Company:

Tibotec

Antiretroviral (non-nucleoside reverse transcriptase inhibitor)

Etravirine 100mg; tabs.

HIV-1 infection, in combination with other antiretrovirals, in treatment-experienced adults with evidence of viral replication and HIV-1 strains resistant to an NNRTI and other antiretrovirals.

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It works by blocking RNA-dependent and DNA-dependent DNA polymerase activity of HIV-1.

The approval for this drug was based on analyses of two randomized, double-blind, placebo-controlled studies that were conducted in clinically advanced, three-class antiretroviral treatment-experienced adults. These studies compared etravirine + background regimen to placebo + background regimen. All subjects received darunavir/ritonavir as part of their background regimen and at least two other investigator-selected antiretrovirals. Subjects were treatment-experienced HIV-1 infected patients with plasma HIV-1 RNA levels of >5000copies/mL while on a stable antiretroviral regimen for at least 8 weeks; they had at least one NNRTI resistance-associated mutation and three or more specific protease inhibitor (PI) mutations. Virologic response was defined as an undetectable viral load (<50copies/mL of viral RNA) at 24 weeks. Pooled results for the two studies indicated that, at 24 weeks, 59.8% of the patients given etravirine + background regimen were responders, compared to 40.2% for the placebo group. At week 24, 74% of the etravirine-treated group had a viral load of <400copies/mL, compared to 51.5% of the placebo group. Studies are continuing.

Take after meals. May disperse tabs in water and drink. 200mg twice daily.

Not recommended.

Severe hepatic impairment. Pregnancy (Cat.B). Nursing mothers: not recommended.

Concomitant tipranivir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir, PIs without ritonavir (eg, atazanavir, fosamprenavir, nelfinavir, indinavir), ritonavir (600mg twice daily), NNRTIs (eg, efavirenz, nevirapine, delavirdine): not recommended. Avoid rifampin, rifapentine, St. John's wort, carbamazepine, phenytoin, phenobarbital; rifabutin with darunavir/ritonavir. May affect, or be affected by, drugs that induce or inhibit, or that are substrates of, CYP3A4, CYP2C9, CYP2C19 (eg, azole antifungals, immunosuppressants); monitor. Potentiated by lopinavir/ritonavir. May antagonize antiarrhythmics (eg, amiodarone, bepridil, quinidine) (monitor), sildenafil. May potentiate warfarin, diazepam. May be antagonized by anticonvulsants, dexamethasone. Clarithromycin (consider azithromycin for treating MAC). Adjust statin dose (except pravastatin, rosuvastatin). Rifabutin (adjust dose with etravirine monotherapy). See literature.

Rash (may be serious, eg, Stevens-Johnson syndrome, hypersensitivity, erythema multiforme; discontinue if occurs), GI upset, fat redistribution, immune reconstitution syndrome, lab value changes (eg, lipids, blood glucose).

Report pregnant patients exposed to etravirine by calling (800) 258-4263.

Tabs—120

3/6/08