Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretrovirals to specifically treat human immunodeficiency virus type 1 (HIV-1). It is a diarylpyrimidine derivative.
- Mechanism
- Curator reviewed · 4 references
Rilpivirine is a non-competitive NNRTI that binds to reverse transcriptase. Its binding results in the blockage of RNA and DNA- dependent DNA polymerase activities, like HIV-1 replication. It does not present activity against human DNA polymerases α, β and γ. Rilpivirine's flexible structure around the aromatic rings allows the adaptation to changes in the non-nucleoside RT binding pocket, reducing the likelihood of viral mutations conferring resistance.
- Primary indication
- Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm3.Curator reviewed · 4 structured indications
- Formula / weight
- C22H18N6 · 366.4185 g/mol (avg)
- First approval
- Canada, 2014 · United States, 2011 · European Union, 2016
- Code names
- R-278474 · TMC-278
- Brand names
Resolves to
YIBOMRUWOWDFLG-ONEGZZNKSA-NSMILESCC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC2=CC=C(C=C2)C#N)=N1What you can answer from here — as of September 13, 2026
Which drugs share a target with Rilpivirine, and which of those have an active Phase 3 trial?
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