Intelence (Etravirine)

Etravirine is used as part of antiretroviral therapy for HIV‑1 infection.

• HIV‑1 infection (treatment‑experienced): Used in combination with other antiretroviral agents to achieve viral suppression in patients who have received prior therapy.
• HIV‑1 infection (resistant virus): Provides an option for patients with resistance to other NNRTIs.
• HIV‑1 infection (adults and adolescents): Approved for use in individuals aged 12 years and older as part of a complete regimen.

• Etravirine binds to a specific allosteric site on the HIV‑1 reverse transcriptase enzyme, distinct from the nucleoside binding site. This binding inhibits the enzyme's RNA‑dependent DNA polymerase activity, preventing conversion of viral RNA into DNA and thereby blocking viral replication within infected cells.

Etravirine may cause a range of adverse reactions, most of which are mild to moderate.

Common Side Effects

• Rash: mild to moderate skin eruptions.
• Nausea: occasional upset stomach.
• Diarrhea: loose stools.
• Headache: transient head discomfort.
• Fatigue: feeling of tiredness.
• Insomnia: difficulty sleeping.

Serious or Rare Side Effects

• Stevens‑Johnson syndrome: severe skin reaction requiring immediate medical attention.
• Hepatic dysfunction: elevated liver enzymes or hepatitis.
• Severe hypersensitivity: including anaphylaxis.
• Mood changes: depression or suicidal thoughts.
• Cardiovascular events: rare cases of arrhythmia.
• Visual disturbances: blurred vision or eye pain.

When prescribing Intelence, consider the following precautions.

• Pregnancy: safety not established; use only if potential benefit justifies the risk.
• Breastfeeding: unknown safety; advise against nursing while on therapy.
• Liver function: assess hepatic status before initiation and monitor periodically.
• Drug resistance: evaluate prior antiretroviral exposure to avoid ineffective therapy.
• Drug interactions: review concomitant medications for CYP3A4 modulators.
• Store at ambient temperature: keep tablets in the original container, protect from moisture and excessive heat.

Etravirine interacts with several medications; careful management is required.

Major Interactions (Avoid)

• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin): may markedly reduce etravirine plasma concentrations.
• Protease inhibitors boosted with ritonavir: can increase etravirine levels, raising risk of toxicity.

Moderate Interactions (Monitor Closely)

• Other NNRTIs (e.g., efavirenz, nevirapine): may affect plasma levels of both agents.
• Hormonal contraceptives: etravirine may reduce contraceptive efficacy.
• Antacids containing aluminum or magnesium: may decrease absorption if taken simultaneously.
• Statins metabolized by CYP3A4 (e.g., simvastatin): monitor for increased statin exposure.