Document Detail

188Re-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases.
MedLine Citation:
PMID:  15701408     Owner:  NLM     Status:  MEDLINE    
Two new bisphosphonates have been examined for their ability to bind 188Re and deliver it selectively to bone. The bisphosphonates are prototype compounds with potential to deliver rhenium radionuclides and a second therapy modality to bone metastases. A conjugate between diethylenetriaminepentaacetic acid and bisphosphonate (DTPA/BP) and a conjugate between 5-fluorouracil and bisphosphonate (5-FU/BP) were prepared and labeled at high radiochemical purity with 188Re and biodistribution studies were carried out in normal Balb/C mice. The compounds showed rapid blood clearance and elimination from soft tissues with substantial retention of activity in the bone comparable to 188Re-hydroxyethylidine diphosphonate used as a control. At 8 h bone activity was 3.51% of injected dose for 188Re-DTPA/BP and 6.38% of injected dose for 188Re-5-FU/BP representing 69.6% and 80.6% of total body radioactivity, respectively. The two compounds show the potential for combination therapy of painful bone metastases.
Amal El-Mabhouh; John R Mercer
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine     Volume:  62     ISSN:  0969-8043     ISO Abbreviation:  Appl Radiat Isot     Publication Date:  2005 Apr 
Date Detail:
Created Date:  2005-02-09     Completed Date:  2005-04-08     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9306253     Medline TA:  Appl Radiat Isot     Country:  England    
Other Details:
Languages:  eng     Pagination:  541-9     Citation Subset:  IM    
Faculty of Pharmacy and Pharmaceutical Sciences, 3118 Dentistry Pharmacy Center, University of Alberta, Edmonton Alta, Canada T6G-2N8.
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MeSH Terms
Bone Neoplasms / drug therapy,  metabolism*,  radiotherapy,  secondary
Diphosphonates / chemistry,  pharmacokinetics*,  pharmacology
Fluorouracil / chemistry,  pharmacokinetics*,  pharmacology
Isotope Labeling
Mice, Inbred BALB C
Pentetic Acid / chemistry,  pharmacokinetics*,  pharmacology
Radioisotopes / chemistry,  pharmacokinetics*,  pharmacology
Radiopharmaceuticals / chemical synthesis,  pharmacokinetics*,  pharmacology
Rhenium / chemistry,  pharmacokinetics*,  pharmacology
Tissue Distribution
Reg. No./Substance:
0/Diphosphonates; 0/Radioisotopes; 0/Radiopharmaceuticals; 51-21-8/Fluorouracil; 67-43-6/Pentetic Acid; 7440-15-5/Rhenium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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