Functional Characterization of Wild-type and 49 CYP2D6 Allelic Variants for N-Desmethyltamoxifen 4-Hydroxylation Activity

• Published in: DRUG METABOLISM AND PHARMACOKINETICS Vol. 29; no. 5; pp. 360 - 366
• Main Authors: Muroi, Yuka, Saito, Takahiro, Takahashi, Masamitsu, Sakuyama, Kanako, Niinuma, Yui, Ito, Miyabi, Tsukada, Chiharu, Ohta, Kiminori, Endo, Yasuyuki, Oda, Akifumi, Hirasawa, Noriyasu, Hiratsuka, Masahiro
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 2014; Japanese Society for the Study of Xenobiotics
• Subjects: Alleles; Animals; Biocatalysis; Cercopithecus aethiops; Cloning, Molecular; COS Cells; CYP2D6; Cytochrome P-450 CYP2D6 - genetics; Cytochrome P-450 CYP2D6 - metabolism; cytochrome P450; drug metabolism; genetic polymorphisms; Genetic Variation - genetics; Humans; Hydroxylation - genetics; Kinetics; pharmacogenomics; tamoxifen; Tamoxifen - analogs & derivatives; Tamoxifen - chemistry; Tamoxifen - metabolism; pharmacogenomics; cytochrome P450; genetic polymorphisms; CYP2D6; tamoxifen; drug metabolism

Genetic variations in cytochrome P450 2D6 (CYP2D6) contribute to interindividual variability in the metabolism of clinically used drugs, e.g., tamoxifen. CYP2D6 is genetically polymorphic and is associated with large interindividual variations in therapeutic efficacy and drug toxicity. In this study...