Currently available interleukin 1 inhibitors
| Agent | Mechanism of action | Current FDA-approved indications and dosing | Contraindications and cautions |
|---|---|---|---|
| Anakinra (Kineret) | Recombinant human IL-1 receptor antagonist Inhibits activity of IL-1 alpha and IL-1 beta | Rheumatoid arthritis: 100 mg subcutaneously once a day CAPS/NOMID: 1-2 mg/kg subcutaneously once a day; can increase by 0.5-1 mg/kg increments; maximum dose 8 mg/kg Renal dosing: if creatinine clearance is < 30 mL/min or patient is in end-stage renal disease, consider alternate dosing | Use with caution in patients with: Concomitant TNF inhibitor use Serious active infection Neutropenia |
| Canakinumab (Ilaris) | Human monoclonal anti-IL-1 beta Neutralizes IL-1 beta activity | Systemic juvenile idiopathic arthritis: 4 mg/kg subcutaneously once a month; not to exceed 300 mg/dose (≥ 2 years and weight ≥ 7.5 kg) CAPS: If 15-40 kg, 2 mg/kg subcutaneously every 8 weeks If ≥ 40 kg, 150 mg subcutaneously every 8 weeks FMF, TRAPS and HIDS/MVD: If ≤ 40 kg, 2 mg/kg subcutaneously every 4 weeks, can increase to 4 mg/kg every 4 weeks If > 40 kg, 150 mg subcutaneously every 4 weeks; can increase to 300 mg every 4 weeks | Use with caution in patients with serious active infection |
| Rilonacept (Arcalyst) | Fusion protein of extracellular domains of IL-1-RAcP and IL-1-R1 fused to FC portion of human IgG1 Binds to IL-1 alpha and IL-1 beta to block IL-1 signaling | CAPS: Adults—loading dose 320 mg subcutaneously, followed by 160 mg subcutaneously weekly Children (12-17 years)—loading dose of 4.4 mg/kg (maximum dose 320 mg), followed by 2.2 mg/kg subcutaneously weekly (maximum dose 160 mg) | Use with caution in patients with serious active infection |
CAPS = cryopyrin-associated periodic syndromes; FC = fragment crystallizable; FMF = familial Mediterranean fever, HIDS/MKD = hyperimmunoglobulin D syndrome/mevalonate kinase deficiency; IG = immunoglobulin; IL = interleukin; IL-1-RAcP = IL-1 receptor accessory protein; IL-1-R1 = interleukin 1 receptor, type I; NOMID = neonatal-onset multisystem inflammatory disease; TNF = tumor necrosis factor; TRAPS = tumor necrosis factor receptor associated periodic syndrome