Sofosbuvir

索磷布韋
Mechanism of action:
Sofosbuvir 是一種 C 型肝炎病毒 NS5B RNA 依賴型 RNA 聚合酶抑制劑(NS5B RNA-dependent RNA polymerase inhibitor)。Sofosbuvir 進入肝細胞後,經多步驟酵素作用轉化為其活性形式 GS-461203(uridine triphosphate 類似物)。GS-461203 會被病毒的 NS5B 聚合酶誤認為是 UTP,摻入正在合成的病毒 RNA 中,導致 RNA 生成中斷,使病毒基因體無法完成複製。
Reference(s):
1. Asselah T et al. (2014). Sofosbuvir for the treatment of hepatitis C virus. Expert Opin Pharmacother.
2. Fung A et al. (2014). Efficiency of incorporation and chain termination determines the inhibition potency of 2'-modified nucleotide analogs against hepatitis C virus polymerase. Antimicrob Agents Chemother.
3. Molina JM et al. (2015). Sofosbuvir plus ribavirin for treatment of hepatitis C virus in patients co-infected with HIV (PHOTON-2): a multicentre, open-label, non-randomised, phase 3 study. Lancet.
