Etravirine
- Atc Codes:J05AG04
- CAS Codes:269055-15-4
- PHARMGKB ID:269055-15-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Intelence; Belgium: Intelence; Bulgaria: Intelence; Czech Republic: Intelence; Denmark: Intelence; Estonia: Intelence; Finland: Intelence; France: Intelence; Germany: Intelence; Greece: Intelence; Hungary: Intelence; Ireland: Etravirine; Italy: Intelence; Latvia: Intelence; Lithuania: Intelence; Malta: Intelence; Netherlands: Intelence; Poland: Intelence; Portugal: Intelence; Romania: Intelence; Slovakia: Intelence; Slovenia: Intelence; Spain: Intelence; Sweden: Intelence; UK: Intelence.
North America
Canada: Intelence; USA: Intelence.
Latin America
Argentina: Intelence.
Drug combinations
Chemistry
Etravirine: C~20~H~15~BrN~6~O. Mw: 435.28. (1) Benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-; (2) 4-[[6-Amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile. CAS-269055-15-4 (2005).
Pharmacologic Category
Antiretrovirals; Non-nucleoside Reverse Transcriptase Inhibitors. (ATC-Code: J05AG04).
Mechanism of action
A synthetic antiretroviral agent, etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Has activity against HIV-1 by binding to reverse transcriptase. It consequently blocks the RNA-dependent and DNA-dependent DNA polymerase activities, including HIV-1 replication. It does not require intracellular phosphorylation for antiviral activity.
Therapeutic use
Etravirine is used in conjunction with other antiretroviral agents for treatment of HIV-1 infection in previously treated adults exhibiting viral replication with documented NNRTI resistance.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women, and use during pregnancy is not recommended unless other alternatives are not available. Not recommended for use during lactation.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Severe and potentially life-threatening skin reactions, including Stevens-Johnson syndrome, hypersensitivity reaction, and erythema multiforme, reported rarely. Rash of mild to moderate intensity may also occur. Possible redistribution or accumulation of body fat. Patients may develop an inflammatory response to indolent or residual opportunistic infections. High potential for CYP interactions. Not recommended for use with other NNRTIs, unboosted protease inhibitors, high-dose ritonavir, tipranavir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir, enzyme-inducing anticonvulsants, clarithromycin, St. John’s wort, rifampin, or rifapentine. Not for use in treatment-naïve patients, or experienced patients without evidence of viral mutations conferring resistance to NNRTIs and protease inhibitors.