ATC Group: L04AB Tumor necrosis factor alpha (TNF-α) inhibitors

Adalimumab binds specifically to TNF and neutralizes the biological function of TNF by blocking its interaction with the p55 and p75 cell surface TNF receptors. Adalimumab also modulates biological responses that are induced or regulated by TNF, including changes in the levels of adhesion molecules responsible for leukocyte migration (ELAM-1, VCAM-1, and ICAM-1 with an IC₅₀ of 0.1-0.2 nM).

Afelimomab is an anti-TNFα monoclonal antibody. Administration of afelimomab reduces the concentration of interleukin-6 in patients with sepsis, but reduces mortality only marginally.

Certolizumab pegol has a high affinity for human TNFα and binds with a dissociation constant (KD) of 90 pM. TNFα is a key pro-inflammatory cytokine with a central role in inflammatory processes. Certolizumab pegol was shown to neutralise membrane associated and soluble human TNFα in a dose-dependent manner. By inhibiting the action of TNFα, certolizumab pegol reduces inflammation and other symptoms in patients with rheumatoid arthritis.

Etanercept is a competitive inhibitor of TNF binding to its cell surface receptors, and thereby inhibits the biological activity of TNF. The mechanism of action of etanercept is thought to be its competitive inhibition of TNF binding to cell surface TNFR, preventing TNF-mediated cellular responses by rendering TNF biologically inactive.

Golimumab is a human monoclonal antibody that forms high affinity, stable complexes with both the soluble and transmembrane bioactive forms of human TNF-α, which prevents the binding of TNF-α to its receptors.

Infliximab is a chimeric human-murine monoclonal antibody that binds with high affinity to both soluble and transmembrane forms of TNFα but not to lymphotoxin α (TNFβ).