indication

Investigated for use/treatment in rheumatoid arthritis, juvenile rheumatoid arthritis, inflammatory disorders (unspecified), and autoimmune diseases.

pharmacology

Novartis AG is developing canakinumab, an intravenously or subcutaneously infused, fully human mAb that neutralizes the bioactivity of human IL-1beta, which is involved in several inflammatory disorders. Canakinumab has promising clinical safety and pharmacokinetic properties, and demonstrated potential for the treatment of cryopyrin-associated periodic syndromes (CAPS) and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, systemic-onset juvenile idiopathic arthritis (SoJIA), COPD disease and ocular diseases. Early clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist anakinra, which must be injected daily and which is often poorly tolerated by patients.

mechanism of action

Canakinumab is a human monoclonal anti-human IL-1β antibody of the IgG1/κ isotype. Canakinumab binds to human IL-1β and neutralizes its activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1α or IL-1 receptor antagonist (IL-1ra).

absorption

The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.

half life

26 days