Document Detail


188Re-labeled bisphosphonates as potential bifunctional agents for therapy in patients with bone metastases.
MedLine Citation:
PMID:  15701408     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Amal El-Mabhouh; John R Mercer
Related Documents :
8441038 - Enthesopathy of the patellar tendon insertion associated with isotretinoin therapy.
3156878 - Does aspiration of bones and joints affect results of later bone scanning?
536788 - The appearance of bone scans following fractures, including immediate and long-term stu...
8039308 - Scintigraphic appearance of bone during external beam irradiation.
8919208 - Site of origin of nasal polyps. transcranially removed naso-ethmoidal blocks as a scree...
22362818 - In situ removal of the pipeline embolization device: the 'corking' and 'pseudo-corking'...
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    
Affiliation:
Faculty of Pharmacy and Pharmaceutical Sciences, 3118 Dentistry Pharmacy Center, University of Alberta, Edmonton Alta, Canada T6G-2N8.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Animals
Bone Neoplasms / drug therapy,  metabolism*,  radiotherapy,  secondary
Diphosphonates / chemistry,  pharmacokinetics*,  pharmacology
Female
Fluorouracil / chemistry,  pharmacokinetics*,  pharmacology
Isotope Labeling
Mice
Mice, Inbred BALB C
Pentetic Acid / chemistry,  pharmacokinetics*,  pharmacology
Radioisotopes / chemistry,  pharmacokinetics*,  pharmacology
Radiopharmaceuticals / chemical synthesis,  pharmacokinetics*,  pharmacology
Rhenium / chemistry,  pharmacokinetics*,  pharmacology
Tissue Distribution
Chemical
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


Previous Document:  Experimental studies on excitation functions of the proton-induced activation reactions on silver.
Next Document:  Comparison of mammography radiation dose values obtained from direct incident air kerma measurements...