(en FYOO vir tide)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution Reconstituted, Subcutaneous:
Fuzeon: 90 mg (1 ea)
Brand Names: U.S.
- Antiretroviral, Fusion Protein Inhibitor (Anti-HIV)
Binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein. Inhibits the fusion of HIV-1 virus with CD4 cells by blocking the conformational change in gp41 required for membrane fusion and entry into CD4 cells
SubQ: Absorption is comparable when injected into abdomen, arm, or thigh
Vd: 5.5 ± 1.1 L; CSF concentrations (2-18 hours after administration; n=4): nondetectable (<0.025 mcg/mL)
Expected to undergo catabolism via peptidases and proteinases in the liver and kidneys to amino acids; amino acids would then be recycled in the body pool. A deaminated metabolite (with 20% activity compared to parent drug) was formed via hydrolysis during in vitro human microsomal and hepatocyte studies.
Plasma clearance is decreased in adults with lower body weight and in females after adjusting for body weight (clearance in adults females is 20% lower compared to adults males). However, no adjustment in dose is recommended for gender or weight.
Compared to patients with normal renal function, enfuvirtide clearance is decreased by 38% in patients with severe renal impairment (CrCl 11 to 35 mL/minute) and by 14% to 28% in patients with end-stage renal disease who are maintained on dialysis. However, no adjustment in dose is recommended for patients with renal impairment.
Apparent clearance: Multiple dosing: Children: 40 ± 17 mL/hour/kg; Adults: 30.6 ± 10.6 mL/hour/kg
Time to Peak
SubQ: Single dose: Median: 8 hours (range: 3 to 12 hours); Multiple dosing: Median: 4 hours (range: 4 to 8 hours)
3.8 ± 0.6 hours
92%; primarily to albumin, but also to alpha-1 acid glycoprotein (to a lesser extent)
Use: Labeled Indications
HIV-1 infection: Treatment of HIV-1 infection in combination with other antiretroviral agents in treatment-experienced patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy
Hypersensitivity to enfuvirtide or any component of the formulation
HIV-1 infection, treatment: SubQ: 90 mg twice daily
Refer to adult dosing.
HIV-1 infection, treatment:
Children and Adolescents 6 to 16 years: SubQ: 2 mg/kg twice daily (maximum dose: 90 mg/dose)
Adolescents >16 years: SubQ: Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment necessary.
Dosing: Hepatic Impairment
No dosage adjustment necessary (has not been studied).
Reconstitute with 1 mL SWFI; tap vial for 10 seconds and roll gently between the hands to avoid foaming and to ensure contact with diluent; then allow vial to stand until complete dissolution. May require up to 45 minutes to form solution; allow more time if solution is foamy or jelled. Use immediately or refrigerate reconstituted solution and use within 24 hours; bring refrigerated solution to room temperature before administration.
SubQ: Inject subcutaneously into upper arm, abdomen, or anterior thigh. Do not inject into moles, the navel, over a blood vessel or skin abnormalities such as scar tissue, surgical scars, bruises, tattoos, or burn sites. In addition, do not inject in or near sites where large nerves are close to the skin including the elbow, knee, groin, or buttocks. Rotate injection site, give injections at a site different from the preceding injection site; do not inject into any site where an injection site reaction is evident. Bioequivalence was found to be similar in a study comparing standard administration using a needle versus a needle-free device (True 2006).
Store intact vials at 25°C (77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Store reconstituted solution in the original vial at 2°C to 8°C (36°F to 46°F); use within 24 hours. Vials are for single use only; discard unused portion.
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Monitor therapy
Protease Inhibitors: May increase the serum concentration of Enfuvirtide. Enfuvirtide may increase the serum concentration of Protease Inhibitors. Monitor therapy
Central nervous system: Fatigue (20%), insomnia (11%)
Gastrointestinal: Diarrhea (32%), nausea (23%)
Local: Injection site reaction (98%; may include cyst at injection site, erythema at injection site, induration at injection site, injection site ecchymosis, injection site nodule, injection site pruritus, pain at injection site), injection site infection (children: 11%, adults: 2%)
1% to 10%:
Dermatologic: Folliculitis (2%)
Endocrine & metabolic: Weight loss (7%)
Gastrointestinal: Abdominal pain (4%), decreased appetite (3%), pancreatitis (3%), anorexia (2%), xerostomia (2%)
Hematologic & oncologic: Eosinophilia (2% to 9%)
Hepatic: Increased serum transaminases (4%, grade 4: 1%)
Infection: Infection (4% to 6%), herpes simplex infection (4%)
Neuromuscular & skeletal: Increased creatine phosphokinase (3% to 7%), limb pain (3%), myalgia (3%)
Ophthalmic: Conjunctivitis (2%)
Respiratory: Sinusitis (6%), cough (4%), bacterial pneumonia (3%), flu-like symptoms (2%)
<1%, postmarketing, and/or case reports: Amyloidosis (cutaneous; at the injection site), angina pectoris, anxiety, constipation, depression, dysgeusia, glomerulonephritis, Guillain-Barré syndrome, hyperglycemia; hypersensitivity exacerbation (to abacavir), hypersensitivity reaction (symptoms may include fever, hypotension, increased serum transaminases, nausea, skin rash, vomiting); increased amylase, increased gamma-glutamyl transferase, insomnia, increased serum lipase, increased serum triglycerides, liver steatosis, lymphadenopathy, neutropenia, peripheral neuropathy, pulmonary disease, renal failure, renal insufficiency, renal tubular necrosis, respiratory distress, sepsis, sixth nerve palsy, suicidal tendencies, thrombocytopenia, toxic hepatitis, weakness
Concerns related to adverse effects:
• Hypersensitivity reactions: May cause hypersensitivity reactions (symptoms may include rash, fever, nausea, vomiting, chills, rigors, hypotension, and/or elevated liver transaminases). Discontinue therapy immediately if systemic reactions occur; do not rechallenge patient.
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Injection site reactions: Local injection site reactions are common. Administration using a needle-free device has been associated with nerve pain (including neuralgia and/or paresthesia lasting up to 6 months), bruising, and hematomas when administered at sites where large nerves are close to the skin; only administer medication in recommended sites.
• Pneumonia: Monitor closely for signs/symptoms of pneumonia; associated with an increased incidence during clinical trials, particularly in patients with a low CD4 cell count, high initial viral load, IV drug use, smoking, or a history of lung disease.
• Bleeding disorders: Use with caution in patients with coagulation disorders (eg, hemophilia) or receiving anticoagulants; increased risk of bleeding at injection site.
• Appropriate use: Use is not recommended in antiretroviral therapy-naive patients.
Viral load; CD4 count; hypersensitivity and injection site reactions; pediatric weight (periodically; adjust dose accordingly); signs and symptoms of pneumonia
Pregnancy Risk Factor
Enfuvirtide has minimal to low transfer across the human placenta. Data collected by the antiretroviral pregnancy registry is insufficient to evaluate human teratogenic risk. Maternal antiretroviral therapy (ART) may increase the risk of preterm delivery, although available information is conflicting possibly due to variability of maternal factors (disease severity; gestational age at initiation of therapy); however, maternal antiretroviral medication should not be withheld due to concerns of preterm birth. Information related to stillbirth, low birth weight, and small for gestational age infants is limited. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children who develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential mitochondrial dysfunction.
The Health and Human Services (HHS) Perinatal HIV Guidelines note that there are insufficient data to recommend use of enfuvirtide as initial therapy in antiretroviral-naive pregnant females. Pharmacokinetic data are insufficient to make dosing recommendations during pregnancy.
In general, ART is recommended for all pregnant females with HIV to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. When HIV is diagnosed during pregnancy in a female who has never received antiretroviral therapy, ART should begin as soon as possible after diagnosis. Females who become pregnant on a stable ART regimen may continue that regimen if viral suppression is effective, appropriate drug exposure can be achieved, contraindications for use in pregnancy are not present, and the regimen is well tolerated. Monitoring during pregnancy is more frequent than in nonpregnant adults; ART should be continued postpartum for all females living with HIV.
Health care providers are encouraged to enroll pregnant females exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com). Health care providers caring for HIV-infected females and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal] 2017).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience insomnia, diarrhea, loss of strength and energy, lack of appetite, constipation, rhinitis, weight loss, or muscle pain. Have patient report immediately to prescriber signs of infection, signs of kidney problems (urinary retention, hematuria, change in amount of urine passed, or weight gain), signs of skin infection, signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), severe injection site irritation, chills, severe nausea, vomiting, burning or numbness feeling, severe dizziness, passing out, cough, difficulty breathing, shortness of breath, swelling of arms or legs, swollen glands, or depression (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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- Drug class: miscellaneous antivirals
Other brands: Fuzeon