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In vitro metabolic interactions between black cohosh (Cimicifuga racemosa) and Tamoxifen

机译:黑蹄(Cimicifuga Haremosa)和Tamoxifen之间的体外代谢相互作用

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Women with a history of ER-positive breast cancer taking tamoxifen (TAM) as a chemoprevention agent often suffer from hot flashes as a side effect. To manage these hot flashes, many women taking TAM also use the botanical dietary supplement black cohosh (Cimicifuga racemosa L.). TAM undergoes extensive oxidation by cytochrome P450 2D6 and 3A4 to the active metabolites 4-hydroxy-TAM and 4-hydroxy-N-demethyl TAM (endoxifen). In addition, CYP3A4 converts TAM into alpha-hydroxy-TAM which has been implicated in toxicity of TAM. The purpose of the present study was to examine whether black cohosh might interfere with the efficacy of TAM by inhibiting the production of active metabolites.
机译:作为化学预防剂的患有Tamoxifen(TAM)的患者患有ER阳性乳腺癌的妇女通常遭受热闪光作为副作用。为了管理这些热闪光,许多女性服用TAM也使用植物膳食补充剂黑色科鼻(Cimicifuga Racemosa L.)。 TAM通过细胞色素P450 2D6和3A4经历广泛的氧化至活性代谢物4-羟基-TAM和4-羟基-N-脱甲基TAM(Endoxifen)。此外,CYP3A4将TAM转化为α-羟基-TAM,这与TAM的毒性有关。本研究的目的是通过抑制活性代谢物的产生,检查黑色COHOSH是否会干扰TAM的功效。

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