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Research ArticleExperimental Studies

Thorium and Actinium Polyphosphonate Compounds as Bone-seeking Alpha Particle-emitting Agents

GJERMUND HENRIKSEN, ØYVIND S. RULAND and ROY H. LARSEN
Anticancer Research January 2004, 24 (1) 101-106;
GJERMUND HENRIKSEN
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ØYVIND S. RULAND
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ROY H. LARSEN
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Abstract

The present study explores the use of α-particleemitting, bone-seeking agents as candidates for targeted radiotherapy. Actinium and thorium 1,4,7,10 tetraazacyclododecane N, N’, N”, N”’ 1,4,7,10-tetra(methylene) phosphonic acid (DOTMP) and thorium-diethylene triamine N, N’, N” penta(methylene) phosphonic acid (DTMP) were prepared and their biodistribution evaluated in conventional Balb/C mice at four hours after injection. All three bone-seeking agents showed a high uptake in bone and a low uptake in soft tissues. Among the soft tissue organs, only kidney had a relatively high uptake. The femur/kidney ratios for 227Th- DTMP, 228Ac-DOTMP and 227Th-DOTMP were 14.2, 7.6 and 6.0, respectively. A higher liver uptake of 228Ac-DOTMP was seen than for 227Th-DTMP and 227Th-DOTMP. This suggests that some demetallation of the 228Ac-DOTMP complex had occurred. The results indicate that 225Ac-DOTMP, 227Th- DOTMP and 227Th-DTMP have promising properties as potential therapeutic bone-seeking agents.

  • Received August 28, 2003.
  • Accepted October 27, 2003.
  • Copyright© 2004 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved
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Anticancer Research: 24 (1)
Anticancer Research
Vol. 24, Issue 1
January-February 2004
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Thorium and Actinium Polyphosphonate Compounds as Bone-seeking Alpha Particle-emitting Agents
GJERMUND HENRIKSEN, ØYVIND S. RULAND, ROY H. LARSEN
Anticancer Research Jan 2004, 24 (1) 101-106;

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Thorium and Actinium Polyphosphonate Compounds as Bone-seeking Alpha Particle-emitting Agents
GJERMUND HENRIKSEN, ØYVIND S. RULAND, ROY H. LARSEN
Anticancer Research Jan 2004, 24 (1) 101-106;
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