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Identification
NameOmalizumab
Accession NumberDB00043  (BIOD00081, BTD00081)
TypeBiotech
GroupsApproved, Investigational
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 structureDb00043
Protein chemical formulaC6450H9916N1714O2023S38
Protein average weight145058.2000
Sequences
>Omalizumab heavy chain
EVQLVESGGGLVQPGGSLRLSCAVSGYSITSGYSWNWIRQAPGKGLEWVASITYDGSTNY
ADSVKGRFTISRDDSKNTFYLQMNSLRAEDTAVYYCARGSHYFGHWHFAVWGQGTLVTVS
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK
>Omalizumab light chain
DIQLTQSPSSLSASVGDRVTITCRASQSVDYDGDSYMNWYQQKPGKAPKLLIYAASYLES
GVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSHEDPYTFGQGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNR
Download FASTA Format
Synonyms
SynonymLanguageCode
Ig gamma-1 chain C regionNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
XolairGenentech Inc
Brand mixturesNot Available
Categories
CAS number242138-07-4
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationFor treatment of asthma caused by allergies
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.
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
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionSubcutaneous
Prices
Unit descriptionCostUnit
Xolair 150 mg vial715.42USDvial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada21138132005-04-122012-08-14
Canada13402331998-12-152015-12-15
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
References
Synthesis ReferenceNot Available
General Reference
  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
External Links
ResourceLink
UniProtP01857
GenbankJ00228
PharmGKBPA164752253
Drug Product Database2260565
RxListhttp://www.rxlist.com/cgi/generic/xolair.htm
Drugs.comhttp://www.drugs.com/cdi/omalizumab.html
WikipediaOmalizumab
ATC CodesR03DX05
AHFS Codes
  • 48:92.00
PDB Entries
FDA labelshow(53.5 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
BelimumabAvoid combination due to enhanced toxic effects of monoclonal antibodies.
DenosumabMonitor therapy due to increased risk of infections consequent to increased adverse effects of immunosuppressants.
LeflunomideConsider modifying therapy due to increased adverse effects of leflunomide including hematological toxicity.
NatalizumabAvoid combination due to enhanced adverse effects of natalizumab including the risk of infections.
PimecrolimusAvoid combination due to enhanced adverse effects of immunosuppressants.
RoflumilastConsider therapy modification due to enhanced immunosuppressive effects.
Sipuleucel-TMonitor therapy due to diminished therapeutic effect of sipuleucel-t.
TacrolimusAvoid combination due to enhanced adverse toxic effects.
TofacitinibAvoid combination due to enhanced immunosuppressive effect of tofacitinib.
TrastuzumabMonitor therapy due to enhanced neutropenic effect of immunosuppressants.
Food InteractionsNot Available

Targets

1. High affinity immunoglobulin epsilon receptor subunit alpha

Kind: protein

Organism: Human

Pharmacological action: yes

Components

Name UniProt ID Details
High affinity immunoglobulin epsilon receptor subunit alpha P12319 Details

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
  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

2. High affinity immunoglobulin epsilon receptor subunit beta

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
High affinity immunoglobulin epsilon receptor subunit beta Q01362 Details

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
  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
  3. DuBuske LM: IgE, allergic diseases, and omalizumab. Curr Pharm Des. 2006;12(30):3929-44. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on January 22, 2014 11:15