top of page
The Sound of Evolution
Dolutegravir
Mechanism of action:
Dolutegravir is an integrase strand transfer inhibitor. Dolutegravir binds to the divalent metal ions (Mg²⁺ or Mn²⁺) at the active site of viral integrase, preventing integrase from binding to viral DNA and completing the strand transfer reaction. As a result, viral DNA cannot be integrated into the host chromosome, and the integration step of the viral replication cycle is blocked.
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.
bottom of page