Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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(b) (c) and 90 Y colloids, both series with a volume ratio of 1:10. For the 186 Re colloid, radionuclide mobilization is achieved by admixing 65% HNO 3 . The extent of release of low molecular species from the radiocolloids is determined using thin layer chromatography (TLC) and ultrafiltration after incubation times of 1 h, 4 h, 24 h, 48 h, 6 d, 9 d, 13 d and 15 d. TLC is performed using 20 cm × 20 cm ITLC SG strips (Varian). The distribution of radioactivity is measured using a linear radioactivity scanner. For ultrafiltration, the Ultrafree MC filter with 5000 nominal molecular weight limit (Millipore) is used. After filtration, probe volumes of 200 µL are centrifuged for 7 h at 5000 U/min (2250g) using the ultracentrifuge Optima L-70K (Beckman Coulter) and the rotor model 70 Ti. Thus, the free or low molecular radionuclides 90 Y, 186 Re or 169 Er released from the radiocolloids are detected. Subsequent measurements of both filter and filtrate are performed after centrifugation in a well counter (such as ISOMED 100, Nuklear-Medizintechnik). A–8.3. Conclusion The two independent methods, TLC and ultrafiltration/ultracentrifugation, can differentiate between intact radioactive colloids and mobilized radionuclides with good conformity. REFERENCES TO ANNEX [A–1] NATIONAL BUREAU OF STANDARDS, “Maximum permissible body burden and maximum permissible concentrations of radionuclides in air and water for occupational exposure”, National Bureau of Standards Handbook, Vol. 69, NBS, Gaithersburg (1959) 38. [A–2] EUROPEAN MEDICINES AGENCY, Ytracis: European Public Assessment Report (EPAR), EMEA/H/C/470, European Medicines Agency (2008), http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_ the_public/human/000460/WC500045979.pdf [A–3] UNITED STATES PHARMACOPEIAL CONVENTION, Yttrium (Y-90) ybritumomab tiuxetan injection, United States Pharmacopeia 30 NF 25, USP Convention, Rockville (2007) 3487. [A–4] 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. [A–5] 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) 33–35. 298
[A–6] MARWAH, U.R., “Synthesis of organophosphorous extractants for solvent extraction of metals”, Proc. Natl Symp. Organic Reagents–Synthesis and Use in Extraction Metallurgy (ORSEUM-94), BARC, Mumbai (1994). [A–7] INTERNATIONAL COMMISSION ON RADIOLOGICAL PROTECTION, Radiation Dose to Patients from Radiopharmaceuticals (Addendum to ICRP Publication 53), Publication 80, Pergamon Press, Oxford and New York (1998). [A–8] BONARDI, M.L., MARTANO, L., GROPPI, F., CHINOL, M., Rapid determination of 90 Sr impurities in freshly “generator eluted” 90 Y for radiopharmaceutical preparation, Appl. Radiat. Isot. 67 (2009) 1874. [A–9] HORWITZ, E.P., McALISTER, D.R., BOND, A.H., BARRANS, R.E., Jr., Novel extraction of chromatographic resins based on tetraalkyldiglycolamides: Characterization and potential applications, Solvent Extr. Ion Exch. 23 (2005) 319. [A–10] URBANO, N., et al., Evaluation of a new biotin-DOTA conjugate for pretargeted antibody-guided radioimmunotherapy (PAGRIT), Eur. J. Nucl. Med. Mol. Imaging 34 (2007) 68. [A–11] PAGANELLI, G., et al., Intraopearative avidination for radionuclide therapy: A prospective new development to accelerate radiotherapy in breast cancer, Clin. Cancer Res. 13 Suppl. 18 (2007) 5646s. 299
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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
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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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.
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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
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 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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