Elvitegravir (GS-9137)

What is elvitegravir?

• Elvitegravir is an experimental integrase inhibitor being developed by Gilead Sciences.
   
• After HIV’s genetic material is deposited inside a cell, its RNA must be converted (reverse transcribed) into DNA. A viral enzyme called integrase then helps to hide HIV’s DNA inside the cell’s DNA. Once this happens, the cell can begin producing genetic material for new viruses. Integrase inhibitors, such as elvitegravir, are designed to block the activity of the integrase enzyme and to prevent HIV DNA from entering healthy cell DNA.
   
• Elvitegravir will need to be used in combination with other drugs. Clinical trials will evaluate its effect in combination with other drugs, including those currently approved for the treatment of HIV.

What is already known about elvitegravir?

• The elvitegravir dose, to be explored in advanced Phase II and III clinical trials, will be 150mg once daily, combined with 100mg Norvir (ritonavir). Norvir is used to boost elvitegravir in the bloodstream, making it more effective against HIV.
   
•  Elvitegravir, especially when combined with Norvir, 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.
   
• Elvitegravir holds promise for HIV-positive patients who have taken other anti-HIV drugs in the past. Because elvitegravir targets HIV differently than currently available drugs, chances are that most people living with the virus—regardless of their treatment history—will likely benefit from using elvitegravir.
   
• Phase II studies of elvitegravir in people who are treatment experienced have been completed. Phase III studies in treatment experienced patients are ongoing. A phase II study of elvitegravir in people who have never taken antiretroviral therapy is underway. This study will also be evaluated a boosting agent in place of Norvir, currently called GS9350.

What about drug interactions?

• Studies on potential interactions between elvitegravir and other drugs have not yet been reported, but are planned and ongoing.

What is known about side effects?

• Very little is known about the side effects of elvitegravir. However, in the 278-patient study, side effects after 16 weeks of treatment were similar in the elvitegravir groups and the control group, meaning that no additional short-term side effects associated with elvitegravir use were documented.
   
• Additional studies evaluating the short- and long-term safety of elvitegravir are planned and ongoing.

Who should not take elvitegravir?

•  It is not known whether elvitegravir 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 elvitegravir 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 elvitegravir?

• If you would like to find out if you are eligible for any clinical trials that include elvitegravir, 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).