Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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FIG. 3.20. Variation of RCP (%) of 188 Re rituximab (best formulation) at different times and different temperatures. CT: cold temperature (5°C); DI: dry ice; RT: room temperature. A different approach was employed for labelling anti-CD20 antibody using the 99m Tc and 188 Re tricarbonyl technique. This project was developed at the Paul Scherrer Institute (Switzerland), in cooperation with R. Schibli. The study was successful and the results (not described here) have been published [3.5]. 3.2.2. DMSA(V) 3.2.2.1. Preparation of 188 Re-DMSA(V) The RCP was evaluated using TLC on SG strips to determine the labelling efficiency and impurity formation. TLC SG strips (1.5 cm × 12 cm) were developed in two different solvent systems. Acetone was used to separate 188 ReO 4 – (R f = 1) from 188 Re DMSA(V) and 188 ReO 2 (R f = 0), and 5% glycine was used to separate 188 ReO 2 (R f = 0) from 188 Re DMSA(V) and 188 ReO 4 – (R f = 1). Method I: Initially, 188 Re DMSA(V) was prepared using a commercial kit of DMSA(III) for labelling with 99m Tc (IPEN-CNEN/SP). The kit contained 1.0 mg of DMSA, 0.44 mg of SnCl 2 ⋅2H 2 O, 0.70 mg of ascorbic acid and 50 mg of inositol. The labelling was performed using 1 mL of 188 ReO 4 – (185 MBq), and the reaction time was 30 min at high temperature (100°C). The variables studied were reaction temperature (100°C and room temperature), reaction time 48
(20 and 30 min) and volume of 188 ReO 4 – (1.0 and 2.0 mL). Figures 3.21, 3.22 and 3.23 show the results of the effect of the variation of reaction temperature, time and volume on the labelling efficiency of 188 Re DMSA(V) prepared using a commercial kit of 99m Tc DMSA(III). The best labelling yield (>98%) was achieved when 1 mL 188 ReO 4 – was used for 30 min of reaction while heating at 100°C [3.6]. FIG. 3.21. Variation of labelling yield with reaction temperature. FIG. 3.22. Variation of labelling yield with reaction time. 49
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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 ..
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 and 44: [2.52] GOLDENBERG, D.M., et al., Mu
Page 45 and 46: Chapter 3 DEVELOPMENT OF RADIOPHARM
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: FIG. 3.18. Variation of RCP (%) of
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
Page 103 and 104: (a) (b) (c) FIG. 6.5. PD-10 column
Page 105 and 106: FIG. 6.7. SDS PAGE pattern of ritux
Page 107 and 108: FIG. 6.10. HPLC pattern of pure 90
Page 109 and 110: FIG. 6.13. Cell binding studies wit
Page 111 and 112: 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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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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