Intelence (etravirine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Etravirine, an antiretroviral agent, is a human immunodeficiency virus (HIV) nonnucleoside reverse transcriptase inhibitor (NNRTI).
Etravirine, a diarylpyrimidine human immunodeficiency virus (HIV) nonnucleoside reverse transcriptase inhibitor (NNRTI), inhibits replication of HIV type 1 (HIV-1) by interfering with viral RNA- and DNA-directed polymerase activities of reverse transcriptase. Etravirine is highly active against wild-type HIV-1 and has been active against some clinical HIV-1 isolates resistant to some other commercially available NNRTIs (delavirdine, efavirenz, nevirapine). Etravirine appears to have a different resistance profile than other NNRTIs and certain single mutations that result in class resistance to other NNRTIs may not necessarily result in resistance to etravirine.
However, cross-resistance can occur between etravirine and other commercially available NNRTIs (delavirdine, etravirine, nevirapine, rilpivirine), and is expected in patients who have virologic failure while receiving a regimen that contains etravirine.
The absolute oral bioavailability of etravirine is unknown. Following oral administration in adults, peak plasma concentrations are attained within approximately 2.5-4 hours. Food enhances etravirine bioavailability; systemic exposure is 50% lower if the drug is administered under fasting conditions compared with following a meal.
The effect of food on etravirine bioavailability was studied using various meals (standard, light, enhanced-fiber, high-fat); the magnitude of the food effect is similar with all meal types. Distribution of etravirine into compartments other than plasma (e.g., CSF, genital tract secretions) has not been evaluated. Etravirine crosses the placenta and has been detected in cord blood.
Based on limited data, etravirine has been shown to be present in human breast milk. Etravirine is 99.9% bound to protein, principally albumin and alpha 1-acid glycoprotein.
Etravirine is metabolized principally in the liver by cytochrome P-450 (CYP) isoenzymes 3A, 2C9, and 2C19. In cell culture, the major metabolites of etravirine are at least 90% less active than the parent drug against wild-type HIV. Following oral administration of a single etravirine dose in adults, the majority (93.7%) of the dose is eliminated in feces as unchanged etravirine (81.2-86.4%).
Up to 1.2% of the dose is eliminated in urine as metabolites. Etravirine is not likely to be removed by hemodialysis or peritoneal dialysis. The mean terminal elimination half-life of etravirine in adults is about 41 hours.
The pharmacokinetics of etravirine have not been studied in patients with renal impairment; alterations are not expected because renal clearance is minimal. The pharmacokinetics of etravirine are not altered in patients with mild or moderate hepatic impairment (Child-Pugh Class A or B); data are not available regarding patients with severe hepatic impairment (Child-Pugh Class C). Clearance of etravirine may be reduced in HIV-infected patients coinfected with hepatitis B virus (HBV) and/or hepatitis C virus (HCV).
Studies in geriatric individuals up to 77 years of age did not identify any substantial differences in etravirine pharmacokinetics relative to younger adults. In pediatric patients 2 years to less than 18 years of age weighing at least 10 kg, weight-based etravirine dosage results in etravirine systemic exposures similar to those reported in adults receiving 200 mg twice daily.
USES: Etravirine is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life.
This medication is usually prescribed to people who have taken other HIV medications (such as efavirenz, nevirapine, delavirdine) that did not work well enough to control their HIV. Etravirine is known as a non-nucleoside reverse transcriptase inhibitor (NNRTI). It blocks the virus from growing and infecting more cells.
Etravirine is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, continue to take all HIV medications exactly as prescribed by your doctor. Use an effective barrier method (latex or polyurethane condoms/dental dams) during sexual activity as directed by your doctor.
Do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details.
Generic name: etravirine
Pronunciation: (et-ra-VIR-een)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Intelence
Indications
The following indications are listed for Intelence:
- Hiv Infection
Also known as: Human Immunodeficiency Virus Disease, Human Immunodeficiency Virus Infection.
Dosing
No dosing information is available for this tab.
Etravirine is administered orally twice daily following a meal.
Etravirine tablets should be swallowed whole with a liquid (e.g., water) and should not be chewed.
For patients unable to swallow tablets whole, the dose of etravirine tablets may be placed in 5 mL of water (enough water to cover the tablets) and stirred until a uniform, milky dispersion occurs. Add 15 mL (1 tablespoon) of liquid; water may be used, but orange juice or milk may improve taste. Do not use carbonated beverages or warm (>40degreesC) water. The dispersion should be consumed immediately; to ensure consumption of the entire dose, the glass should be rinsed several times with water, orange juice, or milk and each rinse swallowed.
Store etravirine tablets at 25degreesC (excursions permitted between 15-30degreesC). Store in the original bottle. Keep the bottle tightly closed in order to protect from moisture. Do not remove the desiccant pouches.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Concomitant use of etravirine and other drugs may result in potentially significant drug interactions, some of which may lead to loss of therapeutic effect of the concomitant drug or etravirine and possible development of resistance. Such drug interactions may also result in potentially clinically significant adverse reactions from greater exposure of etravirine or other concomitant drugs.
Consider the potential for drug interactions prior to and during etravirine therapy and review concomitant medications during therapy.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects (>=2%) of moderate to severe intensity occurring at a higher rate than placebo in adults are rash and peripheral neuropathy.
The most common adverse effects (>=2%) of pediatric patients are rash and diarrhea.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of etravirine have not been established in pediatric patients younger than 2 years of age. Five HIV-infected subjects from 1 year to less than 2 years of age were enrolled in the TMC125-C234/IMPAACT P1090 study. Etravirine exposure in these pediatric subjects was lower than that reported in HIV-infected adults.
Safety, efficacy, and pharmacokinetics of etravirine have been evaluated in antiretroviral-experienced pediatric patients 2 years to less than 18 years of age weighing at least 10 kg. Adverse effects reported in pediatric patients in a clinical study after 24 weeks of etravirine therapy were similar to those reported in adults (e.g., rash, diarrhea), although rash was reported more frequently in pediatric patients than in adults. Postmarketing cases of Stevens-Johnson syndrome have been reported in pediatric patients treated with etravirine.
The Antiretroviral Pregnancy Registry (APR) monitors pregnancy outcomes in women exposed to etravirine during pregnancy. Clinicians are encouraged to register patients in the APR by calling 800-258-4263 or visiting https://www.apregistry.com/.
Etravirine has been evaluated in a limited number of women during pregnancy. In animal studies, etravirine was not associated with adverse developmental effects at exposures equivalent to those at the maximum recommended human dose.
Based on prospective reports from the APR of 116 live births following exposure to etravirine-containing antiretroviral regimens during pregnancy, the number of birth defects in live births for etravirine was 1 out of 66 with first trimester exposure and 0 out of 38 with second/third trimester exposure.
Based on limited data, etravirine has been shown to be present in human breast milk. There are no data on the effects on the breastfed infant or the effects of etravirine on milk production.
The HHS perinatal HIV transmission guideline provides updated recommendations on infant feeding. The guideline states that patients with HIV should receive evidence-based, patient-centered counseling to support shared decision making about infant feeding. During counseling, patients should be informed that feeding with appropriate formula or pasteurized donor human milk from a milk bank eliminates the risk of postnatal HIV transmission to the infant. Additionally, achieving and maintaining viral suppression with antiretroviral therapy during pregnancy and postpartum reduces the risk of breastfeeding HIV transmission to <1%, but does not completely eliminate the risk. Replacement feeding with formula or banked pasteurized donor milk is recommended when patients with HIV are not on antiretroviral therapy and/or do not have a suppressed viral load during pregnancy (at a minimum throughout the third trimester), as well as at delivery.
In general, dosage selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Insufficient experience in patients 65 years of age and older to determine whether they respond differently than younger adults. Population pharmacokinetic analysis in HIV-infected subjects showed that etravirine pharmacokinetics are not considerably different within the age range (18-77 years) evaluated.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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