Trade Names:Enbrel- Injection, solution 25 mg per 0.5 mL- Injection, solution 50 mg per mL- Injection, lyophilized powder for solution 25 mg
Binds specifically to tumor necrosis factor (TNF), blocking its interaction with cell surface TNF receptors, and modulating biological responses induced or regulated by TNF.
C max is approximately 1.1 mcg/mL. T max is approximately 69 h (single dose). C max increases 2- to 7-fold, while AUC increases approximately 4-fold with repeated dosing.
The half-life is approximately 102 h. Cl is approximately 160 mL/h.
No studies conducted.Hepatic Function Impairment
No studies conducted.Children
Cl is slightly reduced in patients 4 to 8 yr of age.Age/Gender
Pharmacokinetic parameters are not different.
Reducing signs and symptoms and inhibiting the progression of structural damage in moderately to severely active rheumatoid arthritis (RA); reducing signs and symptoms of moderately to severely active polyarticular-course juvenile idiopathic arthritis in children 2 years of age and older; reducing signs and symptoms in patients with active ankylosing spondylitis; treatment of adult patients with chronic, moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy; reducing signs and symptoms, inhibiting the progression of structural damage of active arthritis, and improving physical function in patients with psoriatic arthritis.
Crohn disease; CHF; pyoderma gangrenosum.
Sepsis; hypersensitivity to etanercept or to any of its components.
Subcutaneous 50 mg/wk, given as 1 injection.
For RA, dosages higher than 50 mg/wk are not recommended.Juvenile Idiopathic ArthritisChildren 2 to 17 yr of age
Subcutaneous 0.8 mg/kg/wk (max, 50 mg/wk).Plaque PsoriasisAdults
Subcutaneous 50 mg 2 times/wk (administered 3 or 4 days apart) for 3 mo followed by reduction to a maintenance dosage of 50 mg/wk.
Starting dosages of 25 or 50 mg/wk were also shown to be efficacious.
Refrigerate single-use prefilled syringe at 36° to 46°F. Do not freeze. Keep prefilled syringes in the original carton to protect from light until time of use. Do not use multiple-use vial or prefilled syringe beyond expiration date.Multiple-use vial
Refrigerate multiple-use vial dose tray at 36° to 46°F. Do not freeze. Use reconstituted solution immediately or refrigerate at 36° to 46°F for up to 14 days. Discard solution if not used within 14 days.
A 7% rate of serious infections was observed in a 24-wk study with patients receiving etanercept and anakinra therapy. Concurrent therapy is not recommended.Cyclophosphamide
Risk of noncutaneous solid malignancies may be increased. Concurrent use is not recommended.Immunosuppressive agents
Use of etanercept in patients with Wegener granulomatosis receiving immunosuppressive agents is not recommended.Sulfasalazine
The incidence of decreased neutrophil counts may be greater than with either drug alone.
None well documented.
Deep vein thrombosis, heart failure, hypertension, hypotension, MI, myocardial ischemia, stroke, thrombophlebitis (5%); chest pain, new-onset CHF, vasodilation (postmarketing).
Headache (24%); asthenia (11%); dizziness (8%); cerebral ischemia, depression, hydrocephalus, multiple sclerosis, seizure (5%); aseptic meningitis, fatigue, isolated demyelinating conditions (eg, transverse myelitis), paresthesias, personality disorder (postmarketing).
Rash (14%); alopecia (6%); worsening psoriasis (5%); cutaneous ulcer, cutaneous vasculitis, erythema multiforme, nonmelanoma skin cancer, pruritus, Stevens-Johnson syndrome, subcutaneous nodules, TEN, urticaria (postmarketing).
Rhinitis (16%); pharyngitis (7%); sinusitis (5%); dry eyes, ocular inflammation, optic neuritis (postmarketing).
Abdominal pain (19%); nausea (15%); vomiting (13%); dyspepsia (11%); mouth ulcer (6%); appendicitis, cholecystitis, GI bleeding, GI hemorrhage, pancreatitis (5%); esophagitis/gastritis; gastroenteritis; altered sense of taste, anorexia, diarrhea, dry mouth, intestinal perforation (postmarketing).
Kidney calculus, membranous glomerulonephropathy (5%); UTI (postmarketing).
Lymphadenopathy (5%); lymphoma; adenopathy, anemia, aplastic anemia, coagulopathy, leukopenia, neutropenia, pancytopenia, thrombocytopenia (postmarketing).
Autoimmune hepatitis (postmarketing).
Transaminase elevations (postmarketing).
Injection-site reactions (37%).
Type 1 diabetes mellitus, weight gain (postmarketing).
Bursitis, polymyositis (5%); joint pain, lupus-like syndrome (postmarketing).
Upper respiratory tract infections (31%); cough (6%); dyspnea, pulmonary embolism, respiratory disorder, sarcoidosis (5%); interstitial lung disease, pulmonary disease, worsening of prior lung disorder (postmarketing).
Non-upper respiratory tract infections (51%); positive anti–double-stranded DNA antibodies (15%); antinuclear antibodies (11%); peripheral edema (8%); nonneutralizing antibodies (6%); group A streptococcal septic shock; malignancy; noncutaneous solid tumors; non-Hodgkin lymphoma; soft tissue and postoperative wound infection; varicella infection; abscess with bacteremia, angioedema, death, fever, flu-like symptoms, generalized pain, infections (including bacteria, fungal, protozoal and viral), sepsis, tuberculous arthritis (postmarketing).
Infections, including serious infections leading to hospitalization or death, have occurred. Infections have included active tuberculosis (TB), including reactivation of latent TB and bacterial sepsis. Patients should be evaluated for TB risk factors and should be tested for latent TB infection prior to starting and during treatment. Start treatment of latent TB prior to etanercept therapy. Monitor patients for signs and symptoms of infection, including patients who tested negative for latent TB infection.
Document baseline disease-state activity. Reassess periodically to document response to therapy. Monitor patient for signs and symptoms of blood dyscrasias. Monitor patient for signs and symptoms of infection while on or after treatment with etanercept. Closely monitor new infections and be prepared to discontinue etanercept if patient develops a serious infection during therapy. Closely monitor patients who are carriers of hepatitis B virus (HBV) throughout therapy and for several months following termination of therapy. Monitor heart failure patients carefully.
Category B .
Safety and efficacy not established in children younger than 2 yr of age with juvenile idiopathic arthritis. Safety and efficacy in children with plaque psoriasis have not been established.
Because there is a higher incidence of infection in elderly patients, use with caution.
Exercise caution when considering the use of etanercept in patients with a history of recurring infections or with underlying conditions that may predispose them to infections such as advanced or poorly controlled diabetes.
Allergic reactions, including anaphylaxis, may occur.
Formation of autoantibodies and, rarely, development of lupus-like syndrome may occur.
The diluent preservative contains benzyl alcohol, which has been associated with fatal gasping syndrome in premature infants.
Worsening of CHF, with and without identifiable precipitating factors, has been reported.
Rare and sometimes fatal cases of pancytopenia, including aplastic anemia, have been reported.
Etanercept has been associated with reactivation of HBV in chronic carriers of the virus.
Do not coadminister with live virus vaccines. If possible, bring juvenile idiopathic arthritis patients up to date with all immunizations in agreement with current guidelines prior to initiating therapy. Temporarily discontinue therapy in patients with significant exposure to varicella virus and consider prophylactic treatment with varicella zoster immune globulin.
Anti-TNF therapy affects host defenses against infections and malignancies. Safety and efficacy in patients with immunosuppression or chronic infections have not been evaluated.
Mild to moderate injection-site reactions (eg, erythema, itching, swelling) may occur.
Needle cover of the prefilled syringe contains natural rubber (latex).
Lymphoma has been reported in patients receiving TNF-blocking agents.
Agents that inhibit TNF have been associated with rare cases of new-onset or exacerbation of CNS demyelinating disorders, some presenting with mental status changes and some associated with permanent disability. Transverse myelitis, optic neuritis, multiple sclerosis, and new onset or exacerbation of seizure disorders have been observed.
Maximum tolerated dosage has not been established.
Copyright © 2009 Wolters Kluwer Health.