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Updated: Jun 27, 2026
05:46
Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Raltegravir: the first HIV integrase inhibitor
Jennifer Cocohoba1, Betty J Dong
1Department of Clinical Pharmacy, School of Pharmacy, University of California San Francisco, San Francisco, California 94143, USA. cocohobaj@pharmacy.ucsf.edu
Clinical Therapeutics
|November 19, 2008
Summary
Raltegravir, an integrase inhibitor, effectively suppresses HIV RNA in treatment-experienced adults with drug resistance. This antiretroviral agent is well-tolerated and offers a new option for managing complex HIV infections.
Area of Science:
- Infectious Diseases
- Virology
- Pharmacology
Background:
- New antiretroviral drugs enable immunologic recovery and virologic suppression in experienced HIV patients.
- Raltegravir is the first FDA-approved integrase inhibitor for treatment-experienced adults with viral resistance.
Purpose of the Study:
- To review the pharmacology, pharmacokinetics, pharmacodynamics, efficacy, tolerability, resistance profile, drug interactions, and dosing of raltegravir.
- To assess the role of raltegravir in managing HIV patients with resistance to other antiretrovirals.
Main Methods:
- Searched MEDLINE and International Pharmaceutical Abstracts (1964-2008) using terms: integrase, raltegravir, MK-0518.
- Extracted relevant data from clinical trials and review articles.
- Searched abstracts from major infectious disease conferences (1998-2007).
Main Results:
- Raltegravir inhibits HIV replication by blocking integrase strand-transfer.
- In Phase III trials, raltegravir significantly reduced HIV RNA in treatment-experienced patients with drug resistance (62.1% vs. 32.9%).
- Raltegravir was generally well-tolerated, with common side effects including diarrhea, nausea, and headache. No significant CYP450 interactions are expected, but coadministration with rifampin should be avoided.
Conclusions:
- Raltegravir is a potent and well-tolerated antiretroviral agent.
- It plays a crucial role in treating patients with resistance to other antiretrovirals.
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