Drug interactions

Interactions with protease inhibitors complicate regimens containing etravirine. This is an especially important issue for a second-line NNRTI that may be used in third-line regimens with protease inhibitors.

Etravirine cannot be co-administered with boosted tipranavir/ritonavir (Aptivus), boosted fosamprenavir (Lexiva), full-dose ritonavir (Norvir 600mg), boosted atazanavir (Reyataz), unboosted protease inhibitors, and other NNRTIs.

Etravirine blood levels increase by 17% when prescribed with lopinavir (Kaletra). This combination may be used, but should be administered with caution. 

Because etravirine is such a potent inducer of the cytochrome p450 CYP3A4 pathway, it greatly speeds up the metabolism of the CCR5 antagonist maraviroc (Celsentri, Selzentry). Co-administration can reduce total maraviroc concentrations over a 12-hour period by 53% (AUC12) and peak levels of maraviroc (Cmax) by 60%.

Therefore, if an individual isn't also taking a potent CYP3A4 inhibitor such as a protease inhibitor, the recommended clinical dose for maraviroc alongside etravirine is 600mg twice daily. However, if maraviroc is being dosed alongside etravirine and darunavir together, a dose reduction to 150mg twice daily is necessary. Data showed no effect of maraviroc on etravirine pharmacokinetics, so no dose adjustment of etravirine is necessary.

Etravirine cannot be given with carbamazepine, phenobarbital, phenytoin, rifabutin (if part of a protease inhibitor/ritonavir containing-regimen), rifampin, rifapentine, or St John's wort (Hypericum perforatum). It does not appear to affect blood levels of methadone. Etravirine may reduce levels of clopidogrel.

Etravirine should be used with caution alongside fluconazole or voriconazole, because these drugs have the potential to raise etravirine levels.

The efficacy of etravirine and/or its side-effect profile can change when given with inhibitors, inducers, or substrates of CYP3A4, CYP2C9, and CYP2C19. Further information on drug interactions is available at www.intelence-info.com.

Community Consensus Statement on Access to HIV Treatment and its Use for Prevention

Together, we can make it happen

We can end HIV soon if people have equal access to HIV drugs as treatment and as PrEP, and have free choice over whether to take them.

Launched today, the Community Consensus Statement is a basic set of principles aimed at making sure that happens.

The Community Consensus Statement is a joint initiative of AVAC, EATG, MSMGF, GNP+, HIV i-Base, the International HIV/AIDS Alliance, ITPC and NAM/aidsmap

This content was checked for accuracy at the time it was written. It may have been superseded by more recent developments. NAM recommends checking whether this is the most current information when making decisions that may affect your health.

NAM’s information is intended to support, rather than replace, consultation with a healthcare professional. Talk to your doctor or another member of your healthcare team for advice tailored to your situation.