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Tamoxifen metabolic activation

The mechanism by which tamoxifen is carcinogenic is via metabolic activation to yield a reactive metabolite, which reacts with DNA. Study of the metabolism in different species has revealed the important metabolic pathways involved in both activation and detoxication. [Pg.304]

Figure 7.9 The metabolism and metabolic activation of tamoxifen. Abbreviations SULT, sulfotransferase UGT, UDP-glucuronosyl transferase. Figure 7.9 The metabolism and metabolic activation of tamoxifen. Abbreviations SULT, sulfotransferase UGT, UDP-glucuronosyl transferase.
This understanding allows a rational risk assessment of tamoxifen, which is that the risk of liver cancer is extremely low because of detoxication pathways and the lack of metabolic activation. [Pg.305]

Robertson DW, Katzenellenbogen JA, Long DJ, Rorke EA, Katzenellenbogen BS (1982) Tamoxifen antiestrogens - a comparison of the activity, pharmacokinetics, and metabolic-activation of the cis-isomer and trans-isomer of tamoxifen. J Steroid Biochem 16 1-13... [Pg.111]

Davis DC, Potter WZ, follow DJ et al (1974) Species differences in hepatic glutathione depletion, covalent binding and hepatic necrosis after acetaminophen. Life Sci 14 2099-2109 Davis W, Venitt S, Phillips DH (1998) The metabolic activation of tamoxifen and a-hydroxyta-moxifen to DNA-binding species in rat hepatocytes proceeds via sulphation. Carcinogenesis 19 861-866... [Pg.187]

Blevins-Primeau AS et al (2009) Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res 69 1892-1900... [Pg.246]

Irvin WJ Jr et al (2011) Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism a multicenter study. J Clin Oncol 29 3232-3239... [Pg.248]

Since EM-800 is rapidly metabolized into the active compound EM-652 in intact cells, we compared the effect of increasing concentrations of the nonsteroidal antiestrogens EM-652 and EM-800 with those of hydroxytamoxifen and tamoxifen and of the steroidal antiestrogen ICI 164384 on basal and E2-induced cell proliferation in T-47D, ZR-75-1 and MCF-7 cells (Simard et al., 1997a). As illustrated in Fig. 20, a 10-day exposure to 0.1 nME2 increased the proliferation of T-47D cells 4.77-fold. This E induced stimulation of cell proliferation was competitively blocked by simultaneous incubation with EM-800, EM-652, hydroxytamoxifen, ICI 164,384, and tamoxifen at respective IC50 values of 0.148, 0.146, 0.522, 2.41, and about 100 nM. It can also be seen in Fig. 20 that none of these compounds affected basal T47-D cell proliferation when incubated alone. [Pg.336]

Foster AB, McCague R, Seago A, Leclercq G, Stoessel S, Roy F (1986) Modification of the basic side chain in tamoxifen effects on microsomal metabolism and in vitro biological activity. Anticancer Drug Des 1 245-257... [Pg.112]


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See also in sourсe #XX -- [ Pg.304 ]




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