Document Detail

Antitumor activity and metabolism of a new anthracycline-containing fluorine (ME2303) in Lewis lung carcinoma-bearing mice.
MedLine Citation:
PMID:  1752788     Owner:  NLM     Status:  MEDLINE    
(7-O-(2,6-Dideoxy-2-fluoro-alpha-L-talopyranosyl)adriamycinone-14- hemipimerate (ME2303) showed a more marked growth inhibition of Lewis lung carcinoma than adriamycin (ADM). When administered to s.c. Lewis lung carcinoma-bearing mice, ME2303 in the plasma and liver was rapidly metabolized and disappeared. However, ME2303 was incorporated into the tumor at higher concentrations and remained in the tumor for a longer period than in the plasma and liver. ME2303 was metabolized to 7-O-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl)adriamycinone (M1), the product of esterolysis, and its reduced derivative at the C-13 position (M2). Larger amounts of these metabolites were found in the analyzed tissues than in plasma. The maximum concentration of M1 in the tumor was observed at 2 h posttreatment, while the maxima in the plasma and liver were observed at 15 min. On the other hand, i.v. injection of M1 into mice showed a weaker antitumor effect than ME2303 injection, though M1 levels in the plasma and tumor were almost the same as those after administration of ME2303 at the maximum tolerated doses. Some metabolites of ME2303 were found in the tumor after administration of ME2303, but not after administration of M1. ADM remained in the analyzed tissues for a long period and ADM concentrations in the tumor were much higher than in the plasma but less than in the liver. M1 reached a concentration higher than that of ADM in the tumor, opposite to the pattern observed in the liver. The conversion process from ME2303 to M1, the metabolites and their locations in the tumor may be important for the marked antitumor effect of ME2303 in vivo.
M Iigo; A Hoshi; H Kadosawa; M Fujigaki
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Japanese journal of cancer research : Gann     Volume:  82     ISSN:  0910-5050     ISO Abbreviation:  Jpn. J. Cancer Res.     Publication Date:  1991 Nov 
Date Detail:
Created Date:  1992-01-24     Completed Date:  1992-01-24     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8509412     Medline TA:  Jpn J Cancer Res     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  1317-21     Citation Subset:  IM    
Chemotherapy Division, National Cancer Center Research Institute, Tokyo.
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MeSH Terms
Antineoplastic Agents / therapeutic use*
Cell Division
Doxorubicin / analogs & derivatives*,  metabolism,  pharmacokinetics,  therapeutic use*
Liver / metabolism
Lung Neoplasms / drug therapy*,  metabolism,  pathology
Mice, Inbred Strains
Time Factors
Tissue Distribution
Reg. No./Substance:
0/Antineoplastic Agents; 116521-53-0/ME 2303; 23214-92-8/Doxorubicin

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