Efalizumab
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.
- Type
- Biotech
- Groups
- Approved, Investigational
- 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.
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- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- 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-L antibodyHumans AIntegrin alpha-X 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
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Efalizumab. Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Efalizumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Efalizumab. Alirocumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Alirocumab. Altretamine The risk or severity of adverse effects can be increased when Efalizumab is combined with Altretamine. Amsacrine The risk or severity of adverse effects can be increased when Efalizumab is combined with Amsacrine. 
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- Not Available
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- 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 Powder, for solution 150 mg / vial Subcutaneous Emd Serono, A Division Of Emd Inc., Canada 2005-10-26 2009-06-08 Canada 
Raptiva Injection, powder, for solution 100 mg/ml Subcutaneous Serono Europe Limited 2016-09-08 2009-08-04 EU
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
- Cell Migration Inhibition
- 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]
- Health Canada Product Monograph: Raptiva (efalizumab) for subcutaneous injection [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
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 3 Completed Treatment Psoriasis 5 3 Completed Treatment Psoriasis, Moderate to Severe 2 2 Completed Treatment Atopic Dermatitis (AD) 1 2 Completed Treatment Rheumatoid Arthritis 1 2 Completed Treatment Type 1 Diabetes Mellitus 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 - 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
- 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]
- 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]
Drug created on June 13, 2005 13:24 / Updated on April 03, 2021 09:33