Efalizumab Explained

Verifiedfields:changed
Verifiedrevid:461092863
Type:mab
Mab Type:mab
Source:zu/o
Target:CD11a
Tradename:Raptiva
Routes Of Administration:Subcutaneous
Atc Prefix:L04
Atc Suffix:AG02
Cas Number:214745-43-4
Drugbank:DB00095
Chemspiderid:none
Unii:XX2MN88N5D
Chembl:1201575
Melting Point:66

Efalizumab (brand name Raptiva, Genentech, Merck Serono) is a formerly available medication designed to treat autoimmune diseases, originally marketed to treat psoriasis. As implied by the suffix -zumab, it is a recombinant humanized monoclonal antibody administered once weekly by subcutaneous injection. Efalizumab binds to the CD11a[1] subunit of lymphocyte function-associated antigen 1 and acts as an immunosuppressant by inhibiting lymphocyte activation and cell migration out of blood vessels into tissues. Efalizumab was associated with fatal brain infections and was withdrawn from the market in 2009.

Known side effects include bacterial sepsis, viral meningitis, invasive fungal disease and progressive multifocal leukoencephalopathy (PML), a brain infection caused by reactivation of latent JC virus infection.[2] [3] Four cases of PML were reported in plaque psoriasis patients, an incidence of approximately one in 500 treated patients.[4]

Due to the risk of PML, the European Medicines Agency (EMA) and the Food and Drug Administration (FDA) recommend suspension from the market in the European Union and the United States, respectively.[5] In April 2009, Genentech Inc. announced a phased voluntary withdrawal of Raptiva from the U.S. market.[4] [6]

Notes and References

  1. Li S, Wang H, Peng B, Zhang M, Zhang D, Hou S, Guo Y, Ding J . Efalizumab binding to the LFA-1 alphaL I domain blocks ICAM-1 binding via steric hindrance . Proceedings of the National Academy of Sciences of the United States of America . 106 . 11 . 4349–54 . March 2009 . 19258452 . 2657446 . 10.1073/pnas.0810844106 . 2009PNAS..106.4349L . free .
  2. Web site: Efalizumab FDA Warning. 16 October 2008. 7 December 2008.
  3. Berger JR, Houff SA, Major EO . Monoclonal antibodies and progressive multifocal leukoencephalopathy . mAbs . 1 . 6 . 583–9 . 2009 . 20073129 . 2791316 . 10.4161/mabs.1.6.9884 .
  4. Major EO . Progressive multifocal leukoencephalopathy in patients on immunomodulatory therapies . Annual Review of Medicine . 61 . 1 . 35–47 . 2010 . 19719397 . 10.1146/annurev.med.080708.082655 .
  5. Web site: EMEA press release regarding suspension . 20 February 2009 . dead . https://web.archive.org/web/20091226101218/http://www.emea.europa.eu/humandocs/PDFs/EPAR/raptiva/2085709en.pdf . 26 December 2009 .
  6. Genentech Announces Voluntary Withdrawal of Raptiva from the U.S. Market . Genentech, Inc. . 8 April 2009 . 9 April 2009 . https://web.archive.org/web/20110528052448/http://www.drugs.com/news/genentech-announces-voluntary-raptiva-u-s-market-17125.html . 28 May 2011 . dead .