Toremifene metabolism in rat, mouse and human liver microsomes: Identification of α-hydroxtoremifene by LC-MS

Biomedical Chromatography

Volumn 16, Issue 5, 2002, Pages 361-363

  Jones, Russell M ^a   Lim, C K ^a  

^a UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BIOMOLECULES; ELECTROSPRAY IONIZATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; METABOLITES; PHYSIOLOGY; RATS;

HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN LIVER MICROSOMES; IN-VITRO; LIQUID CHROMATOGRAPHY-ELECTROSPRAY IONIZATION-MASS SPECTROMETRIES; MICE LIVER; MICROSOMAL PREPARATIONS; N-OXIDES; POLAR METABOLITE; PROTONATED MOLECULES; RAT LIVER MICROSOMES;

METABOLISM;

DRUG METABOLITE; TAMOXIFEN; TOREMIFENE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG METABOLISM; DRUG STRUCTURE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN TISSUE; HYDROXYLATION; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; LIVER CARCINOGENESIS; LIVER MICROSOME METABOLISM; MASS SPECTROMETRY; MOUSE; NONHUMAN; PROTON TRANSPORT; RAT;

EID: 0036689529     PISSN: 02693879     EISSN: None     Source Type: Journal    
DOI: 10.1002/bmc.171     Document Type: Article

References (16)

1. Tamoxifen-the treatment of choice. Why look for alternatives?
2. Alpha-hydroxytamoxifen, a genotoxic metabolite of tamoxifen in the rat: Identification and quantification in vivo and in vitro
3. Identification of tamoxifen-DNA adducts formed by α-sulfate tamoxifen and α-acetoxytamoxifen
4. The metabolic activation of tamoxifen and alpha-hydroxytamoxifen to DNA-binding species in rat hepatocytes proceed via sulfation
5. Induction of covalent DNA adducts in rodent by tamoxifen
6. Major differences in the hepatocarcinogenicity and DNA adduct forming ability between toremifene and tamoxifen in female Cr1: CD(BR) rats
7. The deuterium isotope effect for the α-hydroxylation of tamoxifen by rat liver microsomes accounts for the reduced genotoxicity of D5-ethyltamoxifen
8. A comparative study of tamoxifen metabolism in female rat, mouse and human liver microsomes
9. Cytochrome P450 mediated action and irreversible binding of the antiestrogen tamoxifen to proteins in rat and human liver: Possible involvement of the flavin-containing monooxygenases in tamoxifen activation
10. Minor products of reaction of DNA with α-acetoxytamoxifen
11. α-Hydroxytamoxifen, a metabolite of tamoxifen with exceptionally high DNA binding activity in rat hepatocytes
12. A mechanistic hypothesis for DNA adduct formation by tamoxifen following hepatic oxidative metabolism
13. Sulfation of α-hydroxytamoxifen catalyzed by human hydroxysteroid sulfotransferase results in tamoxifen-DNA adducts
14. Chemoprevention of breast cancer by tamoxifen: Risk and opportunities
15. Multicenter phase II efficacy trial of toremifene in tamoxifen-refractory patients with advanced breast cancer
16. Genotoxic potential of tamoxifen and analogues in female Fischer F344/N rats, DBA/2 and C57B1/6 mice and in human MCL-5 cells