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Dolutegravir

多替拉韋

Mechanism of action:

Dolutegravir 是一種整合酶抑制劑（integrase strand transfer inhibitor）。Dolutegravir 可與病毒的整合酶活性位點的二價金屬離子（Mg²⁺ 或 Mn²⁺）結合，阻止整合酶與病毒 DNA 結合並完成股轉移（strand transfer）反應，導致病毒 DNA 無法整合入宿主染色體，使病毒複製週期中的整合步驟受阻。

​Reference(s):

1. Min S et al. (2010). Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. Antimicrob Agents Chemother. 


2. Lenz JC et al. (2011). S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges. Expert Opin Investig Drugs.

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