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Emtricitabine

恩曲他濱
Mechanism of action:
Emtricitabine 是一種核苷類反轉錄酶抑制劑(nucleoside reverse transcriptase inhibitor), 為胞苷(cytidine)類似物。當 emtricitabine 進入細胞後,會經宿主細胞的酵素磷酸化,轉換為有活性的 emtricitabine triphosphate。Emtricitabine triphosphate 會與 dCTP(deoxycytidine triphosphate)競爭,有機會被 HIV 反轉錄酶誤納入正在合成的病毒 DNA 中,造成 DNA 合成終止,使病毒無法完成反轉錄並進行後續複製。
Reference(s):
1. Shockcor JP et al. (1996). HPLC-NMR identification of the human urinary metabolites of (−)-cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine, a nucleoside analogue active against human immunodeficiency virus (HIV). Xenobiotica.
2. Valade E et al. (2014). Population pharmacokinetics of emtricitabine in HIV-1-infected adult patients. Antimicrob Agents Chemother.
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