Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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[2.69] XIE, J., et al., PET/NIRF/MRI triple functional iron oxide nanoparticles, Biomaterials 31 (2010) 3016. [2.70] TING, G., et al., Nanotargeted radionuclides for cancer nuclear imaging and internal radiotherapy, J. Biomed. Biotechnol. 2010 (2010) 953537. [2.71] LIU, X., et al., Auger radiation-induced, antisense-mediated cytotoxicity of tumor cells using a 3-component streptavidin-delivery nanoparticle with 111 In, J. Nucl. Med. 50 (2009) 582. [2.72] BULTE, J.W., Science to practice: Can theranostic fullerenes be used to treat brain tumors? Radiology 261 (2011) 1. [2.73] LI, Z., et al., Synthesis and cell uptake of a novel dual modality 188 Re-HGRGD (D) F-CdTe QDs probe, Talanta 85 (2011) 936. [2.74] LAWRENCE, J.H., Nuclear physics and therapy: Preliminary report on a new method for the treatment of leukemia and polycythemia, Radiology 52 (1940) 51. [2.75] HERTZ, S., ROBERTS, A., Application of radioactive iodine in therapy of Graves’ disease, J. Clin. Invest. 21 (1942) 624. [2.76] GIOVACCHINI G., et al., Peptide receptor radionuclide therapy with somatostatin analogues in neuroendocrine tumors, Anticancer Agents Med. Chem. 12 (2012) 526. 30
Chapter 3 DEVELOPMENT OF RADIOPHARMACEUTICALS BASED ON 188 Re AND 90 Y FOR RADIONUCLIDE THERAPY AT IPEN-CNEN/SP J.A. OSSO, JR., G. BARRIO, C.R.B.R. DIAS, T.P. BRAMBILLA, D.M. DANTAS, K.N. SUZUKI, A.B. BARBEZAN, N.P. REIS, T.A. FELIX, M.F.S. BARBOZA, N.T. FUKUMORI, J. MENGATTI Radiopharmacy Center, Institute of Energetic and Nuclear Research, IPEN-CNEN/SP, São Paulo, Brazil Abstract The overall objectives of this CRP are the development of radiopharmaceuticals for targeted therapy using 188 Re and 90 Y to study the performance of generators with long lived parent radionuclides and to validate the quality control procedures for estimating the purity of generator eluents. The CRP is expected to enhance the capability in production of 90 Y and 188 Re radiopharmaceuticals to meet the increasing demand of therapeutic products for clinical applications, particularly in Brazil. Efforts have been made towards assembling 90 Sr/ 90 Y generators, performing quality control of 90 Y, labelling of DMSA(V), bisphosphonates and anti-CD20 with 188 Re, and labelling of HA with 90 Y. 3.1. STRONTIUM-90/YTTRIUM-90 GENERATORS 3.1.1. Stronium-90/yttrium-90 ion exchange chromatography generator Two generators were prepared based on cation exchange resins in continuation of the work from the previous CRP on the development of generator technologies for therapeutic radionuclides [3.1–3.3]. The resin employed was Dowex 50WX8 (100–200 mesh), H + form, and the generators dimensions (see Fig. 3.1) were: (a) (b) Generator G 1 : 10 cm high, 1 cm inner diameter; Generator G 2 : 10 cm high, 0.5 cm inner diameter. 31
Page 1 and 2: IAEA RADIOISOTOPES AND RADIOPHARMAC
Page 3 and 4: YTTRIUM-90 AND RHENIUM-188 RADIOPHA
Page 5 and 6: IAEA RADIOISOTOPES AND RADIOPHARMAC
Page 7 and 8: FOREWORD The IAEA helps to promote
Page 9 and 10: CONTENTS CHAPTER 1. INTRODUCTION ..
Page 11 and 12: 7.4. Discussion ...................
Page 13 and 14: CHAPTER 12. DEVELOPMENT OF 90 Sr/ 9
Page 15 and 16: Chapter 1 INTRODUCTION 1.1. BACKGRO
Page 17 and 18: devices were designed to improve th
Page 19 and 20: etention of the antibody’s target
Page 21 and 22: Binding affinity of these derivativ
Page 23 and 24: Chapter 2 FUNDAMENTAL CONCEPTS IN R
Page 25 and 26: A special characteristic of radioph
Page 27 and 28: β particles emitted by 90 Y. Numer
Page 29 and 30: 2.3.1. Exploitation of certain meta
Page 31 and 32: 2.3.3. Antibodies The high specific
Page 33 and 34: cell cultures, presents one example
Page 35 and 36: Another very promising form of radi
Page 37 and 38: destructive processes within the jo
Page 39 and 40: esearch efforts, since then. Howeve
Page 41 and 42: [2.18] HAMILTON, J.G., The metaboli
Page 43: [2.52] GOLDENBERG, D.M., et al., Mu
Page 47 and 48: FIG. 3.3. Elution efficiencies for
Page 49 and 50: FIG. 3.5. Electrodeposition of yttr
Page 51 and 52: The results of the experiments of r
Page 53 and 54: TABLE 3.3. RESULTS FOR 90 Sr/ 90 Y
Page 55 and 56: FIG. 3.11. Elution yield of a 90 Sr
Page 57 and 58: According to Fig. 3.12, there is a
Page 59 and 60: eagent (Sigma). The mean recovery o
Page 61 and 62: FIG. 3.18. Variation of RCP (%) of
Page 63 and 64: (20 and 30 min) and volume of 188 R
Page 65 and 66: FIG. 3.24. Variation of labelling y
Page 67 and 68: (c) Clodronate: 20 mg of clodronate
Page 69 and 70: Chapter 4 EVALUATION OF THE 90 Sr/
Page 71 and 72: Kamadhenu consists of five main com
Page 73 and 74: Quality control of radiolabelling w
Page 75 and 76: The electrochemical deposition of 9
Page 77 and 78: FIG. 4.5. Typical pattern of the wh
Page 79 and 80: FIG. 4.6. Elution profile from the
Page 81 and 82: FIG. 4.8. CD20 recognition in Ramos
Page 83 and 84: 4.5. RECOMMENDATIONS AND FUTURE WOR
Page 85 and 86: adioiodine labelled anti-NCAM antib
Page 87 and 88: FIG. 5.1. Comparison of biodistribu
Page 89 and 90: FIG. 5.3. Three step strategy. Biot
Page 91 and 92: TABLE 5.1. THREE STEP PRETARGETING:
Page 93 and 94: 5.1.4. Therapeutic experiments with
Page 95 and 96:
5.1.4.4. Conclusion The radioiodine
Page 97 and 98:
control procedure for detection of
Page 99 and 100:
6.1.3. Recovery of doped 85/89 Sr 2
Page 101 and 102:
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
Page 109 and 110:
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
Page 137 and 138:
(a) FIG. 8.1. (a) Schematic illustr
Page 139 and 140:
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
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9.4.4. Yttrium-90 and 177 Lu labell
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FIG. 9.14. In vitro stability of 90
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(a) (b) (c) (d) (e) (f) (g) (h) (i)
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TABLE 9.8. YTTRIUM-90 CITRATE COLLO
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(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
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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
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FIG. 10.3. Whole body, SPECT and ta
Page 193 and 194:
TABLE 10.4. ORGAN DISTRIBUTION STUD
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was assessed by measuring the relea
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—— Biological studies: The whol
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or liver) (see Fig. 10.7). The resu
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(b) Results and discussion Healthy
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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
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analysed using ICP OES was within t
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suggested for separation of pure 86
Page 215 and 216:
adionuclidic purity of the 90 Y sol
Page 217 and 218:
FIG. 10.16. (a) Strontium-90/yttriu
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[10.5] DJOKIĆ, D.J., JANKOVIĆ, D.
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Yttrium-90 is one of the radionucli
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(a) (b) (c) The generator was prepa
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—— 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
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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
Page 269 and 270:
was in the form of either pertechne
Page 271 and 272:
FIG. 13.19. Absolute uptake of 99m
Page 273 and 274:
[13.2] ZHANG, S., GANGAL, G., ULUDA
Page 275 and 276:
[13.31] DE ROSALES, R.T.M., et al.,
Page 277 and 278:
The activity due to 90 Sr should be
Page 279 and 280:
14.3.1.2. Operation of the 90 Sr/ 9
Page 281 and 282:
antibody were taken, to which 90 Y
Page 283 and 284:
operation, radiopharmaceutical grad
Page 285 and 286:
14.4.1.3. Operation of the stage II
Page 287 and 288:
A typical EPC pattern for a 90 Y pr
Page 289 and 290:
FIG. 14.10. Decay curve of carrier
Page 291 and 292:
FIG. 14.12. ITLC of 90 Y rituximab.
Page 293 and 294:
FIG. 14.13. Reaction scheme for lab
Page 295 and 296:
TABLE 14.6. STABILITY (%) OF 90 Y D
Page 297 and 298:
FIG. 14.18. Microsphere albumin siz
Page 299:
[14.3] PANDEY, U., DHAMI, P.S., JAG
Page 302 and 303:
naphthalene and 1.2 g of 2,5-diphen
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A-2.2. Materials The method for sep
Page 306 and 307:
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
Page 315:
CONTRIBUTORS TO DRAFTING AND REVIEW
Page 318 and 319:
INDIA Allied Publishers 1 st Floor,
Page 320:
A key requirement for the effective
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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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