Efavirenz is a non-nucleoside reverse transcriptase inhibitor used to treat HIV infection or prevent the spread of HIV. For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen.
- Mechanism
- Curator reviewed
Similar to zidovudine, efavirenz inhibits the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). Antiviral activity of efavirenz is dependent on intracellular conversion to the active triphosphorylated form. The rate of efavirenz phosphorylation varies, depending on cell type. It is believed that inhibition of reverse transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body. Even though human DNA polymerase is less susceptible to the pharmacologic effects of triphosphorylated efavirenz, this action may nevertheless account for some of the drug's toxicity.
- Primary indication
- For use in combination treatment of HIV infection (AIDS)Curator reviewed · 1 structured indication
- Formula / weight
- C14H9ClF3NO2 · 315.675 g/mol (avg)
- First approval
- Canada, 2004 · United States, 1998 · European Union, 2020
- Code names
- DMP 266 · L 743726
- Brand names
Resolves to
XPOQHMRABVBWPR-ZDUSSCGKSA-NSMILESFC(F)(F)[C@]1(OC(=O)NC2=C1C=C(Cl)C=C2)C#CC1CC1What you can answer from here — as of September 23, 2026
Which drugs share a target with Efavirenz, and which of those have an active Phase 3 trial?
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