Currently available IL-6 inhibitors
| Agent | Mechanism of action | Current FDA-approved indications and dosing | Contraindications and cautions |
|---|---|---|---|
| Tocilizumab (Actemra) | Binds to soluble and membrane-bound IL-6 receptors and inhibits IL-6-mediated signaling | Rheumatoid arthritis: 4 mg/kg IV every 4 weeks (up to 8 mg/kg every 4 weeks); 162 mg SQ every other week (up to every week) Giant cell arteritis: 162 mg SQ once weekly or every other week Polyarticular juvenile idiopathic arthritis: 8 mg/kg IV every 4 weeks (10 mg/kg if < 30 kg); 162 mg SQ every other week (every 3 weeks if < 30 kg) Systemic juvenile idiopathic arthritis:8 mg/kg IV every other week (12 mg/kg if < 30 kg); 162 mg SQ every week (every other week if < 30 kg) Cytokine release syndrome (due to CAR-T cell therapy): 8 mg/kg IV (10 mg/kg if < 30 kg) | Avoid use in patients with: • ANC < 2,000/mm3 • Platelet count < 100,000/mm3 • ALT/AST > 1.5 × ULN • Tuberculosis or latent tuberculosis infection Use with caution in patients with: • Serious active infection • Increased risk of gastrointestinal perforation |
| Sarilumab (Kevzara) | Binds to soluble and membrane-bound IL-6 receptors and inhibits IL-6-mediated signaling | Moderately to severely active rheumatoid arthritis: 200 mg SQ every other week | Avoid use in patients with: • ANC < 2,000/mm3 • Platelet count < 150,000/mm3 • ALT/AST > 1.5 × ULN • Tuberculosis or latent tuberculosis infection Use with caution in patients with: • Serious active infection • Increased risk of gastrointestinal perforation |
| Siltuximab (Sylvant) | Binds to IL-6 and prevents binding of IL-6 to soluble and membrane-bound IL-6 receptors | Multicentric Castleman disease: 11 mg/kg IV over 1 hour every 3 weeks until treatment failure | Use with caution in patients with: • Serious active infection • Increased risk of gastrointestinal perforation |
ALT = alanine aminotransferase; ANC = absolute neutrophil count; AST = aspartate aminotransferase; CAR-T = chimeric antigen receptor T cell; IV = intravenously; SQ = subcutaneously; ULN = upper limit of normal