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Table 1 Selected TNF inhibitors.

From: TNF signaling inhibition in the CNS: implications for normal brain function and neurodegenerative disease

Inhibitor (Trade name) Class Description/Mode of Action Specificity Developer and Stage References
Adalimumab (Humira) Monoclonal antibody Humanized bivalent mouse IgG1 monoclonal antibody; binds to ligands solTNF, tmTNF Abbott FDA approved 2005 [100103, 179, 180]
Apratastat Small molecule Dual TACE and MMP inhibitor MMPs, TACE Wyeth Phase II terminated 2006 [121]
BMS-561392 Small molecule Specific TACE inhibitor TACE Bristol-Myers Squibb Phase II [121]
Certolizumab (Cimzia) Monoclonal antibody PEGylated antibody fragment solTNF, tmTNF UCB FDA approved 2008 [182]
CYT007-TNFQb Vaccine Anti-TNF vaccine TNF Cytos Biotechnology Phase I-IIa [181]
DN-TNF (XPro1595) Inactive TNF variant TNF monomers engineered with point mutations to disrupt binding to TNFRs; exchange with solTNF to form dominant-negative heterotrimers; tmTNF-sparing solTNF Xencor Preclinical [105, 106]
ESBA105 Antibody fragment Single-chain antibody fragment directed against TNF TNF Esbatech (Zurich) Preclinical [181]
Etanercept (Enbrel) Receptor biologic Human IgG fused to a dimer of the extracellular regions of TNFR2; binds to ligands solTNF, tmTNF,
Lympotoxin A
Amgen; Wyeth; Takeda FDA approved 1998 [179, 180]
Golimumab (CNTO148) Monoclonal antibody Human monoclonal antibody; binds to ligands solTNF, tmTNF Centocor, Schering-Plough Phase III [101]
GW333 Small molecule Dual TACE and MMP inhibitor MMPs, TACE GlaxoSmithKline Preclinical [121]
Infliximab (Remicade) Monoclonal antibody Murine-human Chimeric bivalent IgG1 monoclonal antibody; binds to ligands solTNF, tmTNF Centocor Schering-Plough FDA approved 1998 [179, 180]
Lenercept Receptor biologic Dimeric TNFR1 receptor extracellular domain fused to a human IgG1heavy chain fragment; binds to ligands solTNF, tmTNF,
Lympotoxin A
Roche Phase III terminated [101, 131, 183]
Minocycline Small molecule Broad-spectrum tetracycline antibiotic; inhibits synthesis of TNF and other inflammatory mediators solTNF, tmTNF, MMPs, COX-2, prostaglandin E2 Off patent [110117]
tgAAC94 Gene therapy AAV vectors containing the TNFR2:Fc fusion solTNF, tmTNF,
Lympotoxin A
Targeted Genetics Phase I-II [184]
Thalidomide Small molecule Immunomodulatory drug; increases degradation of mRNA of a number of inflammatory genes TNF, COX-2, IL-1β, TGF-β, IL-12 and IL-6. Celgene Corporation FDA approved 1998 [118, 119]
  1. Abbreviations: solTNF, soluble tumor necrosis factor; tmTNF, transmembrane tumor necrosis factor; TACE, tumor necrosis factor alpha converting enzyme; MMP, matrix metalloprotease; DN-TNF, dominant-negative tumor necrosis factor; TNFR, tumor necrosis factor receptor; COX-2, cyclo-oxygenase-2; IL1-β, interleukin-1beta; TGF-β, transforming growth factor beta; IL-12, interleukin-12; IL-6, interleukin-6.