Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2014 Mar 18:7:73-84.
doi: 10.2147/IDR.S40168. eCollection 2014.

Long-term efficacy and safety of raltegravir in the management of HIV infection

Michelle D Liedtke  1 , C Ryan Tomlin  1 , Staci M Lockhart  1 , Misty M Miller  1 , R Chris Rathbun  1
Affiliations
Review

Long-term efficacy and safety of raltegravir in the management of HIV infection

Michelle D Liedtke et al. Infect Drug Resist. .

Abstract

Raltegravir is an integrase strand-transfer inhibitor approved for the treatment of HIV infection. It was the first medication in a novel class of antiretroviral agents to be approved for use in the United States in 2007. Raltegravir exhibits potent activity against wild-type HIV-1, but resistance development has been noted through three different pathways. It is metabolized primarily through uridine diphosphate glucuronosyltransferase 1A1 and has a single inactive glucuronide metabolite. Raltegravir is not a substrate, inhibitor, or inducer of cytochrome P450 enzymes and exhibits low potential for drug-drug interactions; however, strong uridine diphosphate glucuronosyltransferase 1A1 inhibitors or inducers can alter the pharmacokinetics of raltegravir. It is well tolerated, and the most commonly reported adverse effects include headache, nausea, and diarrhea. Serious adverse effects with raltegravir are rare but include rhabdomyolysis and severe skin and hypersensitivity reactions. It has been approved for use in both treatment-naïve and treatment-experienced patients and is a preferred first-line agent in both United States and European HIV treatment guidelines. Although initial approval was granted on 48-week data, 5-year clinical data have recently been published. This article reviews the data supporting long-term efficacy and safety of raltegravir in the treatment of HIV infection.

Keywords: INSTI; Isentress®; antiretroviral; integrase inhibitor.

PubMed Disclaimer

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. NME drug and new biologic approvals in 2007 [webpage on the Internet] Silver Spring, MD: US Food and Drug Administration; [Accessed October 31, 2013]. [updated February 10, 2009]. Available from: http://www.fda.gov/drugs/developmentapprovalprocess/howdrugsaredeveloped....
    1. US Food and Drug Administration . FDA approves new combination pill for HIV treatment for some patients [press release] Silver Spring, MD: US Food and Drug Administration; 2012. [Accessed October 31, 2013]. [August 27; updated August 29, 2012]. Available from: http://www.fda.gov/news-events/newsroom/pressannouncements/ucm317004.htm.
    1. US Food and Drug Administration . FDA approves new drug to treat HIV infection [press release] Silver Spring, MD: US Food and Drug Administration; 2013. [Accessed October 31, 2013]. [August 12; updated August 13, 2013]. Available from: http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm364744.htm.
    1. US Food and Drug Administration . Isentress (raltegravir) indication extended for the treatment of HIV-1 infection in treatment-naïve patients [press release] Silver Spring, MD: US Food and Drug Administration; [Accessed October 31, 2013]. [updated July 13, 2009]. Available from: http://www.fda.gov/forconsumers/byaudience/forpatientadvocates/hivandaid....
    1. US Food and Drug Administration . FDA expands use of HIV drug Isentress to children and adolescents [press release] Silver Spring, MD: US Food and Drug Administration; 2011. [Accessed October 31, 2013]. [December 21]. Available from: http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm284473.htm.