Intelence
Approved for treatment-experienced adults and children 2 years and older weighing at least 22 pounds (10 kg). See the package insert for specific weight-based dosing in children. Also available in 25 mg and 100 mg tablets.
Take missed dose as soon as possible, as long as it is at least 12 hours before your next dose. Do not double up on your next dose. People unable to swallow pills (Intelence tablets are “chalky”) can dissolve tablets in one teaspoon (5 mL) of water or at least enough liquid to cover the medication; stir well until the water turns milky, add more water if desired—or use a small amount (about one tablespoon) of orange juice or milk as an alternative, always placing tablets in water first. Avoid warm (over 104° F) or carbonated beverages. Drink immediately, rinse the glass several times with water, orange juice or milk and completely swallow the rinse each time to make sure the entire dose is taken.
- Generic and brand name available for 600 mg. Generic available only for 50 mg and 200mg oral tablets.
- See package insert for more complete information on potential side effects and interactions.
intelence.com
(800) JANSSEN (526-7736)
etravirine generic: 100 mg, 120 tablets: $1,609.11/month
Intelence: 200 mg, 60 tablets: $1,762.22/month
etravirine generic: 200 mg, 60 tablets: $1,609.11/month
JO-ANN JOSE, MD, MPH:
Intelence (etravirine) is not very commonly used. It’s a fantastic little drug, but it’s really difficult to manage because of all the side effect potential and the low barrier to resistance, and it’s still twice daily.
If Intelence is taken in combination with a protease inhibitor, the PI must be boosted with Norvir. Intelence should be avoided with Tivicay unless administered with one of the following combinations: Reyataz/Norvir, Prezista/Norvir or Kaletra. Fostemsavir levels may be decreased by 50%, so caution is recommended. If using fostemsavir with ritonavir-boosted darunavir, use with caution and monitor for side effects due to the potential for increased levels of fostemsavir. Co-administration with lenacapavir has not been studied but is not recommended as it may impair lenacapavir efficacy. Taking it in combination with Selzentry requires a Selzentry dose adjustment to 600 mg twice daily when used without a boosted PI, and 150 mg twice daily when used with a boosted PI. Do not take Intelence with carbamazepine, phenobarbital, phenytoin, rifapentine, rifampin or the herb St. John’s wort. Use with caution when combined with the antifungals Diflucan (fluconazole) and Vfend (voriconazole). Dose adjustments of the antifungals ketoconazole, itraconazole and posaconazole may be needed. Some statins may require monitoring or dose adjustment. Monitor the effectiveness of Coumadin (warfarin) and adjust dose as needed based on clinical response. Alternatives to clopidogrel should be considered when used with Intelence. Alternatives to clarithromycin—such as azithromycin—should be considered for treatment of MAC. Lower Valium dose may be needed. Use caution with systemic dexamethasone or consider alternatives. Intelence can be taken with rifabutin (Mycobutin) 300 mg daily; however, it should be avoided by people who are also taking a boosted PI. Concentrations of some antiarrhythmics may be decreased when co-administered with Intelence. Intelence and antiarrhythmics should be co-administered with caution. Drug concentration monitoring is recommended, if available. Intelence can be safely combined with methadone or buprenorphine with additional monitoring for potential signs of withdrawal. Intelence can also be safely combined with Viagra, Cialis and Levitra, though a dosage adjustment of Viagra may be necessary. Interaction with Harvoni has not been studied, but based on the metabolism, a clinically significant interaction is not expected. Taking with Zepatier is not recommended. Tell your provider or pharmacist about all medications, herbals and supplements you are taking or thinking of taking, prescribed or not, as there are other drug interactions which are not listed here.
Generally well tolerated, but most common side effects of moderate to severe intensity in adults include rash as well as numbness, tingling or pain in the hands or feet. Discontinue Intelence immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise [general ill feeling], fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia or angioedema). Levels of liver enzymes called transaminases should be monitored. Rash is associated with all of the current NNRTIs, but if you develop a rash from Intelence, you may still be able to take one of the other NNRTIs. In pediatric patients ages 2–18, the frequency, type and severity of adverse drug reactions were comparable to those observed in adult subjects, except for rash, which was observed more frequently. In ages 6–18, rash of moderate intensity or greater (Grade 2 or greater) was reported more frequently in girls than boys (20.3% versus 5.4%). Half of the children 2–6 years old experienced rash of any grade, whereas rash of moderate intensity or greater was reported in 10% of adults. Rash is typically described as mild to moderate, pruritic (itchy), with pimple-like skin eruptions. For pediatric patients, rash usually appeared in the second week of therapy and generally resolved within a week. Discuss discontinuing etravirine if fever, blistering or severe reaction occurs.
For people who have had virologic failure on an NNRTI-containing regimen, do not use Intelence in combination with a nucleoside backbone alone. Although taking once daily is not FDA approved, some providers have prescribed Intelence once daily (two of the 200 mg tablets) based on clinical trials that showed once-daily Intelence was not inferior to Sustiva-based regimens. In Europe, it is approved as a once-daily medication. Once-daily dosing may improve adherence. Although the HHS recommendation for Intelence specifies drug resistance strains before taking it, the drug label does not—you do not need to have drug resistance before taking Intelence. The TRIO study reported the combination of Intelence with Prezista/Norvir and Isentress in highly treatment-experienced people was successful in getting many people to undetectable. Some people complain of hard-to-swallow, large chalky pills; see dissolving instructions in dose section or package insert. For individuals with HIV-2, primarily found in West Africa but also present in other countries, an NNRTI would not be recommended, as HIV-2 is inherently resistant to NNRTIs. The pharmacokinetics (PK) of etravirine are not significantly altered during pregnancy, so no dosage adjustment is necessary. The PK data demonstrated exposure to total etravirine was generally higher during pregnancy compared with postpartum levels. Etravirine is known to have a variable (moderate to high) level of transfer across the human placenta, although insufficient data exist to evaluate the effects on a fetus. Pregnant individuals can voluntarily enroll in the Antiretroviral Pregnancy Registry through their provider; GO TO apregistry.com.
JUAN MICHAEL PORTER II:
Intelence must be taken with food, though one of my friends said, “Why take it at all?” It’s only for treatment-experienced people. But even then, there are better options. Especially because of its chalky taste. But when it first came out, it was considered a great saver because it worked and got people off of some truly terrible drug combinations.