K. Hemminki et al., DNA-ADDUCTS CAUSED BY TAMOXIFEN AND TOREMIFENE IN HUMAN MICROSOMAL SYSTEM AND LYMPHOCYTES IN-VITRO, Carcinogenesis, 16(7), 1995, pp. 1661-1664
DNA-binding of tamoxifen and toremifene was studied in rat in vivo, in
human and rat microsomes in vitro, and in cultured primary human lymp
hocytes by P-32-postlabelling. Only tamoxifen caused DNA adducts in ra
t liver. Both compounds induced adducts in both rat and human microsom
al systems and in cultured lymphocytes. The levels of adducts in micro
somes and lymphocytes were low, ca. 1 adduct/10(9) nucleotides. Toremi
fene showed lower binding in each system, and in lymhocytes adducts we
re only detected at a cytotoxic dose level.