Etacept SC Injection

Etanercept is a tumor necrosis factor (TNF) blocker. This is a dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids and has an apparent molecular weight of approximately 150 kilodaltons. Etanercept is a TNF alpha inhibitor that binds specifically to tumor necrosis factor (TNF) and blocks its interaction with cell surface TNF receptors. TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Elevated levels of TNF are found in the synovial fluid of RA patients. It plays an important role in the inflammatory processes of rheumatoid arthritis (RA), polyarticular-course juvenile rheumatoid arthritis (JRA) and the resulting joint pathology.

Rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis: Patients aged 18 years or older- 50 mg Etanercept per week administered either once weekly (as one subcutaneous injection using a 50 mg syringe or as two 25 mg injections given at the same time) or 25 mg Etanercept twice weekly (72 to 96 hours apart) as a subcutaneous injection. Methotrexate, glucocorticoids, salicylates, nonsteroidal anti- inflammatory drugs (NSAIDs), or analgesics may be continued during treatment with Etanercept in adults. 25 mg once weekly gives a slower response and may be less effective.

Plaque psoriasis: The dose of etanercept is 50 mg syringe once weekly (as one subcutaneous injection using a 50 mg syringe or as two 25 mg injections given at approximately the same time) or 25 mg twice weekly (72 to 96 hours apart) as a subcutaneous injection. Higher responses may be achieved from initial treatment with a dose of 50 mg twice weekly for up to 12 weeks, followed, if necessary, by a dose of 50 mg once weekly or 25 mg twice weekly.

Adult patients may be treated intermittent or continuously based on physician judgment and individual patient needs. Treatment should be discontinued in patients who show no response after 12 weeks. With intermittent use, treatment cycles subsequent to the initial cycle should use a dose of 50 mg once weekly. No dose adjustment is required for elderly and or patient with renal and hepatic impairment. Patient weighs less than 62.5kg should be accurately dosed on an mg/kg basis. Patients weighing 62.5 kg or more may be fixed-dose prefilled syringe.

Juvenile idiopathic arthritis: Children (⩾2 to <18 years): 0.4mg/kg (up to maximum of 25 mg per dose) twice weekly (72 to 96 hours apart). Glucocoticoids, nonsteroidal anti-inflammatory drugs (NSAIDs), or analgesics may be continued during treatment with etanercept in children. Etanercept has not been studied in children <2 years of age.

Pediatric plaque psoriasis: Children (⩾6 to <18 years): 0.8mg/kg (up to a maximum of 50 mg per dose) once weekly for up to 24 weeks. Treatment should be discontinued in patients who show no response after 12 weeks. If retreatment of etanercept is indicated, the above guidance on treatment duration should be followed. The dose should be 0.8 mg/kg (up to maximum of 50 mg per dose) once weekly.

Administer etanercept as subcutaneous injections in the thigh, abdomen or upper arm. Given each new injection at least 3 cm from a previous site. Do not use in the area where the skin is tender, bruised, red or hard. The injection should be performed under supervision of qualified healthcare professional. Before injection, single-use prefilled syringe should be allowed to reach room temperature (approximately 15-30 minutes). The needle cover should not be removed while allowing the pre-filled syringe to reach at room temperature. Before disposal of blank PFS, please activate the needle guard to avoid any chance of needle-stick injury.

If any hypersensitivity to etanercept or to any component of the formulation. Incase of sepsis or risk of sepsis. Treatment with etanercept should not be initiated in patients with serious active infections, including chronic or localized infection.

Very common: Infections (including colds, sinusitis, bronchitis, urinary tract infections and skin infections); injection site reactions (including bleeding, bruising, redness, itching, pain, and swelling). Reactions at the injection site (these do not occur as often after the first month of treatment. Some patients have developed a reaction at an injection site that was used before.

Common: Allergic reactions; fever; itching; antibodies directed against normal tissue (autoantibody formation).

Uncommon: Serious infections (including pneumonia, deep skin infections, joint infections, blood infection, and infections at various sites); low blood platelet count; skin cancer (excluding melanoma); localized swelling of the skin (angio edema); hives (elevated patches of red or pale skin that often itch); eye inflammation; psoriasis (new or worsening); rash; inflammation or scarring of the lungs; inflammation of the blood vessels affecting multiple organs.

The safe use of etanercept during pregnancy has not been established. Use etanercept during pregnancy only if clearly needed. The safe use of etanercept during lactation has not been established. It is not known whether etanercept is excreted in human milk. Following subcutaneous administration to lactating rats, etanercept was excreted in the milk and detected in the serum of the pups. Because immunoglobulins and many medicinal products can be excreted in human milk, a decision should be made whether to discontinue nursing or to discontinue etanercept while nursing.

Special warning and special precautions for use-

• Allergic reactions
• Infections/surgery
• Infections/diabetes
• Infections/monitoring
• Tuberculosis
• Hepatitis-B
• Hepatitis-C
• Blood disorders
• Nervous system and eye disorders
• Congestive heart failure
• Cancer
• Chickenpox
• Latex
• Alcohol abuse
• Wegener's granulomatosis
• Anti-diabetic medicine

The maximum tolerated dose of Etacept has not been established in humans. Single intravenous doses up to 60 mg/m² have been administered to healthy volunteers in an endotoxemia study without evidence of dose-limiting toxicities. The highest dose level evaluated in rheumatoid arthritis patients has been an intravenous loading dose of 32 mg/m² followed by subcutaneous doses of 16 mg/m² (25 mg) administered twice weekly. No dose-limiting toxicities were observed during clinical trials of rheumatoid arthritis patients. There is no known antidote to Etacept.

Immunosuppressant

Etacept should be stored in refrigerator at 2-8°C. Do not freeze. Do not shake. Keep away from light. Keep out of reach of children.