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Identification
NameOmalizumab
Accession NumberDB00043  (BTD00081, BIOD00081)
TypeBiotech
GroupsApproved, Investigational
DescriptionA recombinant DNA-derived humanized IgG1k monoclonal antibody that selectively binds to human immunoglobulin E (IgE). Xolair is produced by a Chinese hamster ovary cell suspension culture in a nutrient medium containing the antibiotic gentamicin.
Protein structureDb00043
Related Articles
Protein chemical formulaC6450H9916N1714O2023S38
Protein average weight145058.2 Da
Sequences
>Omalizumab heavy chain
EVQLVESGGGLVQPGGSLRLSCAVSGYSITSGYSWNWIRQAPGKGLEWVASITYDGSTNY
ADSVKGRFTISRDDSKNTFYLQMNSLRAEDTAVYYCARGSHYFGHWHFAVWGQGTLVTVS
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK
>Omalizumab light chain
DIQLTQSPSSLSASVGDRVTITCRASQSVDYDGDSYMNWYQQKPGKAPKLLIYAASYLES
GVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSHEDPYTFGQGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNR
Download FASTA Format
Synonyms
Ig gamma-1 chain C region
External IDs Not Available
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
XolairPowder, for solution150 mgSubcutaneousNovartis2005-02-03Not applicableCanada
XolairInjection, solution202.5 mg/1.4mLSubcutaneousGenentech, Inc.2003-06-20Not applicableUs
XolairSolution75 mgSubcutaneousNovartisNot applicableNot applicableCanada
XolairSolution150 mgSubcutaneousNovartisNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNII2P471X1Z11
CAS number242138-07-4
Pharmacology
IndicationFor treatment of asthma caused by allergies
Structured Indications
PharmacodynamicsXolair inhibits the binding of IgE to the high-affinity IgE receptor (FceRI) on the surface of mast cells and basophils. Reduction in surface-bound IgE on FceRI-bearing cells limits the degree of release of mediators of the allergic response. Xolair is used to treat severe, persisten asthma.
Mechanism of actionXolair binds to IgE (a class of antibodies normally secreted in allergic responses), which prevents their binding to mast cells and basophils.
TargetKindPharmacological actionActionsOrganismUniProt ID
High affinity immunoglobulin epsilon receptor subunit alphaProteinyesNot AvailableHumanP12319 details
High affinity immunoglobulin epsilon receptor subunit betaProteinyes
antagonist
HumanQ01362 details
Related Articles
AbsorptionNot Available
Volume of distribution
  • 78 ± 32 mL/kg
Protein bindingNot Available
Metabolism

Most likely removed by opsonization via the reticuloendothelial system.

Route of eliminationLiver elimination of IgG includes degradation in the liver reticuloendothelial system (RES) and endothelial cells. Intact IgG is also excreted in bile.
Half life26 days
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
BelimumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Belimumab.Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Omalizumab.Investigational
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Omalizumab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Omalizumab.Investigational
LoxapineThe risk or severity of adverse effects can be increased when Omalizumab is combined with Loxapine.Approved
RindopepimutThe therapeutic efficacy of CDX-110 can be decreased when used in combination with Omalizumab.Investigational
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Omalizumab.Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Karagiannis SN, Wang Q, East N, Burke F, Riffard S, Bracher MG, Thompson RG, Durham SR, Schwartz LB, Balkwill FR, Gould HJ: Activity of human monocytes in IgE antibody-dependent surveillance and killing of ovarian tumor cells. Eur J Immunol. 2003 Apr;33(4):1030-40. [PubMed:12672069 ]
External Links
ATC CodesR03DX05
AHFS Codes
  • 48:92.00
PDB Entries
FDA labelDownload (53.5 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0Unknown StatusTreatmentMilk Allergy1
1Active Not RecruitingTreatmentSjogren's Syndrome / Systemic Lupus Erthematosus1
1CompletedBasic ScienceEosinophilic Esophagitis1
1CompletedTreatmentAllergic Rhinitis (AR) / Asthma, Allergic / Healthy Volunteers / Moderate, refractory Atopic dermatitis1
1CompletedTreatmentHyper-IgE Syndrome / Job's Syndrome1
1CompletedTreatmentImmune System Diseases1
1CompletedTreatmentModerate, refractory Atopic dermatitis1
1RecruitingSupportive CareColon Cancer1
1RecruitingTreatmentDrug Allergy1
1, 2Active Not RecruitingTreatmentFood Allergy / Peanut Allergies1
1, 2CompletedTreatmentAsthma, Allergic1
1, 2CompletedTreatmentFood Allergy1
1, 2CompletedTreatmentPeanut Allergies1
1, 2CompletedTreatmentPeanut Hypersensitivity1
2Active Not RecruitingBasic ScienceAsthma1
2Active Not RecruitingTreatmentCholinergic Urticaria1
2Active Not RecruitingTreatmentChronic Spontaneous Urticaria1
2Active Not RecruitingTreatmentPeanut Allergies1
2CompletedBasic ScienceCat Allergy1
2CompletedTreatmentAllergies / Hay Fever / Hypersensitivity / Rhinitis1
2CompletedTreatmentAsthma1
2CompletedTreatmentAsthma, Allergic1
2CompletedTreatmentAsthma / Nasal Polyposis1
2CompletedTreatmentChronic Idiopathic Urticaria1
2CompletedTreatmentChronic Rhinosinusitis1
2CompletedTreatmentChronic Urticaria1
2CompletedTreatmentCold Contact Urticaria1
2CompletedTreatmentEczema, Atopic / Moderate, refractory Atopic dermatitis1
2CompletedTreatmentEsophagitis1
2CompletedTreatmentFood Allergy1
2CompletedTreatmentFood Allergy / Peanut Allergies1
2CompletedTreatmentGastroenteritis1
2CompletedTreatmentMilk Allergy1
2CompletedTreatmentPeanut Hypersensitivity1
2CompletedTreatmentSolar Urticaria1
2CompletedTreatmentSymptomatic Dermographism1
2CompletedTreatmentUrticarias1
2Enrolling by InvitationTreatmentChronic Urticaria1
2RecruitingTreatmentAcute Interstitial Nephritis1
2RecruitingTreatmentAnaphylaxis / Angioedema / Bronchospasm / Hypotension1
2RecruitingTreatmentFood Allergy1
2TerminatedTreatmentAllergies1
2Unknown StatusTreatmentAsthma1
2WithdrawnPreventionPulmonary Disease, Chronic Obstructive1
2, 3CompletedBasic ScienceChronic Idiopathic Urticaria / Chronic Spontaneous Urticaria / Chronic Urticaria1
2, 3CompletedTreatmentAsthma1
2, 3CompletedTreatmentAsthma, Allergic1
2, 3RecruitingTreatmentEosinophilic Bronchitis / Steroid and/or Prednisone Dependent Asthma1
2, 3Unknown StatusTreatmentBronchial Asthma1
3CompletedBasic ScienceAsthma1
3CompletedBasic ScienceAsthma, Allergic1
3CompletedTreatmentAngioedema / Chronic Spontaneous Urticaria1
3CompletedTreatmentAsthma11
3CompletedTreatmentAsthma, Allergic3
3CompletedTreatmentChonic Spontaneous Urticaria1
3CompletedTreatmentChronic Idiopathic Urticaria3
3CompletedTreatmentChronic Spontaneous Uriticaria1
3CompletedTreatmentInterstitial Cystitis / Painful Bladder Syndrome (PBS)1
3CompletedTreatmentPersistent Allergic Asthma1
3Not Yet RecruitingPreventionAsthma1
3Unknown StatusTreatmentChronic Idiopathic Urticaria1
4Active Not RecruitingTreatmentAsthma1
4Active Not RecruitingTreatmentChronic Idiopathic Urticaria1
4Active Not RecruitingTreatmentChronic Urticaria1
4CompletedNot AvailableAsthma, Allergic1
4CompletedNot AvailableModerate, refractory Atopic dermatitis1
4CompletedBasic ScienceAsthma1
4CompletedDiagnosticAsthma, Allergic1
4CompletedTreatmentAllergic Rhinitis (AR) / Asthma / Moderate, refractory Atopic dermatitis1
4CompletedTreatmentAspirin Sensitivity1
4CompletedTreatmentAsthma14
4CompletedTreatmentAsthma, Allergic3
4CompletedTreatmentBullous Pemphigoid (BP)1
4CompletedTreatmentChronic Lung Diseases1
4CompletedTreatmentChronic Spontaneous Urticaria1
4CompletedTreatmentPersistent Allergic Asthma1
4CompletedTreatmentSinusitis1
4Not Yet RecruitingTreatmentIdiopathic angioedema1
4RecruitingTreatmentAsthma1
4RecruitingTreatmentChildren / Eczema, Atopic / Moderate, refractory Atopic dermatitis1
4RecruitingTreatmentSevere IgE-mediated Asthma1
4RecruitingTreatmentUrticarias1
4TerminatedTreatmentAspergillosis, Allergic Bronchopulmonary / Cystic Fibrosis (CF)1
4Unknown StatusBasic ScienceAllergies1
4Unknown StatusTreatmentAsthma1
4Unknown StatusTreatmentAsthma, Allergic2
4WithdrawnTreatmentAllergy Induced Asthma1
4WithdrawnTreatmentChronic Rhinosinusitis1
Not AvailableCompletedNot AvailableAsthma1
Not AvailableCompletedBasic ScienceAllergic Rhinitis (AR)1
Not AvailableCompletedBasic ScienceAllergies1
Not AvailableCompletedBasic ScienceAsthma1
Not AvailableRecruitingNot AvailableChronic Idiopathic Urticaria1
Not AvailableRecruitingTreatmentAllergies / Bee Venom / Immunotherapy / Omalizumab1
Not AvailableTerminatedPreventionAllergies / Asthma1
Not AvailableTerminatedTreatmentAsthma1
Not AvailableUnknown StatusTreatmentAllergic Rhinitis (AR) / Asthma1
Not AvailableUnknown StatusTreatmentUrticarias1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous202.5 mg/1.4mL
Powder, for solutionSubcutaneous150 mg
SolutionSubcutaneous150 mg
SolutionSubcutaneous75 mg
Prices
Unit descriptionCostUnit
Xolair 150 mg vial715.42USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340233 No1998-12-152015-12-15Canada
CA2113813 No2005-04-122012-08-14Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point61 °C (FAB fragment), 71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.432Not Available
isoelectric point7.03Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Ige receptor activity
Specific Function:
Binds to the Fc region of immunoglobulins epsilon. High affinity receptor. Responsible for initiating the allergic response. Binding of allergen to receptor-bound IgE leads to cell activation and the release of mediators (such as histamine) responsible for the manifestations of allergy. The same receptor also induces the secretion of important lymphokines.
Gene Name:
FCER1A
Uniprot ID:
P12319
Molecular Weight:
29595.67 Da
References
  1. Beck LA, Marcotte GV, MacGlashan D, Togias A, Saini S: Omalizumab-induced reductions in mast cell Fce psilon RI expression and function. J Allergy Clin Immunol. 2004 Sep;114(3):527-30. [PubMed:15356552 ]
  2. Mirkina I, Schweighoffer T, Kricek F: Inhibition of human cord blood-derived mast cell responses by anti-Fc epsilon RI mAb 15/1 versus anti-IgE Omalizumab. Immunol Lett. 2007 Apr 15;109(2):120-8. Epub 2007 Mar 1. [PubMed:17368811 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Ige receptor activity
Specific Function:
High affinity receptor that binds to the Fc region of immunoglobulins epsilon. Aggregation of FCER1 by multivalent antigens is required for the full mast cell response, including the release of preformed mediators (such as histamine) by degranulation and de novo production of lipid mediators and cytokines. Also mediates the secretion of important lymphokines. Binding of allergen to receptor-bou...
Gene Name:
MS4A2
Uniprot ID:
Q01362
Molecular Weight:
26533.365 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. DuBuske LM: IgE, allergic diseases, and omalizumab. Curr Pharm Des. 2006;12(30):3929-44. [PubMed:17073688 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23