Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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The following States are Members of the International Atomic Energy Agency: AFGHANISTAN ALBANIA ALGERIA ANGOLA ARGENTINA ARMENIA AUSTRALIA AUSTRIA AZERBAIJAN BAHAMAS BAHRAIN BANGLADESH BELARUS BELGIUM BELIZE BENIN BOLIVIA BOSNIA AND HERZEGOVINA BOTSWANA BRAZIL BRUNEI DARUSSALAM BULGARIA BURKINA FASO BURUNDI CAMBODIA CAMEROON CANADA CENTRAL AFRICAN REPUBLIC CHAD CHILE CHINA COLOMBIA CONGO COSTA RICA CÔTE D’IVOIRE CROATIA CUBA CYPRUS CZECH REPUBLIC DEMOCRATIC REPUBLIC OF THE CONGO DENMARK DOMINICA DOMINICAN REPUBLIC ECUADOR EGYPT EL SALVADOR ERITREA ESTONIA ETHIOPIA FIJI FINLAND FRANCE GABON GEORGIA GERMANY GHANA GREECE GUATEMALA HAITI HOLY SEE HONDURAS HUNGARY ICELAND INDIA INDONESIA IRAN, ISLAMIC REPUBLIC OF IRAQ IRELAND ISRAEL ITALY JAMAICA JAPAN JORDAN KAZAKHSTAN KENYA KOREA, REPUBLIC OF KUWAIT KYRGYZSTAN LAO PEOPLE’S DEMOCRATIC REPUBLIC LATVIA LEBANON LESOTHO LIBERIA LIBYA LIECHTENSTEIN LITHUANIA LUXEMBOURG MADAGASCAR MALAWI MALAYSIA MALI MALTA MARSHALL ISLANDS MAURITANIA, ISLAMIC REPUBLIC OF MAURITIUS MEXICO MONACO MONGOLIA MONTENEGRO MOROCCO MOZAMBIQUE MYANMAR NAMIBIA NEPAL NETHERLANDS NEW ZEALAND NICARAGUA NIGER NIGERIA NORWAY OMAN PAKISTAN PALAU PANAMA PAPUA NEW GUINEA PARAGUAY PERU PHILIPPINES POLAND PORTUGAL QATAR REPUBLIC OF MOLDOVA ROMANIA RUSSIAN FEDERATION RWANDA SAN MARINO SAUDI ARABIA SENEGAL SERBIA SEYCHELLES SIERRA LEONE SINGAPORE SLOVAKIA SLOVENIA SOUTH AFRICA SPAIN SRI LANKA SUDAN SWAZILAND SWEDEN SWITZERLAND SYRIAN ARAB REPUBLIC TAJIKISTAN THAILAND THE FORMER YUGOSLAV REPUBLIC OF MACEDONIA TOGO TRINIDAD AND TOBAGO TUNISIA TURKEY UGANDA UKRAINE UNITED ARAB EMIRATES UNITED KINGDOM OF GREAT BRITAIN AND NORTHERN IRELAND UNITED REPUBLIC OF TANZANIA UNITED STATES OF AMERICA URUGUAY UZBEKISTAN VENEZUELA, BOLIVARIAN REPUBLIC OF VIET NAM YEMEN ZAMBIA ZIMBABWE The Agency’s Statute was approved on 23 October 1956 by the Conference on the Statute of the IAEA held at United Nations Headquarters, New York; it entered into force on 29 July 1957. The Headquarters of the Agency are situated in Vienna. Its principal objective is “to accelerate and enlarge the contribution of atomic energy to peace, health and prosperity throughout the world’’.
IAEA RADIOISOTOPES AND RADIOPHARMACEUTICALS SERIES No. 5 YTTRIUM-90 AND RHENIUM-188 RADIOPHARMACEUTICALS FOR RADIONUCLIDE THERAPY INTERNATIONAL ATOMIC ENERGY AGENCY VIENNA, 2015
Page 1 and 2: IAEA RADIOISOTOPES AND RADIOPHARMAC
Page 3: YTTRIUM-90 AND RHENIUM-188 RADIOPHA
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 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 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
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
Page 113 and 114:
FIG. 6.17. Elution profile of 90 Y
Page 115 and 116:
form NADH, which, in turn, causes t
Page 117 and 118:
FIG. 6.19. In vivo distribution pat
Page 119 and 120:
ACKNOWLEDGEMENTS The authors of thi
Page 121 and 122:
Chapter 7 DEVELOPMENT OF THERAPEUTI
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the residual breast tissue becoming
Page 125 and 126:
7.2.5.2. Automatic procedure The la
Page 127 and 128:
FIG. 7.2. RCP values of 90 Y r-BHD
Page 129 and 130:
FIG. 7.3. Pyrogen test shows result
Page 131 and 132:
to avidin at the 1:4 avidin:r-BHD m
Page 133 and 134:
[7.9] SU, F.M., GUSTAVSON, L.M., AX
Page 135 and 136:
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
Page 141 and 142:
(a) (b) FIG. 8.4. (a) PEGylated and
Page 143 and 144:
TABLE 8.2. BIODISTRIBUTION IN RATS
Page 145 and 146:
A specific binding to avidin was ev
Page 147 and 148:
[8.13] BOSCHI, A., DUATTI, A., UCCE
Page 149 and 150:
90 Y solution obtained from a 90 Sr
Page 151 and 152:
From each fraction, a ~1 g aliquot
Page 153 and 154:
FIG. 9.2. Relationship between 90 S
Page 155 and 156:
with 188 Re obtained from the 188 W
Page 157 and 158:
9.3.2. Labelling of DPA ale DPA ale
Page 159 and 160:
FIG. 9.8. TLC radiochromatogram of
Page 161 and 162:
(-) 188 Re(CO) 3 (+) (-) 99m Tc(CO)
Page 163 and 164:
the HSA solution containing sodium
Page 165 and 166:
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 and 218:
FIG. 10.16. (a) Strontium-90/yttriu
Page 219 and 220:
[10.5] DJOKIĆ, D.J., JANKOVIĆ, D.
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
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
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,
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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