Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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A key requirement for the effective implementation of the therapeutic approach, based on the intravenous administration of radiolabelled compounds (radionuclide therapy), is the sufficient availability of radionuclides with appropriate physical characteristics. Based on their nuclear properties, 188 Re and 90 Y are considered among the most interesting radionuclides for therapy. Furthermore, they are produced through portable generators, which provide a crucial advantage toward ensuring a worldwide distribution of these radionuclides. This publication illustrates recent studies aimed at investigating efficient quality control methods to ensure both the radionuclidic purity of generator eluates, and the proper preparation of new target specific 188 Re and 90 Y radiopharmaceuticals for various clinical applications. INTERNATIONAL ATOMIC ENERGY AGENCY VIENNA ISBN 978–92–0–103814–2 ISSN 2077–6462
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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
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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
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TABLE 9.10. BIODISTRIBUTION AFTER A
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FIG. 9.19. Structure of DOTA biotin
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[9.8] WESTERA, G., GADZE, A., HORST
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Chapter 10 DEVELOPMENT, PREPARATION
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acidic pH) and the vial heated for
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10.2.2.1. Materials and methods (a)
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Using a semiquantitative method, th
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FIG. 10.3. Whole body, SPECT and ta
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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
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FIG. 10.11. Organ distribution stud
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The procedure was as follows: —
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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
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adionuclidic purity of the 90 Y sol
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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
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FIG. 11.4. Elution curve of 90 Sr e
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11.4. YTTRIUM-90 MAbs The use of th
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FIG. 11.6. RCP measured using ITLC
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FIG. 11.9. Biodistribution of 90 Y
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11.5. YTTRIUM-90 EDTMP Bone metasta
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FIG. 11.14. Electrophoresis of 90 Y
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FIG. 11.15. Particle size distribut
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11.7. CONCLUSION During this CRP, a
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Chapter 12 DEVELOPMENT OF 90 Sr/ 90
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12.1.1.4. Acid vapour trap and radi
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12.1.8. Yttrium-90 peptide labellin
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(a) FIG. 12.3. Yttrium-90 elution p
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FIG. 12.6. HPLC of 90 Y DOTATATE. 1
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Chapter 13 BIFUNCTIONAL BISPHOSPHON
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latter requirement [13.10]. When th
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whether the organometallic core sel
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The fate of a targeted imaging prob
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FIG. 13.7. SPECT/CT images showing
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FIG. 13.9. TLC SG analyses of [ 188
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FIG. 13.11. Stability study (toward
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Ex vivo biodistribution studies at
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Page 279 and 280: 14.3.1.2. Operation of the 90 Sr/ 9
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Page 297 and 298: FIG. 14.18. Microsphere albumin siz
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Page 302 and 303: naphthalene and 1.2 g of 2,5-diphen
Page 304 and 305: A-2.2. Materials The method for sep
Page 306 and 307: out using a Wallac 1411 spectromete
Page 308 and 309: A-5.3. Procedure The technique was
Page 310 and 311: Although acyclic chelators offer ma
Page 312 and 313: (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,
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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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