|What is dolutegravir?
- Dolutegravir, previously referred to by its code number S/GSK 1249572 (GSK-572), is an experimental integrase inhibitor being developed by ViiV Healthcare in collaboration with Japan-based Shionogi & Co.
- 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 dolutegravir, are designed to block the activity of the integrase enzyme and to prevent HIV DNA from entering healthy cell DNA.
- Dolutegravir 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 dolutegravir?
- Dolutegravir dosing has not been finalized. For treatment-experienced individuals, notably those who have HIV with resistance to the first-generation integrase inhibitors Isentress (raltegravir) or elvitegravir, dolutegravir will probably need to be taken twice a day. For people starting HIV treatment for the first time, once-daily dosing may be possible. Either way, dolutegravir can be taken either with or without food and doesn't need to be used with a boosting agent, such as low-dose Norvir (ritonavir).
- Dolutegravir 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.
- Dolutegravir holds promise for HIV-positive patients who are either starting HIV treatment for the first time or have used other HIV drugs, including Isentress or elvitegravir, in the past. In a Phase II study, approximately 75 percent of people with evidence of HIV resistance to Isentress were able to reduce their viral loads to undetectable while using twice-daily dolutegravir in combination with other HIV drugs, at least one of which was also active against the virus.
- A Phase III clinical trial program for people living with HIV with resistance to first-generation integrase inhibtors is set to begin at the end of 2011 or the beginning of 2012. An expanded access program is also be developed to provide the drug on an experimental basis to those who need it.
What about drug interactions?
- Studies on potential interactions between dolutegravir and other drugs have not yet been reported, but are planned and ongoing.
What is known about side effects?
- Like other intergrase inhibitors, dolutegravir has been well tolerated in clinical trials completed thus far. The most common side effect in a Phase II study involving treatment-experienced patients was diarrhea.
- Additional studies evaluating the short- and long-term safety of dolutegravir are planned and ongoing.
Who should not take dolutegravir?
- It is not known whether dolutegravir 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 dolutegravir 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 dolutegravir?
- If you would like to find out if you are eligible for any clinical trials that include dolutegravir, visit ClinicalTrials.gov, a site run by the U.S. National Institutes of Health. The site has information about all HIV-related clinical studies in the United States. For more info, you can call their toll-free number at 1-800-HIV-0440 (1-800-448-0440) or email firstname.lastname@example.org.