Review of Therapeutics
Dolutegravir: A New Integrase Strand Transfer Inhibitor for the Treatment of HIV
Correction(s) for this article
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Dolutegravir: A new integrase strand transfer inhibitor for the treatment of HIV
- Volume 34Issue 6Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
- pages: 667-667
- First Published online: June 9, 2014
Bhavik M. Shah,
Jason J. Schafer,
Joseph A. DeSimone Jr.,
Corresponding Author
Bhavik M. Shah
Department of Pharmacy Practice, Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, Pennsylvania
Address for correspondence: Bhavik M. Shah, Jefferson School of Pharmacy, 901 Walnut Street, Suite 901, Philadelphia, PA 19107; e-mail: [email protected].Search for more papers by this authorJason J. Schafer
Department of Pharmacy Practice, Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, Pennsylvania
Search for more papers by this authorJoseph A. DeSimone Jr.
Division of Infectious Diseases, Jefferson Medical College, Thomas Jefferson University, Philadelphia, Pennsylvania
Search for more papers by this authorBhavik M. Shah,
Jason J. Schafer,
Joseph A. DeSimone Jr.,
Corresponding Author
Bhavik M. Shah
Department of Pharmacy Practice, Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, Pennsylvania
Address for correspondence: Bhavik M. Shah, Jefferson School of Pharmacy, 901 Walnut Street, Suite 901, Philadelphia, PA 19107; e-mail: [email protected].Search for more papers by this authorJason J. Schafer
Department of Pharmacy Practice, Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, Pennsylvania
Search for more papers by this authorJoseph A. DeSimone Jr.
Division of Infectious Diseases, Jefferson Medical College, Thomas Jefferson University, Philadelphia, Pennsylvania
Search for more papers by this authorAbstract
The first two integrase strand transfer inhibitors (INSTIs) approved for treatment of patients infected with human immunodeficiency virus (HIV) were raltegravir and elvitegravir. Both raltegravir and elvitegravir are now guideline-preferred agents as part of an antiretroviral regimen for treatment-naive patients. However, raltegravir is dosed twice/day. Elvitegravir is available in a single-tablet regimen and dosed once/day because it is administered with the pharmacokinetic booster cobicistat, a potent CYP3A4 inhibitor that can lead to clinically significant drug–drug interactions. In addition, raltegravir and elvitegravir have a low genetic barrier to resistance and are associated with cross-resistance. Dolutegravir is a new-generation INSTI administered once/day without a pharmacokinetic booster and can be coformulated in a single-tablet regimen. Phase III studies have demonstrated the efficacy and safety of dolutegravir for treatment-naive and treatment-experienced patients. Compared with other INSTIs, dolutegravir has a higher genetic barrier to resistance. Dolutegravir was approved by the U.S. Food and Drug Administration in August 2013 and joins raltegravir and elvitegravir as guideline-preferred agents for the management for HIV-infected treatment-naive patients.
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