Intelence

Generic Name: Etravirine
Class: Nonnucleoside Reverse Transcriptase Inhibitors
VA Class: AM800
Chemical Name: 4-{[6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl]oxy}-3,5-dimethylbenzonitrile
Molecular Formula: C₂₀H₁₅BrN₆O
CAS Number: 269055-15-4

Introduction

Antiretroviral; nonnucleoside reverse transcriptase inhibitor (NNRTI).^{1 2 3 5}

Uses for Intelence

Treatment of HIV Infection

Treatment of HIV-1 infection in conjunction with other antiretrovirals.¹

Used only in treatment-experienced (previously treated) adults with evidence of HIV-1 replication and HIV-1 strains resistant to an NNRTI and other antiretroviral agents.^{1 2 3}

Selection of etravirine for use in antiretroviral regimens should be guided by viral resistance testing (when available) and the individual’s prior antiretroviral treatment.¹

Concomitant use of etravirine and another NNRTI (e.g., delavirdine, efavirenz, nevirapine) is not recommended.^{1 5}

A regimen that includes etravirine and nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs) as the only antiretroviral agents is not recommended in adults who experienced virologic failure while receiving a previous NNRTI-containing regimen.¹ There is some evidence that such regimens may be less effective in these patients than regimens that include HIV protease inhibitors (PIs).⁵

Do not use in initial antiretroviral regimens.^{5 9} Risks versus benefits not established in treatment-naive adults^{1 5} or in pediatric patients.¹

Intelence Dosage and Administration

Administration

Oral Administration

Administer orally after a meal.¹ Food enhances bioavailability of etravirine.^{1 11} (See Food under Pharmacokinetics.)

Swallow tablets whole; do not chew.

For patients unable to swallow tablets, the tablets may be administered as a dispersion in water.¹ To prepare a dispersion containing 200 mg, place two 100-mg tablets in a glass containing water and stir until a uniform dispersion occurs.¹ Consume the dispersion promptly; rinse the glass with water several times and swallow each rinse to ensure consumption of the entire dose.¹

Dosage

Must be given in conjunction with other antiretrovirals.¹

Adults

Treatment of HIV Infection

Oral

200 mg twice daily.^{1 5}

Special Populations

Hepatic Impairment

Dosage adjustment not necessary in patients with mild or moderate hepatic impairment (Child-Pugh class A or B);^{1 5 12} data not available in patients with severe hepatic impairment (Child-Pugh class C).^{1 5} (See Special Populations under Pharmacokinetics.)

Dosage adjustment not necessary in HIV-infected patients coinfected with hepatitis B virus (HBV) and/or hepatitis C virus (HCV).¹ (See Special Populations under Pharmacokinetics.)

Renal Impairment

Dosage adjustment not necessary.^{1 5} (See Special Populations under Pharmacokinetics.)

Geriatric Patients

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.¹

Cautions for Intelence

Contraindications

• 
  

  Manufacturer states none known.¹

  
  

Warnings/Precautions

Sensitivity Reactions

Dermatologic and Hypersensitivity Reactions

Severe, potentially life-threatening and fatal skin reactions reported.¹ Reactions include Stevens-Johnson syndrome, toxic epidermal necrolysis, and erythema multiforme.¹ Hypersensitivity reactions with rash and systemic symptoms also reported.¹

If severe hypersensitivity reactions (e.g., severe rash or rash with fever, malaise, fatigue, muscle or joint pain, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema) occur, immediately discontinue etravirine and initiate appropriate therapy.¹ Monitor clinical status and liver transaminase concentrations.¹

Rash of mild to moderate intensity also reported;^{1 2 3} generally occurs within first few weeks of therapy and resolves with continued therapy (median duration 12–16 days).^{1 2 3}

Manufacturer states that history of rash while receiving other NNRTIs does not appear to increase the risk for etravirine-related rash.¹

Adipogenic Effects

Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, facial wasting, breast enlargement, and general cushingoid appearance.¹

Immune Reconstitution Syndrome

During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]); this may necessitate further evaluation and treatment.¹

Specific Populations

Pregnancy

Category B.¹

Antiretroviral Pregnancy Registry at 800-258-4263.¹

Some experts state safety and pharmacokinetic data insufficient to recommend etravirine in pregnant women.⁷

Lactation

Not known whether distributed into human milk.¹

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.^{1 7}

Pediatric Use

Safety and efficacy not established in pediatric patients.¹

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults.¹

Common Adverse Effects

Rash, peripheral neuropathy.¹

Interactions for Intelence

Metabolized by CYP isoenzymes 3A, 2C9, and 2C19.^{1 5} Induces CYP3A;¹ inhibits 2C9 and 2C19.¹ Inhibits P-glycoprotein.¹

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Potential pharmacokinetic interactions with drugs that induce or inhibit CYP isoenzymes 3A, 2C9, or 2C19 with possible altered metabolism of etravirine.^{1 5}

Potential pharmacokinetic interaction with drugs that are substrates for CYP isoenzymes 3A, 2C9, or 2C19 with possible altered metabolism of the substrate.^{1 5}

Drugs Affected by P-glycoprotein Transport

Potential pharmacokinetic interaction with drugs that are substrates for P-glycoprotein.¹

Specific Drugs

Drug	Interaction	Comments
Abacavir	No in vitro evidence of antagonistic antiretroviral effects 1
Antiarrhythmics (amiodarone, disopyramide, flecainide, systemic lidocaine, mexiletine, propafenone, quinidine)	Possible decreased antiarrhythmic agent concentrations1	Use caution; monitor concentrations of the antiarrhythmic agent1 5
Anticoagulants, oral	Possible increased warfarin concentrations1 5	Monitor INR; adjust warfarin dosage if needed1 5
Anticonvulsants (carbamazepine, phenobarbital, phenytoin)	Possible decreased etravirine concentrations and decreased antiretroviral efficacy1 5	Concomitant use not recommended;1 5 consider alternative anticonvulsants5
Antifungals, azoles (fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole)	Fluconazole: Substantially increased etravirine concentrations; no change in fluconazole concentrations1 5 Itraconazole: Possible increased etravirine concentrations and decreased itraconazole concentrations1 5 Ketoconazole: Possible increased etravirine concentrations and decreased ketoconazole concentrations1 5 Posaconazole: Possible increased etravirine concentrations; no change in posaconazole concentrations1 5 Voriconazole: Increased etravirine and voriconazole concentrations 1 5	Fluconazole: Dosage adjustment not needed for either drug; use caution because of limited safety data regarding increased etravirine concentrations1 5 Itraconazole: Dosage adjustment of itraconazole may be needed depending on other concomitantly administered drugs;1 5 consider monitoring itraconazole concentrations5 Ketoconazole: Dosage adjustment of ketoconazole may be needed depending on other concomitantly administered drugs1 5 Posaconazole: Dosage adjustment of posaconazole may be needed depending on other concomitantly administered drugs1 Voriconazole: Use caution because of limited safety data regarding increased etravirine concentrations; manufacturer of etravirine states that dosage adjustment not needed for either drug;1 some experts state that dosage adjustment of voriconazole may be needed depending on other concomitantly administered drugs and that consideration should be given to monitoring voriconazole concentrations5
Antimycobacterials (rifabutin, rifampin, rifapentine)	Rifabutin: Decreased concentrations of etravirine and rifabutin1 5 Rifampin: Substantially decreased etravirine concentrations possible1 5 Rifapentine: Substantially decreased etravirine concentrations possible1 5	Rifabutin: Recommended dosage of rifabutin is 300 mg daily in patients receiving etravirine in a regimen that does not include a ritonavir-boosted PI;1 5 rifabutin not recommended in patients receiving etravirine in a regimen that includes ritonavir-boosted darunavir, ritonavir-boosted lopinavir, or ritonavir-boosted saquinavir1 5 Rifampin: Concomitant use not recommended1 5 Rifapentine: Concomitant use not recommended1 5
Atazanavir	Atazanavir or ritonavir-boosted atazanavir: Increased etravirine concentrations; decreased atazanavir concentrations and possible decreased antiretroviral efficacy1 5 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use of atazanavir (with or without low-dose ritonavir) not recommended1 5
Benzodiazepines (alprazolam, diazepam)	Alprazolam: Data not available5 Diazepam: Possible increased diazepam concentrations1 5	Alprazolam: Monitor for therapeutic effects of alprazolam if used concomitantly5 Diazepam: Consider need to decrease diazepam dosage1 5
Clarithromycin	Increased etravirine concentrations; decreased clarithromycin concentrations and increased concentrations of the major metabolite (14-hydroxyclarithromycin)1 5	Consider an alternative to clarithromycin (e.g., azithromycin) for treatment of MAC; 14-hydroxyclarithromycin has reduced activity against MAC1 5
Clopidogrel	Possible decreased concentrations of the active metabolite of clopidogrel1	Consider alternatives to clopidogrel1
Corticosteroids (dexamethasone)	Dexamethasone: Possible decreased etravirine concentrations and decreased antiretroviral efficacy1 5	Caution; consider alternatives to dexamethasone, especially when long-term corticosteroid use anticipated1 5
Darunavir	Ritonavir-boosted darunavir: Decreased etravirine AUC; no change in darunavir concentrations 1 2 3 5 Safety and efficacy of ritonavir-boosted darunavir and etravirine established in phase 3 clinical studies1 2 3 5 No in vitro evidence of antagonistic antiretroviral effects1	Ritonavir-boosted darunavir: Dosage adjustment not needed1 5
Delavirdine	Possible increased etravirine concentrations1	Concomitant use not recommended1 5
Didanosine	No in vitro evidence of antagonistic antiretroviral effects1
Digoxin	Possible increased digoxin concentrations; no change in etravirine concentrations1	If digoxin and etravirine are initiated at the same time, initiate digoxin at the lowest dosage1 If etravirine is initiated in a patient already receiving digoxin, dosage adjustment of either drug not needed1 Monitor serum digoxin concentrations and adjust digoxin dosage to achieve desired clinical effect1
Efavirenz	Decreased etravirine concentrations1 5 and loss of antiretroviral efficacy1	Concomitant use not recommended1 5
Emtricitabine	No in vitro evidence of antagonistic antiretroviral effects1
Enfuvirtide	No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustment not needed1
Estrogens or progestins	Hormonal contraceptives: Slight increase in ethinyl estradiol concentrations; no change in norethindrone concentrations1 5	Dosage adjustment not needed with oral contraceptives containing ethinyl estradiol and norethindrone1 5
Fosamprenavir	Fosamprenavir or ritonavir-boosted fosamprenavir: Substantial increase in amprenavir concentrations1 5 No in vitro evidence of antagonistic antiretroviral effects with amprenavir1	Concomitant use of fosamprenavir (with or without low-dose ritonavir) not recommended1 5
Histamine H2-receptor antagonists	Ranitidine: Decreased etravirine concentrations1	Ranitidine: Dosage adjustment not needed1
HMG-CoA reductase inhibitors (atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin, simvastatin)	Atorvastatin: Decreased atorvastatin concentrations; no change in etravirine concentrations1 5 Fluvastatin: Possible increased fluvastatin concentrations; no change in etravirine concentrations1 5 Lovastatin: Possible decreased lovastatin concentrations1 5 Pravastatin: Pharmacokinetic interaction not expected1 5 Rosuvastatin: Pharmacokinetic interaction not expected1 5 Simvastatin: Possible decreased simvastatin concentrations1 5	Atorvastatin: Usual dosages of etravirine and atorvastatin can be used; however, may need to adjust atorvastatin dosage based on clinical response1 5 (do not exceed maximum recommended dosage)5 Fluvastatin: May need to adjust fluvastatin dosage1 5 Lovastatin: May need to adjust lovastatin dosage based on clinical response1 5 (do not exceed maximum recommended dosage);5 if a ritonavir-boosted PI is included in the regimen, some experts recommend that lovastatin not be used5 Pravastatin: No dosage adjustment needed5 Rosuvastatin: No dosage adjustment needed5 Simvastatin: May need to adjust simvastatin dosage based on clinical response1 5 (do not exceed maximum recommended dosage);5 if a ritonavir-boosted PI is included in the regimen, some experts recommend that simvastatin not be used5
Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus)	Potential for decreased immunosuppressive agent concentrations1	Use with caution1
Indinavir	Indinavir (without low-dose ritonavir): Decreased indinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use of indinavir (without low-dose ritonavir) not recommended1 5
Lamivudine	No in vitro evidence of antagonistic antiretroviral effects 1
Lopinavir	Lopinavir/ritonavir: Decreased etravirine AUC and decreased lopinavir concentrations1 5 No in vitro evidence of antagonistic antiretroviral effects1	Because decrease in etravirine systemic exposure in patients receiving concomitant lopinavir/ritonavir is similar to that in patients receiving etravirine and concomitant ritonavir-boosted darunavir (a combination found to be safe and effective), manufacturer and some experts state that dosage adjustments not needed for either drug1 5
Maraviroc	Decreased maraviroc concentrations; no change in etravirine concentrations1 5 Maraviroc and ritonavir-boosted darunavir: Increased maraviroc concentrations5 No in vitro evidence of antagonistic antiretroviral effects1	Regimens that include maraviroc without a potent CYP3A inhibitor (e.g., ritonavir-boosted PI): Recommended dosage of maraviroc is 600 mg twice daily; dosage adjustment of etravirine not needed1 5 Regimens that include maraviroc and a potent CYP3A inhibitor (e.g., ritonavir-boosted PI): Recommended dosage of maraviroc is 150 mg twice daily; dosage adjustment of etravirine not needed1 5
Methadone	No change in methadone or etravirine concentrations1 5 8	Dosage adjustment not needed1 5 8
Nelfinavir	Nelfinavir (without low-dose ritonavir): Increased nelfinavir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use of nelfinavir (without low-dose ritonavir) not recommended1 5
Nevirapine	Decreased etravirine concentrations1 5 and loss of antiretroviral efficacy1	Concomitant use not recommended1 5
Paroxetine	No change in etravirine or paroxetine concentrations1	Dosage adjustment not needed1
Proton pump inhibitors	Omeprazole: Increased etravirine concentrations1	Omeprazole: Dosage adjustment not needed1
Raltegravir	No change in etravirine concentrations; slight decrease in raltegravir AUC and plasma concentrations1 10 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustment not needed for either drug1 5 10
Ritonavir	Full-dose ritonavir: Substantial decrease in etravirine concentrations and possible loss of antiretroviral efficacy1 No in vitro evidence of antagonistic antiretroviral effects 1	Full-dose ritonavir (600 mg twice daily): Concomitant use not recommended1 5 Low-dose ritonavir (usually 100 mg once or twice daily): Etravirine may be used concomitantly with certain ritonavir-boosted PI regimens (i.e., ritonavir-boosted darunavir, lopinavir/ritonavir, ritonavir-boosted saquinavir);1 concomitant use with ritonavir-boosted atazanavir, ritonavir-boosted fosamprenavir, or ritonavir-boosted tipranavir not recommended1 5
Saquinavir	Ritonavir-boosted saquinavir (saquinavir 1 g twice daily and ritonavir 100 mg twice daily): Decrease in etravirine AUC; no change in saquinavir plasma concentrations1 5 No in vitro evidence of antagonistic antiretroviral effects1	Because decrease in etravirine systemic exposure in patients receiving concomitant saquinavir is similar to that in patients receiving etravirine concomitantly with ritonavir-boosted darunavir (a combination found to be safe and effective), manufacturer and some experts state that dosage adjustments not needed for either drug1 5
Sildenafil	Decreased sildenafil concentrations1 5	Usual dosages of etravirine and sildenafil can be used; however, may need to alter dosage of sildenafil based on clinical effect1 5
Stavudine	No in vitro evidence of antagonistic antiretroviral effects1
St. John’s wort (Hypericum perforatum)	Possible substantially decreased etravirine concentrations and loss of antiretroviral efficacy1	Concomitant use not recommended1 5
Tenofovir	Decreased etravirine concentrations; no change in tenofovir concentrations1 No in vitro evidence of antagonistic antiretroviral effects1	Dosage adjustment not needed1
Tipranavir	Ritonavir-boosted tipranavir: Decreased etravirine concentrations and possible decreased antiretroviral efficacy; increased tipranavir concentrations1 5 No in vitro evidence of antagonistic antiretroviral effects1	Concomitant use of ritonavir-boosted tipranavir not recommended1 5
Zidovudine	No in vitro evidence of antagonistic antiretroviral effects1

Intelence Pharmacokinetics

Absorption

Bioavailability

Absolute oral bioavailability is unknown.¹

Following oral administration, peak plasma concentrations attained within approximately 2.5–4 hours.^{1 11}

Food

Systemic exposure is decreased by about 50% if etravirine is administered under fasting conditions compared with administration after a meal.^{1 11}

Effect of food on etravirine bioavailability was studied using various meals (standard, light, enhanced-fiber, high-fat);¹¹ magnitude of the food effect is similar with all meal types.^{1 11}

Distribution

Extent

Not known whether etravirine is distributed into human milk.¹

Distribution into compartments other than plasma (e.g., CSF, genital tract secretions) not evaluated.¹

Plasma Protein Binding

99.9%, principally albumin and alpha 1-acid glycoprotein.¹

Elimination

Metabolism

Metabolized principally in the liver by CYP isoenzymes 3A, 2C9, and 2C19.¹

In cell culture, the major metabolites are at least 90% less active than etravirine against wild-type HIV.¹

Elimination Route

Following oral administration of a single dose, the majority (93.7%) is eliminated in feces as unchanged etravirine (81.2–86.4%).¹ Up to 1.2% of the dose is eliminated in urine as metabolites.¹

Unlikely to be removed by hemodialysis or peritoneal dialysis.¹

Half-life

Mean terminal elimination half-life is about 41 hours.¹

Special Populations

Renal impairment: Pharmacokinetics not studied; alterations not expected because renal clearance is minimal.¹

Hepatic impairment: Pharmacokinetics not altered in patients with mild or moderate hepatic impairment (Child-Pugh class A or B);^{1 12} not studied in patients with severe hepatic impairment (Child-Pugh class C).¹

HIV-infected individuals coinfected with HBV and/or HCV: Reduced clearance reported.¹

Geriatric individuals: Studies in those up to 77 years of age indicate no substantial differences in pharmacokinetics relative to younger adults.¹

Pediatric patients: Pharmacokinetics not studied.¹

Pregnant patients: Pharmacokinetics not studied.¹

Stability

Storage

Oral

Tablets

25°C (may be exposed to 15–30°C).¹ Tight container; protect from moisture.¹ Dispense and store in original container; the desiccant should remain in the original bottle.¹

Actions and SpectrumActions

• 
  

  Inhibits replication of HIV-1 by interfering with viral RNA- and DNA-directed polymerase activities of reverse transcriptase.^{1 4}

  
  


• 
  

  Highly active against wild-type HIV-1; active against some clinical isolates resistant to other NNRTIs (delavirdine, efavirenz, nevirapine).^{1 3 4 5}

  
  


• 
  

  Different resistance profile than other NNRTIs; single mutations that result in class resistance to other NNRTIs do not necessarily result in resistance to etravirine.^{2 3 4 5}

  
  


• 
  

  Cross-resistance may occur between etravirine and other commercially available NNRTIs^{1 4 5} and is expected in patients who have virologic failure while receiving a regimen that contains etravirine.¹

  
  

Advice to Patients

• 
  

  Critical nature of compliance with HIV therapy.¹ Used in conjunction with other antiretrovirals; do not use for monotherapy.¹

  
  


• 
  

  Antiretroviral therapy is not a cure for HIV infection, and opportunistic infections still may occur.¹ HIV transmission via sexual contact or sharing needles is not prevented by antiretrovirals.¹

  
  


• 
  

  Importance of reading patient information provided by the manufacturer.¹

  
  


• 
  

  Advise patients to take etravirine as prescribed and not to alter or discontinue therapy without consulting their clinician.¹

  
  


• 
  

  Importance of taking etravirine twice daily after a meal.¹ Food enhances absorption of the drug;^{1 11} magnitude of the food effect is similar with all meal types (standard, light, enhanced-fiber, high-fat).^{1 11}

  
  


• 
  

  Advise patients to swallow the tablets whole with liquid (e.g., water).¹ Alternatively, disperse tablets in a glass of water and drink the liquid containing the dispersed etravirine tablets immediately, then rinse the glass with water several times and drink the rinse.¹

  
  


• 
  

  If a missed dose is remembered within 6 hours of the usually scheduled time, it should be taken after a meal as soon as possible and the next dose taken at the regularly scheduled time.¹ If missed dose is remembered >6 hours after the scheduled time, the dose should be omitted and the next dose taken at the regularly scheduled time.¹

  
  


• 
  

  Advise patients that severe and potentially life-threatening rash has occurred (usually within the first few weeks of etravirine therapy).¹ Importance of immediately contacting clinician if rash occurs.¹ Importance of immediately discontinuing etravirine and seeking medical care if rash associated with systemic symptoms (e.g., fever, generally ill feeling, extreme tiredness, muscle or joint aches, blisters, oral lesions, eye inflammation, swelling of the face, eyes, lips, or mouth, breathing difficulties, yellowing of the eyes or skin, dark or tea colored urine, pale colored stools, nausea, vomiting, loss of appetite, or right upper quadrant tenderness/pain) occurs.¹

  
  


• 
  

  Advise patients that redistribution/accumulation of body fat may occur with antiretroviral therapy, with as yet unknown long-term health effects.¹

  
  


• 
  

  Advise patients to contact their clinician if signs or symptoms of an infection occur.¹

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal products (e.g., St. John’s wort), and any concomitant illnesses.¹

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of advising patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Etravirine

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	100 mg	Intelence	Tibotec

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Intelence 100MG Tablets (CENTOCOR ORTHO BIOTECH PRODUCT): 120/$865.97 or 360/$2490.86

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions November 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Tibotec Therapeutics. Intelence (etravirine) tablets prescribing information. Raritan, NJ; 2010 Feb.

2. Madruga JV, Cahn P, Grinsztejn B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1 infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet. 2007; 370:29-38. [PubMed 17617270]

3. Lazzarin A, Campbell T, Clotet B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1 infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet. 2007; 370:39-48. [PubMed 17617271]

4. Vingerhoets J, Azijn H, Fransen E et al. TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J Virol. 2005; 79:12773-82. [PubMed 16188980]

5. US Department of Health and Human Services (HHS) Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. December 1, 2009. Updates available at the HHS HIV/AIDS Information Services (AIDSinfo) website.

6. Tibotec Therapeutics, Bridgewater, NJ: Personal communication.

7. US Department of Health and Human Services (HHS) Panel on Treatment of HIV-infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. May 24, 2010. Updates available at the HHS HIV/AIDS Information Services (AIDSinfo) website.

8. Schöller-Gyüre M, van den Brink W, Kakuda TN et al. Pharmacokinetic and pharmacodynamic study of the concomitant administration of methadone and TMC125 in HIV-negative volunteers. J Clin Pharmacol. 2008; 48:322-9.

9. Working Group on Antiretroviral Therapy and Medical Management of HIV-infected Children convened by the National Resource Center at the François-Xavier Bagnoud Center; UMDN, the Health Resources and Services Administration (HRSA), and the National Institutes of Health (NIH). Guidelines for the use of antiretroviral agents in pediatric HIV infection. February 23, 2009. Updates available at the US Department of Health and Human Services HIV/AIDS Information Services (AIDSinfo) website.

10. Anderson MS, Kakuda TN, Hanley W et al. Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects. Antimicrob Agents Chemother. 2008; 52:4228-32. [PubMed 18838586]

11. Schöller-Gyüre M, Boffito M, Pozniak AL et al. Effects of different meal compositions and fasted state on the oral bioavailability of etravirine. Pharmacotherapy. 2008; 28:1215-22. [PubMed 18823217]

12. Schöller-Gyüre M, Kakuda TN, De Smedt G et al. Effects of hepatic impairment on the steady-state pharmacokinetics of etravirine 200 mg BID: an open-label, multiple-dose, controlled Phase I study in adults. Clin Ther. 2010; 32:328-37. [PubMed 20206790]

More Intelence resources

• Intelence Side Effects (in more detail)
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• Intelence Drug Interactions
• Intelence Support Group
• 0 Reviews for Intelence - Add your own review/rating

• Intelence Prescribing Information (FDA)


• Intelence Consumer Overview


• Intelence Advanced Consumer (Micromedex) - Includes Dosage Information


• Intelence MedFacts Consumer Leaflet (Wolters Kluwer)


• Etravirine Professional Patient Advice (Wolters Kluwer)

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