Table 1.
Type, mechanism of action and FDA- and EMA-approved indications of currently available anti-TNF-α agents (modified from ref. [2]).
Agent | Type | Target | Mechanism of action | Mode of administrationa | Approved indications |
---|---|---|---|---|---|
Infliximab (Remicade® and biosimilars) | Human-mouse chimeric IgG1 monoclonal antibody | mTNF-α, sTNF-α | Neutralization, apoptosis, reverse signaling, ADCC, CDC | IV injection every 6-8 weeks | IBD (CD and UC), RA, AS, PsA,plaque psoriasis |
Etanercept (Enbrel®) | Fusion protein of the soluble TNFR2/p75 receptor and human IgG1 antibody (hinge, CH2 and CH3 domains of the Fc region) | mTNF-α, sTNF-α, TNF-β | Competitive inhibition, ADCC, CDC (weaker) | SC injection once or twice weekly | RA, AS, JIA, PsA, plaque psoriasis |
Adalimumab (Humira®) | Fully human IgG1 monoclonal antibody | mTNF-α, sTNF-α | Neutralization, apoptosis, reverse signaling, ADCC, CDC | SC injection every 2 weeks | IBD (CD and UC), RA, AS, JIA, PsA, plaque psoriasis, hidradenitis, suppurativa, uveitis |
Golimumab (Simponi®) | Fully human IgG1 monoclonal antibody | mTNF-α, sTNF-α | Neutralization, apoptosis, reverse signaling, ADCC, CDC | SC injection every 4 weeks | UC, RA, AS, JIA, PsA |
Certolizumab pegol (Cimzia®) | PEGylated Fab’ fragment of humanized IgG4 monoclonal antibody | mTNF-α, sTNF-α | Neutralization, reverse signaling | SC injection every 2-4 weeks | CD (only FDA), RA, AS, PsA, plaque psoriasis (only EMA) |
ADCC: antibody-dependent cell-mediated cytotoxicity; AS: ankylosing spondylitis; CD: Crohn’s disease; CDC: complement-dependent cytotoxicity; EMA: European Medicines Agency; FDA: Food and Drug Administration; IBD: inflammatory bowel disease; IV: intravenous; JIA: juvenile idiopathic arthritis; PS: plaque psoriasis; PsA: psoriatic arthritis; RA: rheumatoid arthritis; SC: subcutaneous; sTNF-α: soluble tumor necrosis factor α;mTNF- α: membrane-bound tumor necrosis factor α; UC: ulcerative colitis. aMaintenance doses once clinical response has been observed; initial doses vary according to the indication.