Etravirin

Active substance for the treatment of HIV infection from the NNRTI substance class, which is also effective against previously NNRTI-resistant HIV strains and is not affected by the 100% cross-resistance between the previously approved non-nucleoside analogues RT inhibitors.

Good efficacy against HIV wild-type viruses and against resistant mutants, especially against classic NNRTI mutations such as K103N. The resistance barrier is apparently higher than for other NNRTIs, since, as a DAPY analogue, Etravirin can bind flexibly to the reverse transcriptase of HIV-1 through conformational changes. Mutations at the binding site of the enzyme can thus do less harm to the binding and hence the effect of this NNRTI than has been known with the NNRTIs available to date.

HIV-infected persons with limited treatment options after treatment failure against at least three classes of substances (at least 2 PIs, NRTI, NNRTI) or two classes (PI, NRTI) in the case of primary NNRTI resistance as well as at the start of treatment of non-existent virological suppression.

2 times/day 200 mg p.o.

Frequent: diarrhoea, headaches, drug exanthema (approx. 20%), itching, fatigue, visual disturbances, tiredness, dizziness and concentration difficulties, especially at the beginning of treatment.

Tipranavir, nevirapine and efavirenz significantly reduce the exposure to Etravirin and should therefore not be combined. Etravirin increases the exposure to fosamprenavir by about 70%. Dose adjustment of proton pump inhibitors, H2 blockers, methadone and contraceptive hormones is not necessary. Etravirin should not be used together with the following substances which are metabolized in the liver by similar metabolic pathways: midazolam, diazepam, triazepam, phenobarbital, phenytoin, carbamazepine, rifampicin, terfenadine and antiarrhythmics.

Intelence