Table 1.
Monoclonal antibodies approved for therapeutic use
Generic name | Trade name | Antibody format | Antigen | Approved indication | 13FDA approval | 13EMEA approval |
---|---|---|---|---|---|---|
Muromomab | Orthoclone | Murine, IgG2a | CD3 | Allograft rejection in allogeneic renal transplantation | 86/06/19 | NA |
Abciximab1 | ReoPro | Chimeric, IgG1 | GPIIb/IIIa r | Maintenance of coronary patency | 94/12/22 | NA |
Rituximab2 | Mabthera | Chimeric, IgG1 | CD20 | CD20-positive B-cell non-Hodgkin's lymphoma | 97/11/26 | 98/06/02 |
Daclizumab | Zenapax | Humanized, IgG1 | CD25 (Il2r) | Allograft rejection | 97/12/10 | 99/02/26 |
Basiliximab | Simulect | Chimeric, IgG1 | CD25 (Il2r) | Allograft rejection | 98/05/12 | 98/10/09 |
Palivizumab | Synagis | Humanized, IgG1 | Protein F | Respiratory syncytial virus (RSV inhibitor) in children | 98/06/19 | 99/08/13 |
Infliximab | Remicade | Chimeric, IgG1 | TNFα | Crohn's disease and rheumatoid arthritis | 98/08/24 | 99/08/13 |
Trastuzumab | Herceptin | Humanized, IgG1 | HER2/Neu | Metastatic breast cancer | 98/09/25 | 00/08/28 |
Etanercept3 | Enbrel | huFcγ1/TNFr | TNFα and β | Autoimmune diseases such as ankylosing spondylitis | 98/11/02 | 00/02/03 |
Gemtuzumab4 | Mylotarg | Humanized, IgG4 | CD33 | CD33-positive acute myeloid leukemia | 00/05/17 | NA |
Alemtuzumab5 | Mabcampath | Humanized, IgG1 | CD52 | B-cell chronic lymphocytic leukemia | 01/05/07 | 01/07/06 |
Ibritomomab6 | Zevalin 90Y | Mouse, IgG1 | CD20 | B-cell non-Hodgkin's lymphoma | 02/02/19 | 04/01/16 |
Adalimumab7 | Trudexa | Human, IgG1 (PD) | TNFα | Crohn's disease and rheumatoid arthritis | 02/12/31 | 03/09/01 |
Alefacept3 | Amevive | huFcγ1/LFA-3 | CD2 | Chronic plaque psoriasis | 03/01/30 | NA |
Omalizumab | Xolair | Humanized, IgG1 | IgE | Treatment of asthma | 03/06/20 | 05/10/25 |
Tositumomab68 | Bexxar 131I | Murine, IgG2a | CD20 | CD20-positive B-cell non-Hodgkin's lymphoma | 03/06/27 | NA |
Efalizumab | Raptiva | Humanized, IgG1 | CD11a | Moderate to severe plaque psoriasis | 03/10/27 | 04/09/20 |
Cetuximab | Erbitux | Chimeric, IgG1 | EGFR | Metastatic colorectal and head and neck carcinoma | 04/02/12 | 04/06/29 |
Bevacizumab | Avastin | Humanized, IgG1 | VEGF-A | Metastatic colorectal and non-small cell lung carcinoma | 04/02/26 | 05/01/12 |
Natalizumab9 | Tysabri | Humanized, IgG4 | Integrin-α4 | Multiple sclerosis | 04/11/23 | 06/06/27 |
Ranibizumab | Lucentis | Humanized, IgG1 | VEGF-A | Wet-type age-related macular degeneration | 06/06/30 | 07/01/22 |
Panitumumab10 | Vectibis | Human, IgG2 | EGFR | Metastatic colorectal carcinoma | 06/09/27 | 07/12/19 |
Eculizumab11 | Soliris | Humanized, IgG2/4 | C5 | Paroxysmal nocturnal haemoglobinuria | 07/03/16 | 07/06/20 |
Certolizumab12 | Cimzia | Humanized, IgG1 | TNFα | Crohn's disease | 08/04/18 | NA |
Abciximab is a Fab fragment.
Rituximab is commercialized under the trade name Rituxan in USA.
These molecules are fusions between the IgG1 Fc portion and a receptor. On 2 May 2008, the FDA placed a black box warning on Etanercept due to a number of serious infections associated with the drug.
Gemtuzumab ‘ozogamicine’ is coupled to calicheamicin, an anti-tumoural antibiotic.
Alemtuzumab is commercialized under the trade name Campath in USA.
Ibritomomab ‘tiuxetan’ and Tositumomab are coupled to radioisotopes.
Adalimumab is commercialized under the trade name Humira in USA.
All approved antibodies have a κ light chain except Tositumomab that has a γ light chain.
Natalizumab was voluntarily withdrawn from the market in February 2005. On 5 June 2006, FDA approved a special restricted distribution programme.
Panitumumab is the first human antibody obtained from humanized mice.
Eculizumab contains a CH1 domain and hinge from IgG2, and CH2–CH3 domains from IgG4.
Certolizumab pegol is a PEGylated humanized Fab fragment.
Year/month/day; NA, not approved in Europe.
EGFR, epidermal growth factor receptor; EMEA, European Medicines Agency; FDA, US Food and Drug Administration; HER, human epidermal growth factor receptor; TNF, tumour necrosis factor; VEGF, vascular endothelial growth factor.