Etravirine

• 4 - [ 6-amino -5-bromo -2 -(4- cyanphenylamino ) pyrimidin-4- yloxy ] -3,5- dimethylbenzonitril (IUPAC)
• TMC -125

J05AG04

Antiviral, non-nucleoside reverse transcriptase inhibitors

Non- competitive inhibition of reverse transcriptase

Template: Infobox chemical / molecular formula search available

Etravirine (trade name: Intelence ®, manufactured by Tibotec ) is a drug used to treat HIV and its later stages as part of a combination therapy for HIV.

Etravirine belongs to the class of non-nucleoside reverse transcriptase inhibitors ( NNRTI).

History

Intelence in combination with other antiretroviral agents has been approved for the treatment of infections with HIV-1 in patients already treated unsuccessfully in the U.S. in January 2008 and in the European Union in August 2008.

Pharmacology

Etravirine belongs to the class of non-nucleoside reverse transcriptase inhibitors ( NNRTI). The drug binds non- competitively to the reverse transcriptase of HIV-I, near the substrate binding site for nucleosides. Wherein the catalytically active site is blocked. It can bind only a few nucleosides and the polymerization is slowed significantly.

Pharmacokinetics

There is currently no data are available on the pharmacokinetics.

Side effects

In general, etravirine is well tolerated, however, occurred in some studies, the typical NNRTIs side effects are dizziness and rash on. The side effects but rarely led to discontinuation.

Mid-2009 gave the manufacturer announced that it has come with hepatic failure combined to a fatality as a result of Lyell 's syndrome and hypersensitivity reactions.

Resistance

In contrast to other NNRTIs etravirine has the advantage that it, in addition to very good effect is highly effective against the wild type, even against most NNRTI-resistant strains. In phase I / II studies, etravirine showed its high potency in lowering the viral load.