ACTEMRA (tocilizumab) Injection: Uses, Dosage & Side Effects

ACTEMRA (tocilizumab) is an injectable medication approved for intravenous or subcutaneous use. It is primarily used to treat various inflammatory and autoimmune conditions by targeting and blocking the interleukin-6 (IL-6) receptor, which plays a key role in inflammation.

• Rheumatoid Arthritis (RA): Treatment of adult patients with moderately to severely active RA who have not responded adequately to one or more Disease-Modifying Anti-Rheumatic Drugs (DMARDs).
• Giant Cell Arteritis (GCA): Treatment of adult patients with this inflammatory blood vessel condition.
• Systemic Sclerosis-Associated Interstitial Lung Disease (SSc-ILD): To slow the decline in lung function in adults with this disease.
• Polyarticular Juvenile Idiopathic Arthritis (PJIA): Treatment of active disease in patients aged 2 years and older.
• Systemic Juvenile Idiopathic Arthritis (SJIA): Treatment of active disease in patients aged 2 years and older.
• Cytokine Release Syndrome (CRS): Management of severe or life-threatening CRS induced by CAR T-cell therapy in pediatric and adult patients aged 2 years and older.
• Coronavirus Disease 2019 (COVID-19): Treatment of hospitalized patients aged 2 years and older who require systemic corticosteroids and supplemental oxygen or advanced respiratory support.

tocilizumab

ACTEMRA contains tocilizumab, a monoclonal antibody that blocks the interleukin-6 (IL-6) receptor. IL-6 is a protein involved in immune responses and inflammation. By inhibiting IL-6 signaling, ACTEMRA reduces the inflammatory process that contributes to the symptoms and tissue damage in autoimmune and inflammatory diseases.

General Guidelines

• ACTEMRA is given either by intravenous (IV) infusion or subcutaneous (SC) injection depending on the condition treated.
• Before treatment, patients should have baseline blood tests, including complete blood count and liver function.
• Do not initiate treatment in patients with low neutrophil counts, low platelet counts, or elevated liver enzymes above specified thresholds.

Rheumatoid Arthritis (Adults)

• IV dose: Start at 4 mg/kg every 4 weeks; may increase to 8 mg/kg every 4 weeks based on response. Do not exceed 800 mg per infusion.
• SC dose: Under 100 kg: 162 mg every other week, increase to weekly if needed. 100 kg or more: 162 mg every week.

Giant Cell Arteritis (Adults)

• IV dose: 6 mg/kg every 4 weeks with glucocorticoid taper. Do not exceed 600 mg per infusion.
• SC dose: 162 mg once weekly with glucocorticoid taper; in some cases, every other week dosing is an option.

Systemic Sclerosis-Associated Interstitial Lung Disease (Adults)

• SC dose: 162 mg once weekly.
• IV administration is not approved for this use.

Polyarticular Juvenile Idiopathic Arthritis (Patients ≥2 years)

• IV dose every 4 weeks:
  Less than 30 kg: 10 mg/kg
  30 kg or more: 8 mg/kg
• SC dose:
  Less than 30 kg: 162 mg every 3 weeks
  30 kg or more: 162 mg every 2 weeks

Systemic Juvenile Idiopathic Arthritis (Patients ≥2 years)

• IV dose every 2 weeks:
  Less than 30 kg: 12 mg/kg
  30 kg or more: 8 mg/kg
• SC dose:
  Less than 30 kg: 162 mg every 2 weeks
  30 kg or more: 162 mg weekly

Cytokine Release Syndrome (CRS) (Patients ≥2 years)

• IV infusion:
  Less than 30 kg: 12 mg/kg
  30 kg or more: 8 mg/kg
• May be given alone or with corticosteroids.
• Up to 4 doses may be given with at least 8 hours between doses if symptoms persist.
• SC administration is not approved.

COVID-19 (Patients ≥2 years)

• IV infusion:
  Less than 30 kg: 12 mg/kg
  30 kg or more: 8 mg/kg
• Given as a single 60-minute infusion; a second dose may be given after at least 8 hours if needed.
• SC administration is not approved.

Administration Notes

• IV infusions should be diluted in sodium chloride solution and infused over 60 minutes (no bolus or push).
• SC injections should be administered according to instructions; patients or caregivers may self-inject after proper training.
• Injection sites should be rotated to avoid skin irritation.
• Dose adjustments or interruptions may be needed for elevated liver enzymes, low neutrophils, or low platelets.
• Do not use ACTEMRA with other biologic DMARDs due to infection risks.

Risk of Serious Infections

ACTEMRA increases the risk of serious infections that can lead to hospitalization or death. These include tuberculosis (pulmonary and extrapulmonary), invasive fungal infections (e.g., candidiasis, aspergillosis, pneumocystis), bacterial and viral opportunistic infections.

Patients should be tested for latent tuberculosis before starting ACTEMRA (except COVID-19 patients) and monitored closely during and after treatment. If a serious infection develops, ACTEMRA should be interrupted until the infection is controlled.

Liver Enzyme Elevations

Elevations in liver enzymes (ALT, AST) may occur. Dose modification, interruption, or discontinuation is recommended based on the degree of elevation.

Hematologic Abnormalities

Neutropenia and thrombocytopenia have been reported. Treatment should not start in patients with severe neutropenia or thrombocytopenia, and doses should be adjusted or held if these blood counts fall during treatment.

Other Precautions

• Close monitoring of blood counts and liver function is essential.
• Avoid concomitant use with other biologic DMARDs due to increased infection risks.
• ACTEMRA should not be infused with other drugs in the same IV line due to lack of compatibility studies.

Common Adverse Reactions

• Increased risk of infections (bacterial, viral, fungal)
• Elevated liver enzymes
• Neutropenia (low white blood cell count)
• Thrombocytopenia (low platelet count)
• Injection site reactions with subcutaneous use

Serious Reactions

• Serious infections including tuberculosis and invasive fungal infections
• Severe allergic reactions including anaphylaxis

ACTEMRA has not been studied in combination with other biologic DMARDs such as TNF inhibitors, IL-1 receptor antagonists, anti-CD20 antibodies, or selective co-stimulation modulators. Concurrent use is not recommended due to increased immunosuppression and infection risk.

Store fully diluted ACTEMRA infusion solutions at 2°C to 8°C (36°F to 46°F) protected from light. Stability varies depending on diluent concentration and storage temperature (up to 24 hours refrigerated; shorter times at room temperature).

Unused vial contents should be discarded as the product contains no preservatives.

Subcutaneous injection supplies should be inspected before use and discarded if discolored or containing particulates.