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What is the most important information I should know about rilpivirine?
Rilpivirine is an experimental non-nucleoside reverse transcriptase inhibitor (NNRTI) being developed by Tibotec, a biotechnology company in Belgium. It has not yet been evaluated by the U.S. Food and Drug Administration (FDA) for use by people living with HIV.
What is rilpivirine?
Rilpivirine is in a category of HIV medicines called non-nucleoside reverse transcriptase inhibitors (NNRTIs). Rilpivirine prevents HIV from entering the nucleus of healthy T-cells. This prevents the cells from producing new virus and decreases the amount of virus in the body.
The correct dose for rilpivirine has not yet been determined. Preliminary experiments suggest that the drug can be taken by mouth once a day. The developer is also experimenting with a long-lasting formulation of rilpivirine that may allow for once-monthly dosing.
Like other NNRTIs, rilpivirine might interact with other medications, including those used to treat HIV. It is important that your personal physician and/or the research nurse or study investigator be aware of all drugs you are taking, including those you buy without a prescription.
It is expected that rilpivirine, when combined with two NRTIs, will have strong activity against HIV in people who have never taken an NNRTI in the past.
It is not yet known if rilpivirine will work against strains of HIV that are already resistant to currently available NNRTIs. All of the currently marketed NNRTIs, except Intelence (etravirine), are highly cross-resistant to each other. Test tube data suggest that rilpivirine might be effective against strains of HIV that are at least partly resistant to any of the approved drugs. But this cannot be determined until information from clinical trials is made available.
Rilpivirine has completed a 96-week phase IIb clinical trial. The dose selected for further study is 25mg, and larger phase III studies are either planned or under way. It is primarily being studied for use in people who are new to antiretroviral therapy.
Tibotec has announced it is going to work with Gilead Sciences to coformulate rilpivirine with Gilead's Truvada (tenofovir plus emtricitabine) into a single pill.
What about drug interactions?
There have not yet been studies demonstrating which other drugs may interact with rilpivirine. Studies to help determine this are planned or ongoing.
What is known about side effects?
Among the rilpivirine-treated patients in the 96-week study discussed above, approximately 20% of patients experienced nausea, compared to 18% of those taking Sustiva. Central nervous system effects—such as dizziness, somnolence, and vertigo—were significantly more common in the Sustiva group (53%) compared to the rilpivirine groups (33%). Rash was also less likely to occur among those taking any dose of rilpivirine (8%) compared to those receiving Sustiva (19%).
At higher doses, rilpivirine was found to disturb the heart's rhythm, a syndrome called QT-prolongation. It was for this reason that a low dose (25mg) was selected to move forward in development. The 25mg dose was no more likely than Sustiva to cause heart rhythm disturbances.
Who should not take rilpivirine?
It is not known whether rilpivirine will harm an unborn baby. It is very important to treat HIV/AIDS during pregnancy to reduce the risk of infecting your baby. Talk to your doctor about your treatment options.
It is not known whether rilpivirine passes into breast milk and what effect it may have on a nursing baby. To prevent transmission of the virus to uninfected babies, it is recommended that HIV-positive mothers not breast-feed.
Where can I learn more about clinical trials of rilpivirine?
If you would like to find out if you are eligible for any clinical trials that include rilpivirine, there is an interactive web site run by ACRIA, the AIDS Community Research Initiative of America.
Another useful service for finding clinical trials is AIDSinfo.nih.gov, a site run by the U.S. National Institutes of Health. They have "health information specialists" you can talk to at their toll-free number at 1-800-HIV-0440 (1-800-448-0440).
Last Revised: July 22, 2009
This content is written by the editorial team at AIDSmeds.com.
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rilpivirine
belongs to a class of anti-HIV drugs called 
Check My Meds
Like other NNRTIs, rilpivirine might interact with other medications, including those used to treat HIV. It is important that your personal physician and/or the research nurse or study investigator be aware of all drugs you are taking, including those you buy without a prescription.
It is not known whether rilpivirine will harm an unborn baby. It is very important to treat HIV/AIDS during pregnancy to reduce the risk of infecting your baby. Talk to your doctor about your treatment options.
It is not known whether rilpivirine passes into breast milk and what effect it may have on a nursing baby. To prevent transmission of the virus to uninfected babies, it is recommended that HIV-positive mothers not breast-feed.