Dydrogesterone在人类肝脏代谢aldo-keto还原酶和细胞色素P450酶。

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Olbrich M, Weigl K,卡勒E,历经甲级K

Dydrogesterone在人类肝脏代谢aldo-keto还原酶和细胞色素P450酶。

Xenobiotica。2016年10月,46 (10):868 - 74。doi: 10.3109 / 00498254.2015.1134852。Epub 2016年1月21日。

PubMed ID

26796435 (在PubMed

]

文摘

1。的新陈代谢dydrogesterone研究在人类肝细胞溶质(HLC)和人类肝脏微粒体(高)。酶参与新陈代谢dydrogesterone被确定,估计他们的相对贡献。2。Dydrogesterone间隙明显高于HLC比高。主要的活性代谢物20 alpha-dihydrodydrogesterone (20 alpha-dhd)只有在HLC生产。3所示。的形成20 alpha-dhd胞质aldo-keto还原酶1 c (AKR1C)确认isoenzyme-specific AKR抑制剂。4所示。使用重组表达人细胞色素P450 (CYP)同功酶,dydrogesterone被证明被CYP3A4和CYP2C19新陈代谢转化。 5. A clear contribution of CYP3A4 to microsomal metabolism of dydrogesterone was demonstrated with HLM and isoenzyme-specific CYP inhibitors, and confirmed by a significant correlation between dydrogesterone clearance and CYP3A4 activity. 6. Contribution of CYP2C19 was shown to be clearly less than CYP3A4 and restricted to a small group of human individuals with very high CYP2C19 activity. Therefore, it is expected that CYP2C19 genetic variations will not affect dydrogesterone pharmacokinetics in man. 7. In conclusion, dydrogesterone metabolism in the liver is dominated primarily by cytosolic enzymes (particularly AKR1C) and secondarily by CYP3A4, with the former exclusively responsible for 20alpha-DHD formation.

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药物酶

药物	酶	类	生物	药理作用	行动
Dydrogesterone	细胞色素P450 3 a4	蛋白质	人类	没有	底物	细节