What is the other name for etravirine?
The other, and most common, name for the generic drug etravirine is its brand name, Intelence®. In medical and research settings, it may also be referred to by its abbreviation, ETR, or its investigational code, TMC125. Understanding the different names for this medication is crucial for proper communication between patients and healthcare providers. While 'etravirine' refers to the active pharmaceutical ingredient, 'Intelence®' is the proprietary name given by the manufacturer Janssen. The availability of both brand-name and generic forms allows for different treatment options, though both contain the same active compound.
The Pharmacology of Etravirine (Intelence®)
Etravirine belongs to the class of medications known as non-nucleoside reverse transcriptase inhibitors (NNRTIs). It is considered a second-generation NNRTI, distinguishing it from older drugs in the same class, such as nevirapine and efavirenz. The core of its mechanism involves targeting a crucial viral enzyme: HIV-1 reverse transcriptase.
The HIV virus relies on reverse transcriptase to convert its RNA into DNA, a necessary step for viral replication within human cells. Etravirine works by binding non-competitively to a specific site on this enzyme, which indirectly deactivates its catalytic site. This action effectively prevents the virus from replicating and reduces the viral load in the blood. The key difference in etravirine's molecular structure, which includes four flexible pivoting bonds, allows it to adapt to conformational changes in the binding pocket of the enzyme, even when resistance mutations develop. This molecular flexibility gives it a higher genetic barrier to resistance compared to first-generation NNRTIs, making it a valuable option for patients with pre-existing NNRTI resistance.
Therapeutic Use and Indications
Etravirine (Intelence®) is not a standalone treatment but is used in combination with other antiretroviral (ARV) medicines to treat human immunodeficiency virus type 1 (HIV-1) infection. It is primarily indicated for patients who are treatment-experienced, meaning they have taken HIV medicines in the past and may have developed resistance to previous therapies. The FDA has approved its use in adults and pediatric patients aged 2 years and older who weigh at least 10 kg. Its ability to overcome resistance to first-generation NNRTIs, such as the common K103N mutation, is a significant clinical advantage. Clinical trials have demonstrated its effectiveness when used as part of an optimized background regimen, but not alone, in patients with treatment failure and genotypic resistance. For this reason, treatment history and resistance testing are critical before including Intelence® in an antiretroviral regimen.
Dosage and Administration
Proper administration of Intelence® is vital for its effectiveness. It comes in 100 mg and 200 mg tablets and should be taken twice daily following a meal. Taking it with food significantly increases its absorption into the body, as fasting has been shown to reduce systemic exposure by approximately 50%. The type of food eaten does not significantly impact absorption.
For patients unable to swallow the tablets whole, they can be dispersed in a liquid. The process is as follows:
- Add the tablets to a small amount of water (about 1 teaspoon).
- Stir until a milky mixture forms.
- Add a larger amount of liquid (about 1 tablespoon), such as water, orange juice, or milk, to improve taste. Avoid warm or carbonated beverages.
- Drink the mixture immediately.
- Rinse the glass with more liquid and swallow the contents to ensure the full dose is taken.
Side Effects and Drug Interactions
Like many medications, etravirine can cause side effects, with rash being one of the most common, occurring in up to 10% of patients in clinical trials. While typically mild, some cases of severe, life-threatening skin reactions, including Stevens-Johnson syndrome, have been reported. Other potential side effects include gastrointestinal issues like nausea and diarrhea, as well as neurological symptoms such as dizziness and headache. Immune reconstitution syndrome, a condition where the immune system fights previously hidden infections after starting HIV treatment, and changes in body fat distribution have also been reported.
Etravirine can interact with many other drugs through its effect on cytochrome P450 (CYP) enzymes, including inducing CYP3A4 and inhibiting CYP2C9 and CYP2C19. Significant interactions may occur with:
- Herbal supplements like St. John's wort
- Certain antibiotics (e.g., rifampin)
- Some antifungals (e.g., voriconazole)
- Specific seizure medications (e.g., carbamazepine)
- Certain erectile dysfunction medications (e.g., sildenafil)
Patients should always inform their healthcare provider of all medications and supplements they are taking to manage these potential interactions effectively.
Comparison: Etravirine vs. First-Generation NNRTIs
| Feature | Etravirine (Intelence®) | First-Generation NNRTIs (e.g., Efavirenz, Nevirapine) |
|---|---|---|
| Genetic Barrier to Resistance | High. Its flexible structure allows activity against many NNRTI-resistant strains. | Low. Resistance can be quickly developed with single mutations (e.g., K103N). |
| Molecular Structure | Flexible diarylpyrimidine compound. | Inflexible chemical structure. |
| Primary Use | Treatment-experienced patients with confirmed resistance to first-generation NNRTIs. | Can be used in treatment-naive and treatment-experienced patients, but with greater risk of resistance. |
| Common Side Effects | Rash, gastrointestinal issues, dizziness, fatigue. | Rash, CNS side effects (e.g., abnormal dreams, dizziness) more common with efavirenz, hepatotoxicity with nevirapine. |
| Dosing Frequency | Twice daily (200 mg). | Varies (e.g., efavirenz once daily). |
Conclusion
In conclusion, the generic name for Intelence® is etravirine. As a second-generation NNRTI, etravirine provides an essential treatment option for individuals with HIV-1, particularly those who have developed resistance to older NNRTI drugs. Its unique molecular structure gives it a higher genetic barrier to resistance, enhancing its therapeutic value in combination antiretroviral therapy. Proper dosage, administration with food, and careful management of potential drug interactions are crucial for maximizing its efficacy and safety. While not a cure, Intelence® plays a vital role in helping patients manage their HIV infection and live longer, healthier lives. For comprehensive prescribing information, refer to official resources like MedlinePlus.
