Table 7-5 Biologically Engineered Immunomodulators |
| Name | | Route/Category | | Mechanism of Action | | Others |
| Etanercept (Enbrel) | | Subcutaneous
Category B | | TNFα inhibitor: fusion protein consisting of TNFα receptor linked to Fc portion of human IgG1; binds free (soluble) TNFα | | Avoid live vaccines
SE: multiple sclerosis, + ANA and LE symptoms, worsening of CHF, serious infections, TB reactivation, malignancy |
| Infliximab (Remicade) | | Intravenous
Category B | | TNFα inhibitor: chimeric monoclonal Ab against TNFα (mouse Fv/human IgG1); binds soluble and membrane-bound TNFα | | Avoid live vaccines
Category B SE: infusion reaction, other side effects similar to etanercept |
| Adalimumab (Humira) | | Subcutaneous
Category B | | TNFα inhibitor: fully human monoclonal Ab against TNFα; binds soluble and membrane-bound TNFα | | Same as other TNFα inhibitors |
| Golimumab (Simponi) (CNTO 148) | | Subcutaneous
Category B | | | | Same as other TNFα inhibitors |
| Certolizumab pegol (Cimzia) | | Subcutaneous
Category B | | TNFα inhibitor: human monoclonal Ab against TNFα; PEGylated Fab’ fragment of human TNFα monoclonal Ab | | Same as other TNFα inhibitors |
| Efalizumab (Raptiva) | | Subcutaneous
Category C | | Humanized form of murine Ab against CD11a, which blocks LFA1 interaction with CAM1; blocks lymphocyte extravasation | | Removed from market in 2009 due to risk of progressive multifocal leukoencephalopathy (PML) |
| Alefacept (Amevive) | | Intramuscular
Category B | | Fully human dimeric fusion protein: extracellular domain of LFA3 fused with human Fc portion of IgG1; inhibits CD2/LFA3 interaction thus blocking T-cell activation | | Monitor CD4 T-cell count weekly or every other week |
| Ustekinumab (Stelara) (CNTO 1275) | | Subcutaneous
Category B | | IL-12/IL-23 inhibitor: human IgG1 monoclonal antibody against p40 subunit of IL-12 and IL-23 cytokines (both cytokines share same p40 subunit) | | SE comparable to TNFα inhibitors |
| Briakinumab (ABT-874) | | Subcutaneous | | IL-12/IL-23 inhibitor | | Currently under investigation |
| AIN-547 | | | | Monoclonal antibody against IL-17 | | Currently under investigation |
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