Document Detail

Fluoro-, bromo-, and iodopaclitaxel derivatives: synthesis and biological evaluation.
MedLine Citation:
PMID:  12493538     Owner:  NLM     Status:  MEDLINE    
Paclitaxel (Taxol) is a clinically important chemotherapeutic agent. We describe the synthesis of fluoro-, bromo-, and iodopaclitaxel and their [(18)F]fluoro-, [(76)Br]bromo-, and [(124)I]iodo- analogues. [(18)F]Fluoropaclitaxel shows high uptake and rapid clearance from tissues in rats. Preadministration of paclitaxel in normal rats significantly increases (p < 0.005) retention of [(18)F]fluoropaclitaxel and [(76)Br]bromopaclitaxel in blood (33.0%), heart (32.0%), lung (37.6%) kidney (142.4%); and blood (33.4%), lung (42.3%), kidney (62.4%), respectively. [(18)F]Fluoropaclitaxel uptake in the brain of mdr1a/1b(-/-) mice is increased 1400% (p < 1.3e-07) relative to wild-type controls. Preadministration of paclitaxel or XR9576, a modulator, had little effect on the biodistribution in these mdr1a/1b(-/-) mice. As a result, [(18)F]fluoropaclitaxel will be a useful radiopharmaceutical for the study of multidrug resistant tumors.
Dale O Kiesewetter; Elaine M Jagoda; Chih-Hao K Kao; Ying Ma; Laura Ravasi; Kazuaki Shimoji; Lawrence P Szajek; William C Eckelman
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Publication Detail:
Type:  Comparative Study; Evaluation Studies; Journal Article    
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  30     ISSN:  0969-8051     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  2003 Jan 
Date Detail:
Created Date:  2002-12-20     Completed Date:  2003-07-22     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  England    
Other Details:
Languages:  eng     Pagination:  11-24     Citation Subset:  IM    
Positron Emission Tomography Department, Clinical Center, NIH, Bethesda, MD 20892, USA.
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MeSH Terms
Bromine Radioisotopes / chemistry,  diagnostic use,  pharmacokinetics
Cells, Cultured
Drug Resistance, Multiple
Fluorine Radioisotopes / chemistry,  diagnostic use,  pharmacokinetics
Hepatocytes / metabolism*,  radionuclide imaging
Iodine Radioisotopes / chemistry,  diagnostic use,  pharmacokinetics
Isotope Labeling / methods
Mice, Mutant Strains
Organ Specificity
Paclitaxel / analogs & derivatives,  chemical synthesis*,  diagnostic use,  pharmacokinetics*
Radiopharmaceuticals / chemical synthesis*,  diagnostic use,  pharmacokinetics*
Reference Values
Species Specificity
Reg. No./Substance:
0/Bromine Radioisotopes; 0/Fluorine Radioisotopes; 0/Iodine Radioisotopes; 0/Radiopharmaceuticals; 33069-62-4/Paclitaxel

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