elsulfavirine + dolutegravir

Elsulfavirine + dolutegravir is an oral, fixed-dose combination antiretroviral therapy comprising two distinct small molecule agents: elsulfavirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI), and dolutegravir, an integrase strand transfer inhibitor (INSTI). - **Elsulfavirine** acts by binding non-competitively to reverse transcriptase, inhibiting HIV-1 replication by preventing the transcription of viral RNA into DNA. - **Dolutegravir** targets the HIV integrase enzyme by binding to its active site and blocking the strand transfer step necessary for integration of viral DNA into the host genome, thereby preventing viral replication[2][4][5][6][8][10]. This combination is being developed/considered for the treatment of HIV-1 infection, aiming to simplify therapy and improve tolerability by leveraging the two drug classes' distinct mechanisms and resistance profiles. As of September 2025, elsulfavirine + dolutegravir is an investigational combination; elsulfavirine is not globally approved but has been granted regulatory approval in Russia (as standalone elsulfavirine), while dolutegravir is widely approved and used in multiple fixed-dose combination products for HIV-1 treatment.