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Tocilizumab

    Brands

    DEA Class; Rx

    Common Brand Names; Actemra

    • DMARDs, Immunomodulators; 
    • Monoclonal Antibodies

    Humanized IL-6 receptor-inhibiting monoclonal antibody
    Used in adults for moderate to severe rheumatoid arthritis (RA), giant cell arteritis (temporal arteritis), systemic sclerosis-associated interstitial lung disease, cytokine release syndrome, and COVID-19; used in pediatric patients 2 years and older with active juvenile idiopathic arthritis (JIA) or cytokine release syndrome; EUA for COVID-19 in pediatric patients 2 years and older
    Boxed warning in label regarding risk for serious infections

    Indicated for adults with moderate-to-severe active rheumatoid arthritis with inadequate response to 1 or more disease modifying antirheumatic drugs (DMARDs)

    Indicated for treatment of giant cell arteritis (GCA)

    Indicated for slowing the rate of decline in pulmonary function in adults with systemic sclerosis-associated interstitial lung disease (SSc-ILD)

    Indicated for the treatment of chimeric antigen receptor (CAR) T cell-induced severe or life-threatening cytokine release syndrome (CRS)

    Indicated for treatment of coronavirus disease 2019 (COVID-19) in hospitalized adults who are receiving systemic corticosteroids and require supplemental oxygen, noninvasive or invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO)

    Hypersensitivity

    SC injection site reactions (7.1-10.1%)

    COVID-19 EUA

    • Constipation (13%)

    Upper respiratory tract infection (6-8%)

    Nasopharyngitis (4-7%)

    Headache (3-7%)

    Hypertension (3-6%)

    ALT increased (1-6%)

    Bronchitis (2-4%)

    Rash (1-4%)

    Dizziness (1-3%)

    Mouth ulceration (1-2%)

    Upper abdominal pain (2-3%)

    Gastritis (1-2%)

    Oral herpes simplex (<2%)

    Stomatitis (<2%)

    Gastric ulcer (<2%)

    Increased weight (<2%)

    Total bilirubin increased (<2%)

    Leukopenia (<2%)

    Peripheral edema (<2%)

    Dyspnea (<2%)

    Cough (<2%)

    Conjunctivitis (<2%)

    COVID-19

    • Increased AST/ALT (10%)
    • Constipation (9%)
    • Urinary tract infection (5%)
    • Hypertension (4%)
    • Hypokalemia (4%)
    • Anxiety (4%)
    • Diarrhea (4%)
    • Insomnia (4%)
    • Neutrophil counts <1,000 cell/m3 (3.4%)
    • Platelets counts <50,000 cells/mcL (3.2%)
    • Nausea (3%)

    May cause neutropenia, decreased platelets, elevated liver transaminases, and increased lipid parameters; monitor neutrophils, platelets, lipids, and liver function tests every 4-8 weeks

    Impact of treatment is unknown regarding development of malignancies, but malignancies were observed in clinical studies; treatment with immunosuppressants may increase risk of malignancies

    Anaphylaxis or serious hypersensitivity reactions have occurred, including fatalities, with or without concomitant arthritis therapies

    Impact of treatment with tocilizumab on demyelinating disorders is unknown, but multiple sclerosis and chronic inflammatory demyelinating polyneuropathy were reported rarely in RA clinical studies; monitor for signs and symptoms potentially indicative of demyelinating disorders

    Caution if increased risk for GI perforation; gastrointestinal perforation reported, primarily as complications of diverticulitis; promptly evaluate patients presenting with new onset abdominal symptoms for early identification of gastrointestinal perforation

    Insufficient data available in pregnant women to determine whether there is a drug-associated risk for major birth defects and miscarriage

    No data available on the presence of tocilizumab in human milk, effects of the drug on the breastfed infant, or effects of the drug on milk production

    May use alone or in combination with methotrexate or other DMARDs

    Not recommended in patients with an ANC<1,000/mm3 , platelet count <50,000 mm3, or ALT/AST >10x ULN

    IV infusion

    4 mg/kg IV q4Weeks initially; may increase to 8 mg/kg q4Weeks based on clinical response  

    Not to exceed 800 mg/dose q4weeks

    SC injection

    • Weight <100 kg: 162 mg SC every other week, followed by an increase to weekly based on clinical response
    • Weight ≥100 kg: 162 mg SC weekly

    Giant Cell Arteritis

    Not recommended in patients with an ANC<1,000/mm3 , platelet count <50,000 mm3, or ALT/AST >10x ULN

    IV

    • 6 mg/kg IV q4Weeks in combination with tapering course of glucocorticoids
    • May be used alone following glucocorticoid discontinuation; if necessary, interrupt dosing for management of dose-related laboratory abnormalities (eg, elevated liver enzymes, neutropenia, thrombocytopenia)
    • Not to exceed 600 mg/infusion

    SC

    • 162 mg SC weekly in combination with a tapering course of glucocorticoids
    • Based on clinical considerations, may consider 162 mg SC every other week in combination with tapering course of glucocorticoids
    • May be used alone following glucocorticoid discontinuation; if necessary, interrupt dosing for management of dose-related laboratory abnormalities (eg, elevated liver enzymes, neutropenia, thrombocytopenia)
    • Transitioning from IV to SC
      • Administer first SC dose instead of next scheduled IV dose
      • Dose interruption or reduced administration frequency of SC dose from every week to every other week dosing may be needed for management of dose-related laboratory abnormalities

    Systemic Sclerosis-Associated Interstitial Lung Disease

    162 mg SC qWeek

    Dose interruption may be needed for managing dose-related laboratory abnormalities (eg, elevated liver enzymes, neutropenia, thrombocytopenia)

    SC administration with prefilled ACTPen autoinjector not studied in SSc-ILD

    IV administration not approved for SSc-ILD

    Not recommended in patients with an ANC<1,000/mm3, platelet count <50,000 mm3, or ALT/AST >10x ULN

    Cytokine Release Syndrome

    8 mg/kg IV once; may be administered as alone or in combination with corticosteroids

    If no clinical improvement in the signs and symptoms of CRS occurs after initial dose, may administer up to 3 additional doses; allow 8-hr interval between consecutive doses

    Not approved for SC administration

    tocilizumab

    injectable solution

    • 20mg/mL (4-, 10-, and 20-mL single-dose vials)

    injection, single-use autoinjector (ACTPen) for SC

    • 162mg/0.9mL

    injection, single-use prefilled syringe for SC

    • 162mg/0.9mL