Identification
- Summary
Efalizumab is a monoclonal anti-CD11a antibody used to treat moderate to severe plaque psoriasis.
- Generic Name
- Efalizumab
- DrugBank Accession Number
- DB00095
- Background
Humanized IgG1 kappa isotype monoclonal antibody that binds to human CD11a. Efalizumab has a molecular weight of approximately 150 kilodaltons and is produced in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin. The FDA approved efalizumab in 2003. It was later withdrawn in 2009 due to a potential risk of progressive multifocal leukoencephalopathy (PML).4
- Type
- Biotech
- Groups
- Approved, Investigational, Withdrawn
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>Heavy Chain Variable Region EVQLVESGGGLVQPGGSLRLSCAASGYSFTGHWMNWVRQAPGKGLEWVGIMIHPSDSETR YNQKFKDIRFTISVDKSKNTLYLQMNSLRAEDTAVYYCARIGIYFYGTTYFDYIWGQGTL VTVSS
>Light Chain Variable Region DIQMTQSPSSLSASVGDRVTITCRASKTISKYLAWXQQKPGKAPKLLIYSGSTLQSGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQHNEYPLTFGQGTKVEIKR
Download FASTA Format- Synonyms
- anti-CD11a
- antiCD11 alpha
- Efalizumab
- External IDs
- HU-1124
- HU1124
Pharmacology
- Indication
For the treatment of adult patients with moderate to severe chronic plaque psoriasis, who are candidates for phototherapy or systemic therapy.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Moderate to severe chronic plaque psoriasis •••••••••••• •••••••••• ••• •••••••• ••••••• ••• ••••••••• •••••••••• ••••••• ••• •••••••• Management of Moderate to severe chronic plaque psoriasis •••••••••••• •••••••••• ••• •••••••••••• •••••••••• ••••••• ••• •••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Lymphocyte activation and trafficking to skin play a role in the pathophysiology of chronic plaque psoriasis. In psoriatic skin, ICAM-1 cell surface expression is upregulated on endothelium and keratinocytes. Raptiva inhibits the binding of LFA-1 to the intercellular adhesion molecule-1 (ICAM-1), thereby inhibiting the adhesion of leukocytes to other cell types.
- Mechanism of action
Efalizumab binds to CD11a, a subunit of leukocyte function antigen-1 (LFA-1), which is expressed on all leukocytes. As a result efalizumab decreases cell surface expression of CD11a.
Target Actions Organism AIntegrin alpha-X antibodyHumans AIntegrin alpha-L antibodyHumans - Absorption
Average efalizumab bioavailability following subcutaneous administration was estimated at 30 to 50%.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
5 days
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of adverse effects can be increased when Efalizumab is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Efalizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Efalizumab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Efalizumab. Aducanumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Aducanumab. - Food Interactions
- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Xanelim
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Raptiva Injection, powder, for solution 100 mg/ml Subcutaneous Serono Europe Limited 2016-09-08 2009-08-04 EU 
Raptiva Injection, powder, for solution 100 mg/ml Subcutaneous Serono Europe Limited 2016-09-08 2009-08-04 EU Raptiva Injection, powder, for solution 100 mg/ml Subcutaneous Serono Europe Limited 2016-09-08 2009-08-04 EU Raptiva Powder, for solution 150 mg / vial Subcutaneous Emd Serono, A Division Of Emd Inc., Canada 2005-10-26 2009-06-08 Canada 
Categories
- ATC Codes
- L04AA21 — Efalizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antigens, CD11
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Cancer immunotherapy
- CD11a-directed Antibody Interactions
- CD11a-directed Humanized IgG1 Antibody
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Immunotherapy
- Proteins
- Selective Immunosuppressants
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- XX2MN88N5D
- CAS number
- 214745-43-4
References
- General References
- Werther WA, Gonzalez TN, O'Connor SJ, McCabe S, Chan B, Hotaling T, Champe M, Fox JA, Jardieu PM, Berman PW, Presta LG: Humanization of an anti-lymphocyte function-associated antigen (LFA)-1 monoclonal antibody and reengineering of the humanized antibody for binding to rhesus LFA-1. J Immunol. 1996 Dec 1;157(11):4986-95. [Article]
- Descamps V: [Efalizumab]. Ann Dermatol Venereol. 2006 Aug-Sep;133(8-9 Pt 1):666-78. [Article]
- FDA Approved Drug Products: Raptiva (efalizumab) for subcutaneous injection [Link]
- US Food & Drug Administration: FDA Statement on the Voluntary Withdrawal of Raptiva From the U.S. Market [Link]
- External Links
- PubChem Substance
- 46505252
- 356988
- ChEMBL
- CHEMBL1201575
- Therapeutic Targets Database
- DAP001095
- PharmGKB
- PA164748817
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Efalizumab
- FDA label
- Download (1.45 MB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Candidates for Systemic Therapy for Psoriasis / Psoriasis 1 4 Completed Treatment Psoriasis 5 4 Completed Treatment Psoriasis Vulgaris (Plaque Psoriasis) 1 4 Terminated Treatment Chronic Plaque Psoriasis 3 4 Unknown Status Treatment Chronic Plaque Psoriasis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Genentech Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Subcutaneous 100 mg/ml Powder, for solution Subcutaneous 150 mg / vial Injection, powder, lyophilized, for solution Subcutaneous 125 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 61 °C (FAB fragment), 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Integrin alpha-X/beta-2 is a receptor for fibrinogen. It recognizes the sequence G-P-R in fibrinogen. It mediates cell-cell interaction during inflammatory responses. It is especially important in monocyte adhesion and chemotaxis.
- Specific Function
- Metal ion binding
- Gene Name
- ITGAX
- Uniprot ID
- P20702
- Uniprot Name
- Integrin alpha-X
- Molecular Weight
- 127828.18 Da
References
- Pan WZ, Shi CX, Tian M, Yu JG: Anti-CD11c antibody, Efalizumab attenuate ventilator-induced lung injury. Eur Rev Med Pharmacol Sci. 2014;18(15):2182-90. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Metal ion binding
- Specific Function
- Integrin alpha-L/beta-2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. It is involved in a variety of immune phenomena including leukocyte-endothelial cell interaction, cytotoxic T-cell mediated ...
- Gene Name
- ITGAL
- Uniprot ID
- P20701
- Uniprot Name
- Integrin alpha-L
- Molecular Weight
- 128768.495 Da
References
- Frampton JE, Plosker GL: Efalizumab: a review of its use in the management of chronic moderate-to-severe plaque psoriasis. Am J Clin Dermatol. 2009;10(1):51-72. doi: 10.2165/0128071-200910010-00009. [Article]
- Descamps V: [Efalizumab]. Ann Dermatol Venereol. 2006 Aug-Sep;133(8-9 Pt 1):666-78. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Wellington K, Perry CM: Efalizumab. Am J Clin Dermatol. 2005;6(2):113-8; discussion 119-20. doi: 10.2165/00128071-200506020-00006. [Article]
Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:41