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Showing drug card for Omalizumab (DB00043)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:19
Primary Accession Number DB00043
Secondary Accession Number
  • BIOD00081
  • BTD00081
Name Omalizumab
Drug Type
  • Approved
  • Biotech
  • 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.
Synonyms
  1. Ig gamma-1 chain C region
Brand Names
  1. Xolair (Genentech Inc)
Brand Mixtures Not Available
Chemical IUPAC Name Humanized anti-IgE antibody
Chemical Formula C6450H9916N1714O2023S38
Chemical Structure Structure
Protein Sequence(s) >Anti IgE antibody VH domain chain 1 
EVQLVESGGGLVQPGGSLRLSCAVSGYSITSGYSWNWIRQAPGKGLEWVASITYDGSTNY
ADSVKGRFTISRDDSKNTFYLQMNSLRAEDTAVYYCARGSHYFGHWHFAVWGQGTLVTVS
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK

>Anti IgE antibody VH domain chain 2 
EVQLVESGGGLVQPGGSLRLSCAVSGYSITSGYSWNWIRQAPGKGLEWVASITYDGSTNY
ADSVKGRFTISRDDSKNTFYLQMNSLRAEDTAVYYCARGSHYFGHWHFAVWGQGTLVTVS
SGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY
SLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKAEPKSCDKTHTCPPCPAPELLGGPSV
FLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTY
RVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTK
NQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQG
NVFSCSVMHEALHNHYTQKSLSLSPGK

>Anti IgE antibody VL domain chain 1 
DIQLTQSPSSLSASVGDRVTITCRASQSVDYDGDSYMNWYQQKPGKAPKLLIYAASYLES
GVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSHEDPYTFGQGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNR

>Anti IgE antibody VL domain chain 2 
DIQLTQSPSSLSASVGDRVTITCRASQSVDYDGDSYMNWYQQKPGKAPKLLIYAASYLES
GVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQSHEDPYTFGQGTKVEIKRTVAAPSVF
IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS
STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNR
CAS Registry Number 242138-07-4
InChI Identifier Not Available
InChI Key Not Available
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound Not Available
PubChem Substance Not Available
ChEBI ID Not Available
PharmGKB ID PA10374 Link Image
HET ID Not Available
GenBank ID J00228 Link Image
Drug ID Number [DIN] 02260565 Link Image
RxList Link http://www.rxlist.com/cgi/generic/xolair.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Omalizumab Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Sequence in Presta et al., J. of Immunol. 151, 2623 1993
Average Molecular Weight 145058.2000
Monoisotopic Molecular Weight Not Available
State Liquid
Melting Point 61 oC (FAB fragment), 71 oC (whole mAb) - Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000).
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility Not Available Calculated using ALOGPS
Experimental LogP/Hydrophobicity -0.432 Source: PhysProp
Predicted LogP Not Available Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS Not Available Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 7.03
Mass Spectrum Not Available
MOL File Not Available
SDF File Not Available
PDB File Not Available
Experimental PDB ID 1IGT Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES Not Available
Canonical SMILES Not Available
Drug Category
  • Anti-Asthmatic Agents
  • Immunomodulatory Agents
ATC Codes
AHFS Codes
  • 48:92.00
Indication For treatment of asthma caused by allergies
Pharmacology 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.
Absorption Not Available
Toxicity Not Available
Protein Binding Not Available
Biotransformation Most likely removed by opsonization via the reticuloendothelial system.
Half Life 26 days
Dosage Forms
Form Route
Powder, for solution Subcutaneous
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not 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 Link Image]
  2. Drugs.com Link Image
  3. Wikipedia Link Image
  4. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. High affinity immunoglobulin epsilon receptor subunit alpha
  2. High affinity immunoglobulin epsilon receptor subunit beta
Drug Target 1 [top]
Target 1 ID 18
Target 1 Name High affinity immunoglobulin epsilon receptor subunit alpha
Target 1 Synonyms
  1. Fc-epsilon RI-alpha
  2. FcERI
  3. High affinity immunoglobulin epsilon receptor subunit alpha precursor
  4. IgE Fc receptor, alpha-subunit
Target 1 Gene Name FCER1A
Target 1 Protein Sequence >High affinity immunoglobulin epsilon receptor alpha-subunit precursor 
MAPAMESPTLLCVALLFFAPDGVLAVPQKPKVSLNPPWNRIFKGENVTLTCNGNNFFEVS
STKWFHNGSLSEETNSSLNIVNAKFEDSGEYKCQHQQVNESEPVYLEVFSDWLLLQASAE
VVMEGQPLFLRCHGWRNWDVYKVIYYKDGEALKYWYENHNISITNATVEDSGTYYCTGKV
WQLDYESEPLNITVIKAPREKYWLQFFIPLLVVILFAVDTGLFISTQQQVTFLLKIKRTR
KGFRLLNPHPKPNPKNN
Target 1 Number of Residues 261
Target 1 Molecular Weight 29596
Target 1 Theoretical pI 6.67
Target 1 GO Classification Not Available
Target 1 General Function Not Available
Target 1 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
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-25
Target 1 Transmembrane Regions
  • 206-224
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 31318 Link Image
Target 1 UniProtKB/Swiss-Prot ID P12319 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name FCERA_HUMAN Link Image
Target 1 PDB ID 1RPQ Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Membrane
  • single-pass type I membrane protein
Target 1 Gene Sequence >774 bp 
ATGGCTCCTGCCATGGAATCCCCTACTCTACTGTGTGTAGCCTTACTGTTCTTCGCTCCA
GATGGCGTGTTAGCAGTCCCTCAGAAACCTAAGGTCTCCTTGAACCCTCCATGGAATAGA
ATATTTAAAGGAGAGAATGTGACTCTTACATGTAATGGGAACAATTTCTTTGAAGTCAGT
TCCACCAAATGGTTCCACAATGGCAGCCTTTCAGAAGAGACAAATTCAAGTTTGAATATT
GTGAATGCCAAATTTGAAGACAGTGGAGAATACAAATGTCAGCACCAACAAGTTAATGAG
AGTGAACCTGTGTACCTGGAAGTCTTCAGTGACTGGCTGCTCCTTCAGGCCTCTGCTGAG
GTGGTGATGGAGGGCCAGCCCCTCTTCCTCAGGTGCCATGGTTGGAGGAACTGGGATGTG
TACAAGGTGATCTATTATAAGGATGGTGAAGCTCTCAAGTACTGGTATGAGAACCACAAC
ATCTCCATTACAAATGCCACAGTTGAAGACAGTGGAACCTACTACTGTACGGGCAAAGTG
TGGCAGCTGGACTATGAGTCTGAGCCCCTCAACATTACTGTAATAAAAGCTCCGCGTGAG
AAGTACTGGCTACAATTTTTTATCCCATTGTTGGTGGTGATTCTGTTTGCTGTGGACACA
GGATTATTTATCTCAACTCAGCAGCAGGTCACATTTCTCTTGAAGATTAAGAGAACCAGG
AAAGGCTTCAGACTTCTGAACCCACATCCTAAGCCAAACCCCAAAAACAACTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID FCER1A Link Image
Target 1 GenAtlas ID FCER1A Link Image
Target 1 HGNC ID HGNC:3609 Link Image
Target 1 Chromosome Location 1
Target 1 Locus 1q23
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Padlan EA, Helm BA: A modeling study of the alpha-subunit of human high-affinity receptor for immunoglobulin-E. Receptor. 1992 Summer;2(2):129-44. [PubMed Link Image]
  2. Shimizu A, Tepler I, Benfey PN, Berenstein EH, Siraganian RP, Leder P: Human and rat mast cell high-affinity immunoglobulin E receptors: characterization of putative alpha-chain gene products. Proc Natl Acad Sci U S A. 1988 Mar;85(6):1907-11. [PubMed Link Image]
  3. Kochan J, Pettine LF, Hakimi J, Kishi K, Kinet JP: Isolation of the gene coding for the alpha subunit of the human high affinity IgE receptor. Nucleic Acids Res. 1988 Apr 25;16(8):3584. [PubMed Link Image]
  4. Yagi S, Yanagida M, Tanida I, Hasegawa A, Okumura K, Ra C: High-level expression of the truncated alpha chain of human high-affinity receptor for IgE as a soluble form by baculovirus-infected insect cells. Biochemical characterization of the recombinant product. Eur J Biochem. 1994 Mar 1;220(2):593-8. [PubMed Link Image]
Target 1 Drug 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 Link Image]
  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 Link Image]
Drug Target 2 [top]
Target 2 ID 3862
Target 2 Name High affinity immunoglobulin epsilon receptor subunit beta
Target 2 Synonyms
  1. Fc epsilon receptor I beta-chain
  2. FcERI
  3. IgE Fc receptor subunit beta
  4. Membrane-spanning 4-domains subfamily A member 2
Target 2 Gene Name MS4A2
Target 2 Protein Sequence >High affinity immunoglobulin epsilon receptor subunit beta 
MDTESNRRANLALPQEPSSVPAFEVLEISPQEVSSGRLLKSASSPPLHTWLTVLKKEQEF
LGVTQILTAMICLCFGTVVCSVLDISHIEGDIFSSFKAGYPFWGAIFFSISGMLSIISER
RNATYLVRGSLGANTASSIAGGTGITILIINLKKSLAYIHIHSCQKFFETKCFMASFSTE
IVVMMLFLTILGLGSAVSLTICGAGEELKGNKVPEDRVYEELNIYSATYSELEDPGEMSP
PIDL
Target 2 Number of Residues 248
Target 2 Molecular Weight 26534
Target 2 Theoretical pI 4.78
Target 2 GO Classification
Function
signal transducer activity
receptor activity
Process
cellular process
cell communication
signal transduction
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Not Available
Target 2 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
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 60-79
  • 98-117
  • 131-150
  • 181-200
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 219882 Link Image
Target 2 UniProtKB/Swiss-Prot ID Q01362 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name FCERB_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
Target 2 Gene Sequence >735 bp 
ATGGACACAGAAAGTAATAGGAGAGCAAATCTTGCTCTCCCACAGGAGCCTTCCAGTGTG
CCTGCATTTGAAGTCTTGGAAATATCTCCCCAGGAAGTATCTTCAGGCAGACTATTGAAG
TCGGCCTCATCCCCACCACTGCATACATGGCTGACAGTTTTGAAAAAAGAGCAGGAGTTC
CTGGGGGTAACACAAATTCTGACTGCTATGATATGCCTTTGTTTTGGAACAGTTGTCTGC
TCTGTACTTGATATTTCACACATTGAGGGAGACATTTTTTCATCATTTAAAGCAGGTTAT
CCATTCTGGGGAGCCATATTTTTTTCTATTTCTGGAATGTTGTCAATTATATCTGAAAGG
AGAAATGCAACATATCTGGTGAGAGGAAGCCTGGGAGCAAACACTGCCAGCAGCATAGCT
GGGGGAACGGGAATTACCATCCTGATCATCAACCTGAAGAAGAGCTTGGCCTATATCCAC
ATCCACAGTTGCCAGAAATTTTTTGAGACCAAGTGCTTTATGGCTTCCTTTTCCACTGAA
ATTGTAGTGATGATGCTGTTTCTCACCATTCTGGGACTTGGTAGTGCTGTGTCACTCACA
ATCTGTGGAGCTGGGGAAGAACTCAAAGGAAACAAGGTTCCAGAGGATCGTGTTTATGAA
GAATTAAACATATATTCAGCTACTTACAGTGAGTTGGAAGACCCAGGGGAAATGTCTCCT
CCCATTGATTTATAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID MS4A2 Link Image
Target 2 GenAtlas ID MS4A2 Link Image
Target 2 HGNC ID HGNC:7316 Link Image
Target 2 Chromosome Location 11
Target 2 Locus 11q13
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Maekawa K, Imagawa N, Tanaka Y, Harada S: Determination of the sequence coding for the beta subunit of the human high-affinity IgE receptor. FEBS Lett. 1992 May 11;302(2):161-5. [PubMed Link Image]
  2. Kuster H, Zhang L, Brini AT, MacGlashan DW, Kinet JP: The gene and cDNA for the human high affinity immunoglobulin E receptor beta chain and expression of the complete human receptor. J Biol Chem. 1992 Jun 25;267(18):12782-7. [PubMed Link Image]
  3. Hill MR, Cookson WO: A new variant of the beta subunit of the high-affinity receptor for immunoglobulin E (Fc epsilon RI-beta E237G): associations with measures of atopy and bronchial hyper-responsiveness. Hum Mol Genet. 1996 Jul;5(7):959-62. [PubMed Link Image]
  4. Shirakawa T, Mao XQ, Sasaki S, Enomoto T, Kawai M, Morimoto K, Hopkin J: Association between atopic asthma and a coding variant of Fc epsilon RI beta in a Japanese population. Hum Mol Genet. 1996 Aug;5(8):1129-30. [PubMed Link Image]
  5. Shirakawa T, Mao XQ, Sasaki S, Enomoto T, Kawai M, Morimoto K, Hopkin J: Association between atopic asthma and a coding variant of Fc epsilon RI beta in a Japanese population. Hum Mol Genet. 1996 Dec;5(12):2068. [PubMed Link Image]
Target 2 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.