Table 1.
Name (trade name; sponsoring companies) | Effector protein | Impact of Fc domain on PK | Targets | Disease | Proposed mechanisms of action | Reference |
---|---|---|---|---|---|---|
Alefacept (Amevive; Astellas) | Human leukocyte function antigen-3 (LFA-3) | Prolong half-life | CD2 | Plaque psoriasis | Inhibition of CD2-dependent lymphocyte activation | 89 |
Etanercept (Enbrel; Amgen/Pfizer) | p75 TNFαR | Prolong half-life | TNFα | RA, JIA, PA, AS and plaque psoriasis | Neutralization of TNFα activity | 55 |
Abatacept (Orencia; Bristol-Myers Squibb) | Cytotoxic T-lymphocyte antigen-4 (CTLA-4) | Prolong half-life | CD80 and CD86 | RA and JIA | Inhibition of CD80/86-dependent T cell activation | 90 |
Romiplostim (Nplate; Amgen) | Peptide | Prolong half-life | Thrombo-poietin receptor | Thrombocytopaenia in patients with idiopathic thrombocytopaenic purpura | Activation of thrombopoietin receptor | 91 |
Rilonacept (Arcalyst; Regeneron) | Ligand-binding domains of IL-1 receptor and IL-1 receptor accessory protein (IL-1RAcP) | Prolong half-life | IL-1 | CAPS | Neutralization of IL-1 activity | 56 |
Belatacept (Nulojix; tol-Myers Squibb) | Cytotoxic T-lymphocyte antigen-4 (CTLA-4) | Prolong half-life | CD80 and CD86 | prophylaxis of organ rejection in adult patients receiving a kidney transplant | Inhibition of CD80/86-dependent T cell activation | 8 |
Aflibercept (Eylea; Regeneron) | Vascular endothelial growth factor receptor 1 and 2 (VEGFR 1 and 2) | Prolong half-life | VEGF-A, VEGF-B, PIGF | neovascular (Wet) age-related macular degeneration | Neutralization of VEGF activity | 9 |
Abbreviation: AS, ankylosing spondylitis; CAPS, cryopyrin-associated periodic syndrome; Fc, crystallizable fragment; IL, interleukin; JIA, juvenile idiopathic arthritis; PA, psoriatic arthritis; PIGF, placental growth factor; RA, rheumatoid arthritis; TNFα, tumor necrosis factor-α; VEGF, vascular endothelial growth factor.