requirement for the effective
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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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