Data from FDA - Curated by EPG Health - Last updated 09 August 2018

Indication(s)

1 INDICATIONS AND USAGE EMTRIVA® is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. Additional important information regarding the use of EMTRIVA for the treatment of HIV-1 Infection: EMTRIVA should not be coadministered with ATRIPLA®, COMPLERA®, DESCOVY®, GENVOYA®, ODEFSEY®, STRIBILD®, TRUVADA®, or lamivudine-containing products [See Warnings and Precautions (5.3)]. In treatment-experienced patients, the use of EMTRIVA should be guided by laboratory testing and treatment history [See Clinical Pharmacology (12.4)]. EMTRIVA, a nucleoside analog HIV-1 reverse transcriptase inhibitor, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. (1)

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Advisory information

contraindications
4 CONTRAINDICATIONS EMTRIVA is contraindicated in patients with previously demonstrated hypersensitivity to any of the components of the products. EMTRIVA is contraindicated in patients with previously demonstrated hypersensitivity to any of the components of the products. (4)
Adverse reactions
6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: Severe Acute Exacerbations of Hepatitis B [See Boxed Warning, Warnings and Precautions (5.1)]. Lactic acidosis/severe hepatomegaly with steatosis [See Warnings and Precautions (5.2)]. Immune Reconstitution Syndrome [See Warnings and Precautions (5.5)]. Most common adverse reactions (incidence ≥10%) are headache, diarrhea, nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough, and rhinitis. Skin hyperpigmentation was very common (≥10%) in pediatric patients. (6) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-800-GILEAD-5 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Adverse Reactions from Clinical Trials Experience Clinical Trials in Adult Subjects More than 2,000 adult subjects with HIV-1 infection have been treated with EMTRIVA alone or in combination with other antiretroviral agents for periods of 10 days to 200 weeks in clinical trials. 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 most common adverse reactions (incidence greater than or equal to 10%, any severity) identified from any of the three large, controlled clinical trials include headache, diarrhea nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough, and rhinitis. Studies 301A and 303 – Treatment Emergent Adverse Reactions: The most common adverse reactions that occurred in subjects receiving EMTRIVA with other antiretroviral agents in clinical trials 301A and 303 were headache, diarrhea, nausea, and rash, which were generally of mild to moderate severity. Approximately 1% of subjects discontinued participation in the clinical trials due to these events. All adverse reactions were reported with similar frequency in EMTRIVA and control treatment groups with the exception of skin discoloration, which was reported with higher frequency in the EMTRIVA-treated group. Skin discoloration, manifested by hyperpigmentation on the palms and/or soles, was generally mild and asymptomatic. The mechanism and clinical significance are unknown. A summary of EMTRIVA treatment-emergent clinical adverse reactions in Studies 301A and 303 is provided in Table 2. Table 2 Selected Treatment-Emergent Adverse Reactions (All Grades, Regardless of Causality) Reported in ≥3% of EMTRIVA-Treated Subjects in Either Study 301A or 303 (0–48 Weeks) 303 301A EMTRIVA + ZDV/d4T + NNRTI/PI (N=294) Lamivudine + ZDV/d4T + NNRTI/PI (N=146) EMTRIVA + didanosine + efavirenz (N=286) Stavudine + didanosine + efavirenz (N=285) Body as a Whole Abdominal pain 8% 11% 14% 17% Asthenia 16% 10% 12% 17% Headache 13% 6% 22% 25% Digestive System Diarrhea 23% 18% 23% 32% Dyspepsia 4% 5% 8% 12% Nausea 18% 12% 13% 23% Vomiting 9% 7% 9% 12% Musculoskeletal Arthralgia 3% 4% 5% 6% Myalgia 4% 4% 6% 3% Nervous System Abnormal dreams 2% <1% 11% 19% Depressive disorders 6% 10% 9% 13% Dizziness 4% 5% 25% 26% Insomnia 7% 3% 16% 21% Neuropathy/peripheral neuritis 4% 3% 4% 13% Paresthesia 5% 7% 6% 12% Respiratory Increased cough 14% 11% 14% 8% Rhinitis 18% 12% 12% 10% Skin Rash eventRash event includes rash, pruritus, maculopapular rash, urticaria, vesiculobullous rash, pustular rash, and allergic reaction. 17% 14% 30% 33% Studies 301A and 303 – Laboratory Abnormalities: Laboratory abnormalities in these trials occurred with similar frequency in the EMTRIVA and comparator groups. A summary of Grades 3–4 laboratory abnormalities is provided in Table 3. Table 3 Treatment-Emergent Grades 3–4 Laboratory Abnormalities Reported in ≥1% of EMTRIVA-Treated Subjects in Either Study 301A or 303 303 301A EMTRIVA + ZDV/d4T + NNRTI/PI (N=294) Lamivudine + ZDV/d4T + NNRTI/PI (N=146) EMTRIVA + Didanosine + Efavirenz (N=286) Stavudine + Didanosine + Efavirenz (N=285) Percentage with grade 3 or grade 4 laboratory abnormality 31% 28% 34% 38% ALT (>5.0 × ULNULN = Upper limit of normal) 2% 1% 5% 6% AST (>5.0 × ULN) 3% <1% 6% 9% Bilirubin (>2.5 × ULN) 1% 2% <1% <1% Creatine kinase (>4.0 × ULN) 11% 14% 12% 11% Neutrophils (<750 mm3) 5% 3% 5% 7% Pancreatic amylase (>2.0 × ULN) 2% 2% <1% 1% Serum amylase (>2.0 × ULN) 2% 2% 5% 10% Serum glucose <40 or >250 mg/dL) 3% 3% 2% 3% Serum lipase (>2.0 × ULN) <1% <1% 1% 2% Triglycerides (>750 mg/dL) 10% 8% 9% 6% Study 934 – Treatment Emergent Adverse Reactions: In Study 934, 511 antiretroviral-naïve subjects received either VIREAD® + EMTRIVA administered in combination with efavirenz (N=257) or zidovudine/lamivudine administered in combination with efavirenz (N=254). Adverse reactions observed in this trial were generally consistent with those seen in previous trials in treatment-experienced or treatment-naïve subjects (Table 4). Table 4 Selected Treatment-Emergent Adverse ReactionsFrequencies of adverse reactions are based on all treatment-emergent adverse events, regardless of relationship to study drug. (Grades 2–4) Reported in ≥5% in Any Treatment Group in Study 934 (0–144 Weeks) TDFFrom Weeks 96 to 144 of the trial, subjects received TRUVADA with efavirenz in place of VIREAD + EMTRIVA with efavirenz. + EMTRIVA + EFV AZT/3TC + EFV N=257 N=254 Gastrointestinal Disorder Diarrhea 9% 5% Nausea 9% 7% Vomiting 2% 5% General Disorders and Administration Site Condition Fatigue 9% 8% Infections and Infestations Sinusitis 8% 4% Upper respiratory tract infections 8% 5% Nasopharyngitis 5% 3% Nervous System Disorders Headache 6% 5% Dizziness 8% 7% Psychiatric Disorders Depression 9% 7% Insomnia 5% 7% Skin and Subcutaneous Tissue Disorders Rash eventRash event includes rash, exfoliative rash, rash generalized, rash macular, rash maculo-papular, rash pruritic, and rash vesicular. 7% 9% Study 934 – Laboratory Abnormalities: Significant laboratory abnormalities observed in this trial are shown in Table 5. Table 5 Significant Laboratory Abnormalities Reported in ≥1% of Subjects in Any Treatment Group in Study 934 (0–144 Weeks) TDFFrom Weeks 96 to 144 of the trial, subjects received TRUVADA with efavirenz in place of VIREAD + EMTRIVA with efavirenz. + EMTRIVA + EFV AZT/3TC + EFV N=257 N=254 Any ≥ Grade 3 Laboratory Abnormality 30% 26% Fasting Cholesterol (>240 mg/dL) 22% 24% Creatine Kinase (M: >990 U/L) 9% 7% (F: >845 U/L) Serum Amylase (>175 U/L) 8% 4% Alkaline Phosphatase (>550 U/L) 1% 0% AST (M: >180 U/L) 3% 3% (F: >170 U/L) ALT (M: >215 U/L) 2% 3% (F: >170 U/L) Hemoglobin (<8.0 mg/dL) 0% 4% Hyperglycemia (>250 mg/dL) 2% 1% Hematuria (>75 RBC/HPF) 3% 2% Glycosuria (3+) <1% 1% Neutrophils (<750/mm3) 3% 5% Fasting Triglycerides (>750 mg/dL) 4% 2% Clinical Trials in Pediatric Subjects Assessment of adverse reactions is based on data from Study 203, an open label, uncontrolled trial of 116 HIV-1 infected pediatric subjects who received emtricitabine through 48 weeks. The adverse reaction profile in pediatric subjects was generally comparable to that observed in clinical trials of EMTRIVA in adult subjects [See Adverse Reactions (6.1)]. Hyperpigmentation was more frequent in children. Additional adverse reactions identified from this trial include anemia. Selected treatment-emergent adverse events, regardless of causality, reported in subjects during 48 weeks of treatment were the following: infection (44%), hyperpigmentation (32%), increased cough (28%), vomiting (23%), otitis media (23%), rash (21%), rhinitis (20%), diarrhea (20%), fever (18%), pneumonia (15%), gastroenteritis (11%), abdominal pain (10%), and anemia (7%). Treatment-emergent grades 3–4 laboratory abnormalities were experienced by 9% of pediatric subjects, including elevated amylase (>2.0 × ULN) (n=4), decreased neutrophils (<750/mm3) (n=3), elevated ALT (>5 × ULN) (n=2), elevated CPK (>4 × ULN) (n=2) and one subject each with elevated bilirubin (>3.0 × ULN), elevated GGT (>10 × ULN), elevated lipase (>2.5 × ULN), decreased hemoglobin (<7 g/dL), and decreased glucose (<40 mg/dL).

Usage information

Dosing and administration
2 DOSAGE AND ADMINISTRATION EMTRIVA may be taken without regard to food. (2.1) Adult Patients (18 years of age and older) (2.2): EMTRIVA capsules: One 200 mg capsule administered once daily orally. EMTRIVA oral solution: 240 mg (24 mL) administered once daily orally. Pediatric Patients (0–3 months of age) (2.3): EMTRIVA oral solution: 3 mg/kg administered once daily orally. Pediatric Patients (3 months through 17 years) (2.4): EMTRIVA oral solution: 6 mg/kg up to a maximum of 240 mg (24 mL) administered once daily orally. EMTRIVA capsules: For children weighing more than 33 kg who can swallow an intact capsule, one 200 mg capsule administered once daily orally. Dose interval adjustment in adult patients with renal impairment (2.5): Creatinine Clearance (mL/min) Formulation ≥50 mL/min 30–49 mL/min 15–29 mL/min <15 mL/min or on hemodialysisHemodialysis Patients: If dosing on day of dialysis, give dose after dialysis. Capsule (200 mg) 200 mg every 24 hours 200 mg every 48 hours 200 mg every 72 hours 200 mg every 96 hours Oral Solution (10 mg/mL) 240 mg every 24 hours (24 mL) 120 mg every 24 hours (12 mL) 80 mg every 24 hours (8 mL) 60 mg every 24 hours (6 mL) 2.1 Recommended Dose EMTRIVA may be taken without regard to food. 2.2 Adult Patients (18 years of age and older) EMTRIVA capsules: One 200 mg capsule administered once daily orally. EMTRIVA oral solution: 240 mg (24 mL) administered once daily orally. 2.3 Pediatric Patients (0–3 months of age) EMTRIVA oral solution: 3 mg per kg administered once daily orally. 2.4 Pediatric Patients (3 months through 17 years) EMTRIVA oral solution: 6 mg per kg up to a maximum of 240 mg (24 mL) administered once daily orally. EMTRIVA capsules: For children weighing more than 33 kg who can swallow an intact capsule, one 200 mg capsule administered once daily orally. 2.5 Dose Adjustment in Adult Patients with Renal Impairment Significantly increased drug exposures were seen when EMTRIVA was administered to subjects with renal impairment [See Clinical Pharmacology (12.3)]. Therefore, the dosing interval or dose of EMTRIVA should be adjusted in patients with baseline creatinine clearance less than 50 mL/min using the following guidelines (Table 1). The safety and effectiveness of these dose adjustment guidelines have not been clinically evaluated. Therefore, clinical response to treatment and renal function should be closely monitored in these patients. Table 1 Dose Adjustment in Adult Patients with Renal Impairment Creatinine Clearance (mL/min) Formulation ≥50 mL/min 30–49 mL/min 15–29 mL/min <15 mL/min or on hemodialysisHemodialysis Patients: If dosing on day of dialysis, give dose after dialysis. Capsule (200 mg) 200 mg every 24 hours 200 mg every 48 hours 200 mg every 72 hours 200 mg every 96 hours Oral Solution (10 mg/mL) 240 mg every 24 hours (24 mL) 120 mg every 24 hours (12 mL) 80 mg every 24 hours (8 mL) 60 mg every 24 hours (6 mL) Although there are insufficient data to recommend a specific dose adjustment of EMTRIVA in pediatric patients with renal impairment, a reduction in the dose and/or an increase in the dosing interval similar to adjustments for adults should be considered.
Use in special populations
8 USE IN SPECIFIC POPULATIONS Nursing mothers: Women infected with HIV should be instructed not to breastfeed. (8.3) Pediatrics: Dose adjustment based on age and weight. (2.3, 2.4, 12.3) 8.1 Pregnancy Pregnancy Category B The incidence of fetal variations and malformations was not increased in embryofetal toxicity studies performed with emtricitabine in mice at exposures (AUC) approximately 60-fold higher and in rabbits at approximately 120-fold higher than human exposures at the recommended daily dose. There are, however, no adequate and well-controlled trials in pregnant women. Because animal reproduction studies are not always predictive of human response, EMTRIVA should be used during pregnancy only if clearly needed. Antiretroviral Pregnancy Registry: To monitor fetal outcomes of pregnant women exposed to EMTRIVA, an Antiretroviral Pregnancy Registry has been established. Healthcare providers are encouraged to register patients by calling 1–800–258–4263. 8.3 Nursing Mothers Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1. Samples of breast milk obtained from five HIV-1 infected mothers show that emtricitabine is secreted in human milk. Breastfeeding infants whose mothers are being treated with emtricitabine may be at risk for developing viral resistance to emtricitabine. Other emtricitabine-associated risks in infants breastfed by mothers being treated with emtricitabine are unknown. Because of both the potential for HIV-1 transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving EMTRIVA. 8.4 Pediatric Use The safety and efficacy of emtricitabine in patients between 3 months and 21 years of age is supported by data from three open-label, nonrandomized clinical trials in which emtricitabine was administered to 169 HIV-1 infected treatment-naïve and experienced (defined as virologically suppressed on a lamivudine containing regimen for which emtricitabine was substituted for lamivudine) subjects [See Clinical Studies(14.3)]. The pharmacokinetics of emtricitabine were studied in 20 neonates born to HIV-1 positive mothers [See Clinical Studies (14.3)]. All neonates were HIV-1 negative at the end of the trial; the efficacy of emtricitabine in preventing or treating HIV-1 could not be determined. 8.5 Geriatric Use Clinical trials of EMTRIVA did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. In general, dose selection for the elderly patient should be cautious, keeping in mind the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. 8.6 Patients with Impaired Renal Function It is recommended that the dose or dosing interval for EMTRIVA be modified in patients with creatinine clearance less than 50 mL/min or in patients who require dialysis [See Dosage and Administration (2.5)].
Pregnancy and lactation
8.3 Nursing Mothers Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1. Samples of breast milk obtained from five HIV-1 infected mothers show that emtricitabine is secreted in human milk. Breastfeeding infants whose mothers are being treated with emtricitabine may be at risk for developing viral resistance to emtricitabine. Other emtricitabine-associated risks in infants breastfed by mothers being treated with emtricitabine are unknown. Because of both the potential for HIV-1 transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving EMTRIVA.

Interactions

7 DRUG INTERACTIONS The potential for drug interactions with EMTRIVA has been studied in combination with zidovudine, indinavir, stavudine, famciclovir, and tenofovir DF. There were no clinically significant drug interactions for any of these drugs. Drug interactions trials are described elsewhere in the labeling [See Clinical Pharmacology (12.3)].

More information

Category Value
Authorisation number NDA021500
Agency product number G70B4ETF4S
Orphan designation No
Product NDC 61958-0601,61958-0602
Date Last Revised 13-04-2017
Type HUMAN PRESCRIPTION DRUG
RXCUI 403875
Storage and handling Store at 25 °C (77 °F); excursions permitted to 15 °C–30 °C (59 °F–86 °F).
Marketing authorisation holder Gilead Sciences, Inc.
Warnings WARNING: POSTTREATMENT EXACERBATION OF HEPATITIS B EMTRIVA is not approved for the treatment of chronic hepatitis B virus (HBV) infection, and the safety and efficacy of EMTRIVA have not been established in patients coinfected with HBV and HIV-1. Severe acute exacerbations of hepatitis B have been reported in patients who have discontinued EMTRIVA. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue EMTRIVA. If appropriate, initiation of anti-hepatitis B therapy may be warranted [See Warnings and Precautions (5.1)]. WARNING: POSTTREATMENT EXACERBATION OF HEPATITIS B See full prescribing information for complete boxed warning. EMTRIVA is not approved for the treatment of chronic Hepatitis B virus (HBV) infection. Severe acute exacerbations of Hepatitis B have been reported in patients who have discontinued EMTRIVA. Hepatic function should be monitored closely in patients coinfected with HIV-1 and HBV. If appropriate, initiation of anti-Hepatitis B therapy may be warranted. (5.1)