Efalizumab

Pharmaceutical drug

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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 Efalizumab was associated with fatal brain infections and was withdrawn from the market in 2009.^[2]

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.^[3]^[4] Four cases of PML were reported in plaque psoriasis patients, an incidence of approximately one in 500 treated patients.^[2]

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.^[2]^[6]

References

^ Li S, Wang H, Peng B, Zhang M, Zhang D, Hou S, et al. (March 2009). "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. Bibcode:2009PNAS..106.4349L. doi:10.1073/pnas.0810844106. PMC 2657446. PMID 19258452.
^ ^a ^b ^c Major EO (2010). "Progressive multifocal leukoencephalopathy in patients on immunomodulatory therapies". Annual Review of Medicine. 61 (1): 35–47. doi:10.1146/annurev.med.080708.082655. PMID 19719397.
^ "Efalizumab FDA Warning". 16 October 2008. Retrieved 7 December 2008.
^ Berger JR, Houff SA, Major EO (2009). "Monoclonal antibodies and progressive multifocal leukoencephalopathy". mAbs. 1 (6): 583–9. doi:10.4161/mabs.1.6.9884. PMC 2791316. PMID 20073129.
^ "EMEA press release regarding suspension" (PDF). Archived from the original (PDF) on 26 December 2009. Retrieved 20 February 2009.
^ "Genentech Announces Voluntary Withdrawal of Raptiva from the U.S. Market" (Press release). Genentech, Inc. 8 April 2009. Archived from the original on 28 May 2011. Retrieved 9 April 2009.

Immunosuppressive drugs / Immunosuppressants (L04)

Intracellular
(initiation)

Antimetabolites	purine synthesis inhibitors Azathioprine Mycophenolic acid dihydroorotate dehydrogenase inhibitors Leflunomide Teriflunomide antifolate Methotrexate
Macrolides/ other IL-2 inhibitors	FKBP/Cyclophilin/Calcineurin Ciclosporin Pimecrolimus Tacrolimus Voclosporin Abetimus Gusperimus
IMiDs	Lenalidomide Pomalidomide Thalidomide PDE4 inhibitor Apremilast

Intracellular
(reception)

IL-1 receptor antagonists	Anakinra
mTOR	Sirolimus Everolimus Ridaforolimus Temsirolimus Umirolimus Zotarolimus

Extracellular

Antibodies

Monoclonal

Serum target (noncellular)	Complement component 5 Eculizumab TNF Adalimumab Afelimomab Certolizumab pegol Golimumab Infliximab Nerelimomab Interleukin Anakinra Basiliximab Bimekizumab Briakinumab Brodalumab Canakinumab Daclizumab Guselkumab Ixekizumab Netakimab Olokizumab Rilonacept Risankizumab Sarilumab Satralizumab Secukinumab Siltuximab Sirukumab Spesolimab Tildrakizumab Tocilizumab Ustekinumab Interleukin 5 Mepolizumab Immunoglobulin E Omalizumab Interferon Faralimomab IL-6 Elsilimomab IL-12 and IL-23 Lebrikizumab Ustekinumab IL-17A Secukinumab
Cellular target	CD3 Muromonab-CD3 Otelixizumab Teplizumab Visilizumab CD4 Clenoliximab Keliximab Zanolimumab CD11a Efalizumab CD18 Erlizumab CD20 Obinutuzumab Ocrelizumab Pascolizumab Rituximab Ublituximab CD23 Gomiliximab Lumiliximab CD40 Teneliximab Toralizumab CD62L/L-selectin Aselizumab CD80 Galiximab CD147/Basigin Gavilimomab CD154 Ruplizumab Frexalimab BLyS Belimumab CAT Bertilimumab Lerdelimumab Metelimumab Integrin Natalizumab Vedolizumab Interleukin-6 receptor Tocilizumab LFA-1 Odulimomab IL-2 receptor/CD25 Basiliximab Daclizumab Inolimomab T-lymphocyte (Zolimomab aritox)
Unsorted	Alemtuzumab Anifrolumab Atorolimumab Begelomab Cedelizumab Emapalumab Fontolizumab Inebilizumab Maslimomab Morolimumab Ofatumumab Pexelizumab Reslizumab Rovelizumab Siplizumab Talizumab Telimomab aritox Teprotumumab Vapaliximab Vepalimomab

Polyclonal

-cept (Fusion)

CTLA-4
- Abatacept
- Belatacept
TNF inhibitor
- Etanercept
- Opinercept
Aflibercept
Alefacept
Rilonacept

Unsorted

Monoclonal antibodies for the immune system

Immune system

Human	Immunosuppression: Abrilumab Adalimumab^# Anifrolumab Atorolimumab Avelumab Avdoralimab Belimumab Bleselumab Brodalumab Camidanlumab tesirine Carlumab Cemiplimab Dupilumab Eldelumab Emapalumab Fresolimumab Golimumab Ianalumab^† Lanadelumab Lenzilumab Lerdelimumab Lirentelimab Lirilumab Mavrilimumab Metelimumab Morolimumab Namilumab Oleclumab Oxelumab§ Pamrevlumab Placulumab Relatlimab^† Sarilumab Sifalimumab Tabalumab Tezepelumab Ulocuplumab Varlilumab Immune activation: Ipilimumab Durvalumab Nivolumab Tremelimumab Urelumab Other: Bertilimumab Ontamalimab Zanolimumab Combination: Nivolumab/relatlimab
Mouse	Afelimomab Elsilimomab Faralimomab Gavilimomab Inolimomab Maslimomab Nerelimomab Odulimomab Telimomab aritox Vepalimomab Zolimomab aritox
Chimeric	Andecaliximab^† Basiliximab Clenoliximab Galiximab Gomiliximab Infliximab Keliximab Lumiliximab Priliximab Teneliximab Vapaliximab
Humanized	Immunosuppressive: Apolizumab^§ Aselizumab Atezolizumab Benralizumab Camrelizumab^† Cedelizumab Certolizumab pegol Crizanlizumab Daclizumab Eculizumab Efalizumab^‡ Epratuzumab Erlizumab Etrolizumab^† Fontolizumab Frexalimab^† Inebilizumab Itolizumab Lampalizumab^† Letolizumab Ligelizumab^† Lulizumab pegol Mepolizumab Mogamulizumab Natalizumab Ocrelizumab Omalizumab Ozoralizumab Pascolizumab Pateclizumab Pembrolizumab Pexelizumab Pidilizumab Plozalizumab PRO 140^† Quilizumab Ravulizumab Reslizumab Retifanlimab Rontalizumab Rovelizumab Ruplizumab Samalizumab Satralizumab Siplizumab Spartalizumab^† Talizumab Teclistamab Teplizumab Tislelizumab Tocilizumab Toralizumab Tregalizumab Vatelizumab Vedolizumab Visilizumab Vobarilizumab TGN1412^§ Immune activation: Dostarlimab Other: Ibalizumab
Chimeric + humanized	Otelixizumab Rozanolixizumab Sutimlimab

Interleukin

Human	Bermekimab Brazikumab Briakinumab Canakinumab Fezakinumab Fletikumab Guselkumab Secukinumab Sirukumab Tralokinumab Ustekinumab
Humanized	Anrukinzumab Bimekizumab Clazakizumab Gevokizumab Ixekizumab Mirikizumab^† Lebrikizumab Olokizumab^† Perakizumab Risankizumab Spesolimab Tildrakizumab
Veterinary	Lokivetmab

Inflammatory lesions

Mouse	Besilesomab Fanolesomab^‡ Lemalesomab Sulesomab

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

v t e Merck Serono
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Related	Merck Group Serono