NAV

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. 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 It was later withdrawn in 2009 due to a potential risk of progressive multifocal leukoencephalopathy (PML).4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Approved, Investigational, Withdrawn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.

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Associated Conditions
Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
AIntegrin alpha-X
antibody
Humans
AIntegrin alpha-L
antibody
Humans
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
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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.
DrugInteraction
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interactions in your software
AbataceptThe risk or severity of adverse effects can be increased when Efalizumab is combined with Abatacept.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Efalizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Efalizumab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Efalizumab.
AducanumabThe risk or severity of adverse effects can be increased when Efalizumab is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Efalizumab.
AlefaceptThe risk or severity of adverse effects can be increased when Alefacept is combined with Efalizumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Efalizumab.
AlirocumabThe risk or severity of adverse effects can be increased when Efalizumab is combined with Alirocumab.
Allogeneic processed thymus tissueThe therapeutic efficacy of Allogeneic processed thymus tissue can be decreased when used in combination with Efalizumab.
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Food Interactions
Not Available

Products

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International/Other Brands
Xanelim
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
RaptivaPowder, for solution150 mg / vialSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2005-10-262009-06-08Canada flag
RaptivaInjection, powder, for solution100 mg/mlSubcutaneousSerono Europe Limited2016-09-082009-08-04EU flag
RaptivaInjection, powder, for solution100 mg/mlSubcutaneousSerono Europe Limited2016-09-082009-08-04EU flag
RaptivaInjection, powder, for solution100 mg/mlSubcutaneousSerono Europe Limited2016-09-082009-08-04EU flag

Categories

ATC Codes
L04AA21 — Efalizumab
Drug Categories
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
  1. 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]
  2. Descamps V: [Efalizumab]. Ann Dermatol Venereol. 2006 Aug-Sep;133(8-9 Pt 1):666-78. [Article]
  3. FDA Approved Drug Products: Raptiva (efalizumab) for subcutaneous injection [Link]
  4. US Food & Drug Administration: FDA Statement on the Voluntary Withdrawal of Raptiva From the U.S. Market [Link]
PubChem Substance
46505252
RxNav
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
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCandidates for Systemic Therapy for Psoriasis / Psoriasis (PsO)1
4CompletedTreatmentPsoriasis (PsO)5
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4TerminatedTreatmentChronic Plaque Psoriasis3
4Unknown StatusTreatmentChronic Plaque Psoriasis1
3CompletedTreatmentPsoriasis (PsO)5
3CompletedTreatmentPsoriasis, Moderate to Severe2
2CompletedTreatmentAtopic Dermatitis1
2CompletedTreatmentRheumatoid Arthritis1
2CompletedTreatmentType 1 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Genentech Inc.
Dosage Forms
FormRouteStrength
Injection, powder, for solutionSubcutaneous100 mg/ml
Powder, for solutionSubcutaneous150 mg / vial
Injection, powder, lyophilized, for solutionSubcutaneous125 mg
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
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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Details1. Integrin alpha-X
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
  1. 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]
Details2. Integrin alpha-L
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
  1. 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]
  2. Descamps V: [Efalizumab]. Ann Dermatol Venereol. 2006 Aug-Sep;133(8-9 Pt 1):666-78. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  4. 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 November 03, 2022 16:14