Omalizumab

Identification

Name
Omalizumab
Accession Number
DB00043  (BTD00081, BIOD00081)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

A 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 structure
Db00043
Protein chemical formula
C6450H9916N1714O2023S38
Protein average weight
145058.2 Da
Sequences
>Omalizumab heavy chain
EVQLVESGGGLVQPGGSLRLSCAVSGYSITSGYSWNWIRQAPGKGLEWVASITYDGSTNY
ADSVKGRFTISRDDSKNTFYLQMNSLRAEDTAVYYCARGSHYFGHWHFAVWGQGTLVTVS
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK
>Omalizumab light chain
DIQLTQSPSSLSASVGDRVTITCRASQSVDYDGDSYMNWYQQKPGKAPKLLIYAASYLES
GVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSHEDPYTFGQGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNR
Download FASTA Format
Synonyms
Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
XolairPowder, for solution150 mgSubcutaneousNovartis2005-02-03Not applicableCanada
XolairSolution150 mgSubcutaneousNovartis2017-07-06Not applicableCanada
XolairInjection, solution202.5 mg/1.4mLSubcutaneousGenentech, Inc.2003-06-20Not applicableUs
XolairSolution75 mgSubcutaneousNovartis2017-06-28Not applicableCanada
Categories
UNII
2P471X1Z11
CAS number
242138-07-4

Pharmacology

Indication

For treatment of asthma caused by allergies

Structured Indications
Pharmacodynamics

Xolair 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 action

Xolair binds to IgE (a class of antibodies normally secreted in allergic responses), which prevents their binding to mast cells and basophils.

TargetActionsOrganism
AHigh affinity immunoglobulin epsilon receptor subunit alphaNot AvailableHuman
AHigh affinity immunoglobulin epsilon receptor subunit beta
antagonist
Human
Absorption
Not Available
Volume of distribution
  • 78 ± 32 mL/kg
Protein binding
Not Available
Metabolism

Most likely removed by opsonization via the reticuloendothelial system.

Route of elimination

Liver elimination of IgG includes degradation in the liver reticuloendothelial system (RES) and endothelial cells. Intact IgG is also excreted in bile.

Half life

26 days

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Omalizumab.Investigational
BelimumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Belimumab.Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Omalizumab.Approved
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Omalizumab.Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Omalizumab.Investigational
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Omalizumab.Investigational
Hepatitis A VaccineThe therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Omalizumab.Approved
Hepatitis B Vaccine (Recombinant)The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Omalizumab.Approved, Withdrawn
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
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Omalizumab.Approved
RindopepimutThe therapeutic efficacy of Rindopepimut can be decreased when used in combination with Omalizumab.Investigational
Rotavirus VaccineThe therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Omalizumab.Approved
Rubella virus vaccineThe therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Omalizumab.Approved
Salmonella typhi ty21a live antigenThe therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Omalizumab.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Omalizumab.Investigational
TecemotideThe therapeutic efficacy of Tecemotide can be decreased when used in combination with Omalizumab.Investigational
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Omalizumab.Investigational
Yellow fever vaccineThe therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Omalizumab.Approved
Zoster vaccineThe therapeutic efficacy of Zoster vaccine can be decreased when used in combination with Omalizumab.Approved
Food Interactions
Not Available

References

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
UniProt
P01857
Genbank
J00228
PubChem Substance
46507002
ChEMBL
CHEMBL1201589
Therapeutic Targets Database
DAP000387
PharmGKB
PA164752253
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Omalizumab
ATC Codes
R03DX05 — Omalizumab
AHFS Codes
  • 48:92.00 — Respiratory Agents, Miscellaneous
FDA label
Download (53.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Unknown StatusTreatmentMilk Allergy1
1CompletedBasic ScienceOesophagitis, Eosinophilic1
1CompletedTreatmentAllergic Rhinitis (AR) / Asthma, Allergic / Atopic Dermatitis (AD) / Healthy Volunteers1
1CompletedTreatmentAtopic Dermatitis (AD)1
1CompletedTreatmentHyper IgE Syndromes / Hyper-IgE Syndrome1
1CompletedTreatmentImmune System Diseases1
1CompletedTreatmentSjögren's Syndrome / Systemic Lupus Erthematosus1
1RecruitingSupportive CareMalignant Neoplasm of Colon1
1RecruitingTreatmentDrug Allergy1
1, 2Active Not RecruitingTreatmentFood Allergy / Peanut Allergies1
1, 2CompletedTreatmentAsthma, Allergic1
1, 2CompletedTreatmentFood Allergy1
1, 2CompletedTreatmentPeanut Allergies1
1, 2CompletedTreatmentPeanut Hypersensitivity1
2Active Not RecruitingBasic ScienceAsthma Bronchial1
2Active Not RecruitingTreatmentPeanut Allergies1
2CompletedBasic ScienceCat Allergy1
2CompletedTreatmentAllergies / Hypersensitivity / Pollen Allergy / Rhinitis1
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentAsthma Bronchial / Nasal Polyposis1
2CompletedTreatmentAsthma, Allergic1
2CompletedTreatmentAtopic Dermatitis (AD)1
2CompletedTreatmentCholinergic Urticaria1
2CompletedTreatmentChronic Idiopathic Urticaria1
2CompletedTreatmentChronic Rhinosinusitis1
2CompletedTreatmentChronic Spontaneous Urticaria1
2CompletedTreatmentChronic Urticaria2
2CompletedTreatmentCold Contact Urticaria1
2CompletedTreatmentEsophagitis1
2CompletedTreatmentFood Allergy1
2CompletedTreatmentFood Allergy / Peanut Allergies1
2CompletedTreatmentGastroenteritis1
2CompletedTreatmentMilk Allergy1
2CompletedTreatmentPeanut Hypersensitivity1
2CompletedTreatmentSolar Urticaria1
2CompletedTreatmentSymptomatic Dermographism1
2CompletedTreatmentUrticarias1
2RecruitingTreatmentAcute Interstitial Nephritis1
2RecruitingTreatmentAnaphylaxis / Angioedema / Arterial Hypotension / Bronchospasm1
2RecruitingTreatmentFood Allergy2
2TerminatedTreatmentAllergies1
2Unknown StatusTreatmentAsthma Bronchial1
2WithdrawnPreventionPulmonary Disease, Chronic Obstructive1
2, 3CompletedBasic ScienceChronic Idiopathic Urticaria / Chronic Spontaneous Urticaria / Chronic Urticaria1
2, 3CompletedTreatmentAsthma Bronchial1
2, 3CompletedTreatmentAsthma, Allergic1
2, 3RecruitingTreatmentEosinophilic Bronchitis / Steroid and/or Prednisone Dependent Asthma1
2, 3Unknown StatusTreatmentBronchial Asthma1
3CompletedBasic ScienceAsthma Bronchial1
3CompletedBasic ScienceAsthma, Allergic1
3CompletedTreatmentAngioedema / Chronic Spontaneous Urticaria1
3CompletedTreatmentAsthma Bronchial11
3CompletedTreatmentAsthma, Allergic3
3CompletedTreatmentChonic Spontaneous Urticaria1
3CompletedTreatmentChronic Idiopathic Urticaria3
3CompletedTreatmentChronic Spontaneous Uriticaria1
3CompletedTreatmentInterstitial Cystitis / Painful Bladder Syndrome (PBS)1
3CompletedTreatmentPersistent Allergic Asthma1
3Not Yet RecruitingPreventionAsthma Bronchial1
3RecruitingTreatmentChronic Spontaneous Urticaria1
3RecruitingTreatmentNasal Polyps, Chronic Rhinosinusitis1
3RecruitingTreatmentNasal Polyps, Chronic Sinusitis1
3Unknown StatusTreatmentChronic Idiopathic Urticaria1
4Active Not RecruitingTreatmentChronic Urticaria1
4CompletedNot AvailableAsthma, Allergic1
4CompletedNot AvailableAtopic Dermatitis (AD)1
4CompletedBasic ScienceAsthma Bronchial1
4CompletedDiagnosticAsthma, Allergic1
4CompletedTreatmentAllergic Rhinitis (AR) / Asthma Bronchial / Atopic Dermatitis (AD)1
4CompletedTreatmentAspirin Sensitivity1
4CompletedTreatmentAsthma Bronchial15
4CompletedTreatmentAsthma, Allergic3
4CompletedTreatmentBullous Pemphigoid (BP)1
4CompletedTreatmentChronic Idiopathic Urticaria / Urticarias1
4CompletedTreatmentChronic Lung Diseases1
4CompletedTreatmentChronic Spontaneous Urticaria1
4CompletedTreatmentPersistent Allergic Asthma1
4CompletedTreatmentSinusitis1
4RecruitingTreatmentAsthma Bronchial1
4RecruitingTreatmentAtopic Dermatitis (AD) / Children1
4RecruitingTreatmentChronic Urticaria1
4RecruitingTreatmentIdiopathic angioedema1
4RecruitingTreatmentSevere IgE-mediated Asthma1
4RecruitingTreatmentUrticarias1
4TerminatedTreatmentAspergillosis, Allergic Bronchopulmonary / Cystic Fibrosis (CF)1
4Unknown StatusBasic ScienceAllergies1
4Unknown StatusTreatmentAsthma Bronchial1
4Unknown StatusTreatmentAsthma, Allergic2
4WithdrawnTreatmentAllergy Induced Asthma1
4WithdrawnTreatmentChronic Rhinosinusitis1
Not AvailableActive Not RecruitingNot AvailableAsthma Bronchial1
Not AvailableCompletedNot AvailableAsthma Bronchial1
Not AvailableCompletedBasic ScienceAllergic Rhinitis (AR)1
Not AvailableCompletedBasic ScienceAllergies1
Not AvailableCompletedBasic ScienceAsthma Bronchial1
Not AvailableRecruitingOtherChronic Idiopathic Urticaria1
Not AvailableRecruitingTreatmentAllergies / Bee Venom / Immunotherapy / Omalizumab1
Not AvailableTerminatedPreventionAllergies / Asthma Bronchial1
Not AvailableTerminatedTreatmentAsthma Bronchial1
Not AvailableUnknown StatusTreatmentAllergic Rhinitis (AR) / Asthma Bronchial1
Not AvailableUnknown StatusTreatmentUrticarias1

Pharmacoeconomics

Manufacturers
Not 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)
CA2113813No2005-04-122012-08-14Canada
CA1340233No1998-12-152015-12-15Canada

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)
hydrophobicity-0.432Not Available
isoelectric point7.03Not Available

Taxonomy

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

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 t...
Gene Name
FCER1A
Uniprot ID
P12319
Uniprot Name
High affinity immunoglobulin epsilon receptor subunit alpha
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 pre...
Gene Name
MS4A2
Uniprot ID
Q01362
Uniprot Name
High affinity immunoglobulin epsilon receptor subunit beta
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]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34