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Intelence

Last reviewed on RxList: 6/27/2017
Intelence Side Effects Center

Last reviewed on RxList 6/27/2017

Intelence (etravirine) is an antiviral medication used with other medications to treat HIV, which causes the acquired immunodeficiency syndrome (AIDS). This drug is not a cure for HIV or AIDS, and it is usually given after other antiviral drugs have been tried unsuccessfully. Common side effects of Intelence include nausea, rash, numbness or tingly feeling in your hands or feet, dizziness, drowsiness, blurred vision, upset stomach, constipation, heartburn, dry mouth, unusual dreams, or changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

The recommended adult oral dose of Intelence is 200 mg (one 200 mg tablet or two 100 mg tablets) taken twice daily following a meal. Pediatric dose is based on body weight. Intelence may interact with blood thinners, clopidogrel, darunavir, lopinavir/ritonavir, dexamethasone, diazepam, cyclosporine, cholesterol medications, maraviroc, methadone, sildenafil, sirolimus, tacrolimus, antibiotics, antifungals, or heart rhythm medications. Many other medicines can interact with Intelence, or make it less effective. Tell your doctor all medications and supplements you use. During pregnancy, Intelence should be used only when prescribed. It is unknown if this medication passes into breast milk. Because breast milk can transmit HIV, do not breastfeed.

Our Intelence (etravirine) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Intelence Consumer Information

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

In rare cases, etravirine can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Stop taking etravirine and call your doctor at once if you have a serious side effect such as:

  • fever, chills, muscle weakness, joint or muscle pain, mouth sores, feeling very tired, or any other signs of new infection;
  • chest pain, feeling short of breath;
  • confusion, seizure;
  • urinating less than usual or not at all, swelling, rapid weight gain;
  • rapid heart rate, increased sweating, tremors, sleep problems (insomnia), feeling anxious or irritable;
  • severe diarrhea, unexplained weight loss, menstrual changes, impotence, loss of interest in sex;
  • swelling in your neck or throat (enlarged thyroid);
  • weakness or prickly feeling in your fingers or toes;
  • problems with balance or eye movement, trouble speaking or swallowing;
  • severe lower back pain, loss of bladder or bowel control;
  • nausea, upper stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • the first sign of any type of skin rash, no matter how mild; or
  • severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Less serious side effects may include:

  • numbness or tingly feeling in your hands or feet;
  • dizziness, drowsiness;
  • blurred vision;
  • upset stomach, constipation, heartburn, dry mouth;
  • unusual dreams; or
  • changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Intelence (Entravirine Tablets)

Intelence Professional Information

SIDE EFFECTS

The following adverse reactions are described in greater detail in other sections:

  • Severe skin and hypersensitivity reactions [see WARNINGS AND PRECAUTIONS].

Clinical Trials Experience: Adults

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety assessment is based on all data from 1203 subjects in the Phase 3 placebo-controlled trials, TMC125C206 and TMC125-C216, conducted in antiretroviral treatment-experienced HIV-1-infected adult subjects, 599 of whom received INTELENCE® (200 mg twice daily). In these pooled trials, the median exposure for subjects in the INTELENCE® arm and placebo arm was 52.3 and 51.0 weeks, respectively. Discontinuations due to adverse drug reactions (ADRs) were 5.2% in the INTELENCE® arm and 2.6% in the placebo arm.

The most frequently reported ADR at least Grade 2 in severity was rash (10.0%). Stevens-Johnson syndrome, drug hypersensitivity reaction and erythema multiforme were reported in less than 0.1% of subjects during clinical development with INTELENCE® [see WARNINGS AND PRECAUTIONS]. A total of 2.2% of HIV-1-infected subjects in Phase 3 trials receiving INTELENCE® discontinued due to rash. In general, in clinical trials, rash was mild to moderate, occurred primarily in the second week of therapy, and was infrequent after Week 4. Rash generally resolved within 1 to 2 weeks on continued therapy. The incidence of rash was higher in women compared to men in the INTELENCE® arm in the Phase 3 trials (rash ≥ Grade 2 was reported in 9/60 [15.0%] women versus 51/539 [9.5%] men; discontinuations due to rash were reported in 3/60 [5.0%] women versus 10/539 [1.9%] men) [see WARNINGS AND PRECAUTIONS]. Patients with a history of NNRTI-related rash did not appear to be at increased risk for the development of INTELENCE®-related rash compared to patients without a history of NNRTI-related rash.

Common Adverse Reactions

Clinical ADRs of moderate intensity or greater (greater than or equal to Grade 2) and reported in at least 2% of subjects treated with INTELENCE® and occurring at a higher rate compared to placebo (excess of 1%) are presented in Table 1. Laboratory abnormalities considered ADRs are included in Table 2.

Table 1: Treatment-Emergent Adverse Reactions* of at least Moderate Intensity† (Grades 2 to 4) in at least 2% of Adult Subjects in the INTELENCE® Treatment Groups and at a higher rate compared to placebo (excess of 1%)

System Organ Class, Preferred Term, % Pooled TMC125-C206 and TMC125-C216 Trials
INTELENCE® + BR
N=599
Placebo + BR
N=604
Nervous System Disorders
Peripheral neuropathy 4% 2%
Skin and Subcutaneous Tissue Disorders
Rash 10% 3%
N=total number of subjects per treatment group, BR=background regimen
* Includes adverse reactions at least possibly, probably, or very likely related to the drug.
† Intensities are defined as follows: Moderate (discomfort enough to cause interference with usual activity); Severe (incapacitating with inability to work or do usual activity).

Less Common Adverse Reactions

Treatment-emergent ADRs occurring in less than 2% of subjects (599 subjects) receiving INTELENCE® and of at least moderate intensity (greater than or equal to Grade 2) are listed below by body system:

Cardiac Disorders: myocardial infarction, angina pectoris, atrial fibrillation

Ear and Labyrinth Disorders: vertigo

Eye Disorders: blurred vision

Gastrointestinal Disorders: gastroesophageal reflux disease, flatulence, gastritis, abdominal distension, pancreatitis, constipation, dry mouth, hematemesis, retching, stomatitis

General Disorders and Administration Site Conditions: sluggishness

Hematologic Disorders: hemolytic anemia

Hepatobiliary Disorders: hepatic failure, hepatomegaly, cytolytic hepatitis, hepatic steatosis, hepatitis

Immune System Disorders: drug hypersensitivity, immune reconstitution syndrome

Metabolism and Nutrition Disorders: diabetes mellitus, anorexia, dyslipidemia

Nervous System Disorders: paraesthesia, somnolence, convulsion, hypoesthesia, amnesia, syncope, disturbance in attention, hypersomnia, tremor

Psychiatric Disorders: anxiety, sleep disorders, abnormal dreams, confusional state, disorientation, nervousness, nightmares

Renal and Urinary Disorders: acute renal failure

Reproductive System and Breast Disorders: gynecomastia

Respiratory, Thoracic and Mediastinal Disorders: exertional dyspnea, bronchospasm

Skin and Subcutaneous Tissue Disorders: night sweats, lipohypertrophy, prurigo, hyperhidrosis, dry skin, swelling face

Additional ADRs of at least moderate intensity observed in other trials were acquired lipodystrophy, angioneurotic edema, erythema multiforme and haemorrhagic stroke, each reported in no more than 0.5% of subjects.

Laboratory Abnormalities in Treatment-Experienced Patients

Selected Grade 2 to Grade 4 laboratory abnormalities that represent a worsening from baseline observed in adult subjects treated with INTELENCE® are presented in Table 2.

Table 2: Selected Grade 2 to 4 Laboratory Abnormalities Observed in Treatment-Experienced Subjects

Laboratory Parameter Preferred Term, % DAIDS Toxicity Range Pooled TMC125-C206 and TMC125-C216 Trials
INTELENCE® + BR
N=599
Placebo + BR
N=604
GENERAL BIOCHEMISTRY
Pancreatic amylase
Grade 2 > 1.5-2 x ULN 7% 8%
Grade 3 > 2-5 x ULN 7% 8%
Grade 4 > 5 x ULN 2% 1%
Lipase
Grade 2 > 1.5-3 x ULN 4% 6%
Grade 3 > 3-5 x ULN 2% 2%
Grade 4 > 5xULN 1% < 1%
Creatinine
Grade 2 > 1.4-1.8 x ULN 6% 5%
Grade 3 > 1.9-3.4 x ULN 2% 1%
Grade 4 > 3.4 x ULN 0% < 1%
HEMATOLOGY
Decreased hemoglobin
Grade 2 90-99 g/L 2% 4%
Grade 3 70-89 g/L < 1% < 1%
Grade 4 < 70 g/L < 1% < 1%
White blood cell count
Grade 2 1,500-1,999/mm³ 2% 3%
Grade 3 1,000-1,499/mm³ 1% 4%
Grade 4 < 1,000/mm³ 1% < 1%
Neutrophils
Grade 2 750-999/mm³ 5% 6%
Grade 3 500-749/mm³ 4% 4%
Grade 4 < 500/mm³ 2% 3%
Platelet count
Grade 2 50,000-99,999/mm³ 3% 5%
Grade 3 25,000-49,999/mm³ 1% 1%
Grade 4 < 25,000/mm³ < 1% < 1%
LIPIDS AND GLUCOSE
Total cholesterol
Grade 2 > 6.20-7.77 mmol/L 240-300 mg/dL 20% 17%
Grade 3 > 7.77 mmol/L > 300 mg/dL 8% 5%
Low density lipoprotein
Grade 2 4.13-4.9 mmol/L 160-190 mg/dL 13% 12%
Grade 3 >     4.9 mmol/L >     190 mg/dL 7% 7%
Triglycerides
Grade 2 5.65-8.48 mmol/L 500 -750 mg/dL 9% 7%
Grade 3 8.49-13.56 mmol/L 751 - 1200 mg/dL 6% 4%
Grade 4 > 13.56 mmol/L > 1200 mg/dL 4% 2%
Elevated glucose levels
Grade 2 6.95-13.88 mmol/L 161-250 mg/dL 15% 13%
Grade 3 13.89-27.75 mmol/L 251 - 500 mg/dL 4% 2%
Grade 4 > 27.75 mmol/L > 500 mg/dL 0% < 1%
HEPATIC PARAMETERS
Alanine amino transferase
Grade 2 2.6-5 x ULN 6% 5%
Grade 3 5.1-10 x ULN 3% 2%
Grade 4 > 10 x ULN 1% < 1%
Aspartate amino transferase
Grade 2 2.6-5 x ULN 6% 8%
Grade 3 5.1-10 x ULN 3% 2%
Grade 4 > 10 x ULN < 1% < 1%
ULN=Upper Limit of Normal, BR=background regimen

Patients Co-infected With Hepatitis B and/or Hepatitis C Virus

In Phase 3 trials TMC125-C206 and TMC125-C216, 139 subjects (12.3%) with chronic hepatitis B and/or hepatitis C virus co-infection out of 1129 subjects were permitted to enroll. AST and ALT abnormalities occurred more frequently in hepatitis B and/or hepatitis C virus co-infected subjects for both treatment groups. Grade 2 or higher laboratory abnormalities that represent a worsening from baseline of AST, ALT or total bilirubin occurred in 27.8%, 25.0% and 7.1% respectively, of INTELENCE®-treated co-infected subjects as compared to 6.7%, 7.5% and 1.8% of non-co-infected INTELENCE®-treated subjects. In general, adverse events reported by INTELENCE®treated subjects with hepatitis B and/or hepatitis C virus co-infection were similar to INTELENCE®-treated subjects without hepatitis B and/or hepatitis C virus co-infection.

Clinical Trials Experience: Pediatric Subjects (6 years to less than 18 years of age)

The safety assessment in children and adolescents is based on the Week 24 analysis of the single-arm, Phase 2 trial TMC125-C213 in which 101 antiretroviral treatment-experienced HIV-1 infected subjects 6 years to less than 18 years of age and weighing at least 16 kg received INTELENCE® in combination with other antiretroviral agents [see Clinical Studies]. The frequency, type and severity of adverse drug reactions in pediatric subjects were comparable to those observed in adult subjects, except for rash which was observed more frequently in pediatric subjects. The most common adverse drug reactions in at least 2% of pediatric subjects were rash and diarrhea. Rash was reported more frequently in female subjects than in male subjects (rash ≥ Grade 2 was reported in 13/64 [20.3%] females versus 2/37 [5.4%] males; discontinuations due to rash were reported in 4/64 [6.3%] females versus 0/37 [0%] males).Rash (greater than or equal to Grade 2) occurred in 15% of pediatric subjects. In the majority of cases, rash was mild to moderate, of macular/papular type, and occurred in the second week of therapy. Rash was self-limiting and generally resolved within 1 week on continued therapy. The safety profile for subjects who completed 48 weeks of treatment was similar to the safety profile for subjects who completed 24 weeks of treatment.

Postmarketing Experience

The following events have been identified during postmarketing use of INTELENCE®. Because these events are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Immune System Disorders: Severe hypersensitivity reactions including DRESS and cases of hepatic failure have been reported [see WARNINGS AND PRECAUTIONS].

Musculoskeletal and Connective Tissue Disorders: rhabdomyolysis

Skin and Subcutaneous Tissue Disorders: Fatal cases of toxic epidermal necrolysis have been reported [see WARNINGS AND PRECAUTIONS].

Read the entire FDA prescribing information for Intelence (Entravirine Tablets)

Related Resources for Intelence

Read the Intelence User Reviews »

© Intelence Patient Information is supplied by Cerner Multum, Inc. and Intelence Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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