Generic
Tocilizumab
5 brands available in the market
At a glance
Tocilizumab is an interleukin-6 (IL-6) receptor antagonist used for rheumatoid arthritis, polyarticular and systemic juvenile idiopathic arthritis, cytokine release syndrome, giant cell arteritis, and systemic sclerosis-associated interstitial lung disease.
Description
Tocilizumab is a recombinant humanized anti-human IL-6 receptor monoclonal antibody (IgG1κ). It binds to both soluble and membrane-bound IL-6 receptors, inhibiting IL-6-mediated signaling. IL-6 is a pro-inflammatory cytokine involved in T-cell activation, immunoglobulin secretion, hepatic acute phase protein synthesis, and hematopoietic precursor cell proliferation and differentiation.
Indications
- Rheumatoid arthritis (RA) – moderate to severe, inadequate response to DMARDs
- Polyarticular juvenile idiopathic arthritis (PJIA) – ≥2 years
- Systemic juvenile idiopathic arthritis (SJIA) – ≥2 years
- Cytokine release syndrome (CRS) – ≥2 years
- Giant cell arteritis (GCA)
- Systemic sclerosis-associated interstitial lung disease (SSc-ILD)
- COVID-19 (emergency use) – ≥2 years
Therapeutic class
Drugs Used for Rheumatoid Arthritis
Pharmacological class
IL-6 Receptor Antagonist (Monoclonal Antibody)
Pharmacology
Tocilizumab binds to both soluble and membrane-bound IL-6 receptors, inhibiting IL-6-mediated signaling. It reduces inflammation by inhibiting T-cell activation, immunoglobulin secretion, hepatic acute phase protein synthesis, and hematopoietic precursor cell proliferation and differentiation.
Mechanism of action
Reduces inflammation and immune response by blocking IL-6 receptors.
Dosage
Adult Dose (IV):
- Rheumatoid arthritis: 4 mg/kg every 4 weeks; may increase to 8 mg/kg every 4 weeks; max 800 mg/infusion
- Giant cell arteritis: 6 mg/kg every 4 weeks (with glucocorticoids); max 600 mg/infusion
- COVID-19: 8 mg/kg (≥30 kg) single dose; may repeat after 8 hours; max 800 mg/infusion
- CRS: 8 mg/kg (≥30 kg) or 12 mg/kg (<30 kg); up to 3 additional doses 8 hours apart; max 800 mg/infusion
Pediatric Dose (IV):
- PJIA (≥2 years): <30 kg: 10 mg/kg every 4 weeks; ≥30 kg: 8 mg/kg every 4 weeks
- SJIA (≥2 years): <30 kg: 12 mg/kg every 2 weeks; ≥30 kg: 8 mg/kg every 2 weeks
Administration
- IV infusion only (over 60 minutes); not bolus or push
- Dilute to 100 mL in NaCl for adults; 50 mL for children (<30 kg)
- Administered by a healthcare professional in a hospital
Missed dose
If you miss a dose, consult your doctor.
Side effects
Common Side Effects (≥5%):
- Upper respiratory tract infection
- Nasopharyngitis
- Headache
- Hypertension
- Increased ALT
- Injection site reactions
Serious:
- Serious infections (TB, bacterial, fungal, viral)
- GI perforation
- Hepatotoxicity
- Anaphylaxis
- Neutropenia, thrombocytopenia
Precautions & warnings
- Do not use during active infection
- Screen for TB before initiation
- Monitor liver enzymes, neutrophils, platelets, lipids regularly
- Avoid live vaccines
- Do not use with biological DMARDs
- May affect driving ability (dizziness)
Contraindications
- Hypersensitivity to tocilizumab
- Active infection
Drug interactions
- CYP3A4 substrates (oral contraceptives, lovastatin, atorvastatin): Effectiveness may decrease; dose adjustment may be needed
- Biological DMARDs: Do not use
- Live vaccines: Do not use
Food interactions
Alcohol is safe with Tocilizumab.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show fetal harm; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited data suggests no significant risk; consult your doctor.
Pediatric use
Indicated for PJIA, SJIA, CRS in children ≥2 years; not authorized for COVID-19 in children <2 years
Geriatric use
Higher incidence of infections in elderly; caution required
Renal / hepatic impairment
Renal Impairment: Mild-moderate: no dose adjustment; severe: not studied; consult your doctor.
Hepatic Impairment: Not recommended in active liver disease or hepatic impairment; consult your doctor.
Overdose effects
Overdose requires supportive treatment and monitoring; no specific antidote.
Storage conditions
Store at 2-8°C in a refrigerator; do not freeze; keep in a dry place.
Chemical structure
Tocilizumab