Etravirine
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]
Overview
Etravirine (ETR,[1] brand name Intelence, formerly known as TMC125) is a drug used for the treatment of HIV. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Etravirine works by reducing the amount of HIV and increasing the number of CD4 or T cells in the blood. Unlike the currently available agents in the class, resistance to other NNRTIs does not seem to confer resistance to etravirine.[2] Etravirine is marketed by Tibotec, a subsidiary of Johnson & Johnson. In January 2008, the Food and Drug Administration approved its use for patients with established resistance to other drugs, making it the 30th anti-HIV drug approved in the United States and the first to be approved in 2008.[3] It was also approved for use in Canada on April 1, 2008.[4]
Category
Antiretroviral
US Brand Names
INTELENCE®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against HIV-1 replication. It binds to retroviral reverse transcriptase and blocks the RNA-dependent and DNA-dependent DNA polymerase activities. It does not require intracellular phosphorylation for antiviral activity.
References
- ↑ "Appendix A: Key to Acronyms". Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents. Department of Health and Human Services.
- ↑ Stellbrink HJ (October 2007). "Antiviral drugs in the treatment of AIDS: what is in the pipeline?". Eur. J. Med. Res. 12 (9): 483–95. PMID 17933730.
- ↑ "FDA Approves HIV Drug Etravirine". Associated Press. January 18, 2008.[dead link]
- ↑ "First New NNRTI in Nearly a Decade to Benefit Canadians with HIV/AIDS" (PDF) (Press release). Janssen-Ortho Inc. 2008-04-01. Retrieved 2008-07-09.