N

Enbrel (Etanercept)

Immunex (Amgen)

Dimeric fusion protein between TNF

receptor and IgGi

Subcutaneous

Mediates ADCC and CDL

Neutralizes the biological activity of TNF-a; KA = O.lnM

Neutralizes the biological activity of TNF-a

Dose escalation: 3, 10, 30 mgas tolerated. Maintenance dose is 30 mg three times per week.

3 or 10 mg/ kg every 4 or 8 weeks with concurrent methotrexate

Hematologic toxicity; infusion reactions; opportunistic infections resulting in grade 3 or 4 sepsis

Risk of infection; infusion related reactions ANA formation

Risk of infection; ANA formation; mild injection site reaction

Known hypersensitivities to components of drug; preexisting immunodeficiency; no drug interactions

Known IgE hypersensitivity to murine proteins; no drug interactions

Known hypersensitivity to components; sepsis

Half life = 12 days; eliminated by RES

Half-life = 8-9.5 days; eliminated by RES

Half life 102 h; eliminated by RES

tigens have been approved by the FDA as ra-dioconjugates for diagnostic imaging applications. These radiolabeled antibodies search out and bind primary and metastatic tumors, revealing their locations on scanning of cancer patients. Because these radiolabeled antibodies are of mouse origin and have not been humanized using genetic engineering techniques, they will not be discussed here.

Over the past 5-10 years, the promise of antibodies as "magic bullets" in treating disease has been partially realized. The FDA has approved 15 antibodies for use in humans as therapeutic treatments and/or imaging agents at the time of this writing. Therapeutic antibodies for cancer and rheumatoid arthritis are listed in Table 6.1.

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