Identification
- Summary
Omalizumab is a monoclonal anti-immunoglobulin E (IgE) antibody used to treat asthma, chronic idiopathic urticaria, chronic rhinosinusitis with nasal polyps, and IgE-mediated food allergy.
- Brand Names
- Xolair
- Generic Name
- Omalizumab
- DrugBank Accession Number
- DB00043
- Background
Omalizumab is a recombinant DNA-derived humanized monoclonal antibody directed against human immunoglobulin E (IgE).8 IgE promotes the release of inflammatory mediators from mast cells and basophils. By binding to IgE, omalizumab prevents IgE from binding to its receptors on immune cells involved in mediating allergic and inflammatory reactions.1
Omalizumab was first approved in the US in 2003 6 and in Europe in 2005.8
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- 149000.0 Da (approximate)
- Sequences
- Not Available
- Synonyms
- Omalizumab
- RHUMAB-E25
- External IDs
- IGE25
- RG-3648
Pharmacology
- Indication
Omalizumab is indicated for: - the treatment of patients six years of age and older with moderate to severe persistent asthma who have a positive skin test or in vitro reactivity to a perennial aeroallergen and whose symptoms are inadequately controlled with inhaled corticosteroids.7,8 - add-on maintenance treatment of chronic rhinosinusitis with nasal polyps (CRSwNP) in adults with inadequate response to nasal corticosteroids.7,8 - the reduction of allergic reactions (Type I), including anaphylaxis, that may occur with accidental exposure to one or more foods in patients aged one year and older with IgE-mediated food allergy. Omalizumab is used to be used in conjunction with food allergen avoidance.7 - the treatment of adults and adolescents 12 years of age and older with chronic spontaneous urticaria (CSU) who remain symptomatic despite H1 antihistamine treatment.7
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Chronic idiopathic urticaria •••••••••••• ••••••••••• ••••• •••••••••• •••••••• •• ••••••••••••• ••••••••• Management of Chronic rhinosinusitis phenotype with nasal polyps (crswnp) •••••••••••• ••••• •••••••••• •••••••• •• ••••• ••••••••••••••• Management of Moderate asthma •••••••••••• ••••••••••• •••••• ••••••••• •••••••• •••••••••••• •••••••••• •••• ••••••• ••••••••••••••• Management of Severe asthma •••••••••••• ••••••••••• •••••• ••••••••• •••••••• •••••••••••• •••••••••• •••• ••••••• ••••••••••••••• Prophylaxis of Type i hypersensitivity •••••••••••• ••• •••••••• •••• •••••••• •••••••••• •••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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Omalizumab decreases free IgE levels in serum in a dose-dependent manner. Serum total IgE levels, accounting for bound and unbound IgE, increased after the first dose of omalizumab due to the formation of drug:IgE complexes, which have a slower elimination rate compared with free IgE. At 16 weeks after the first dose, average total IgE levels in serum were five-fold higher compared to pre-treatment levels in standard assays. Drug effects on IgE levels are reversible upon drug discontinuation, with no observed rebound in IgE levels after drug washout. Total IgE levels did not return to pre-treatment levels for up to one year after discontinuation of omalizumab.7
- Mechanism of action
Omalizumab binds to the Fc domains of IgE in proximity to the binding site of the high-affinity IgE receptor Fc-epsilon-RI, typically found on eosinophils, mast cells, and basophils.1,6
Target Actions Organism AHigh affinity immunoglobulin epsilon receptor subunit alpha inhibitorHumans AHigh affinity immunoglobulin epsilon receptor subunit beta inhibitorHumans - Absorption
After subcutaneous administration, omalizumab has an average absolute bioavailability of 62%. In adult and adolescent patients with asthma, omalizumab was absorbed slowly and the peak serum concentrations occurred after seven to eight days.7
The pharmacokinetics of omalizumab were linear at doses which were higher than 0.5 mg/kg. In patients with asthma, after several doses of omalizumab, areas under the serum concentration-time curve from Day 0 to Day 14 at steady state were up to 6-fold of those after one dose. After repeated dosing from 75mg-300 mg every 4 weeks, trough serum concentrations of omalizumab increased proportionally with the dose.7
- Volume of distribution
In patients with asthma, the apparent volume of distribution was 78 ± 32 mL/kg following subcutaneous administration.7
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Liver elimination of IgG includes degradation in the liver reticuloendothelial system (RES) and endothelial cells. Intact IgG was also shown to be excreted in bile. In studies with mice and monkeys, omalizumab:IgE complexes were eliminated by interactions with Fc-gamma receptors within the RES at rates that were generally faster than IgG clearance.7
- Half-life
In asthma patients, the serum elimination half-life averaged 26 days. In CSU patients, at steady state, based on population pharmacokinetics, omalizumab serum elimination half-life averaged 24 days.7
- Clearance
In pharmacokinetic studies, the clearance of omalizumab involved IgG clearance as well as clearance by specific binding and complex formation with its target ligand, IgE. The apparent clearance averaged 2.4 ± 1.1 mL/kg/day in patients with asthma. The apparent clearance averaged 240 mL/day (corresponding to 3.0 mL/kg/day for an 80 kg patient).8
- Adverse Effects
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The intravenous LD50 in monkeys is 200 mg/kg.9
Maximum tolerated dose of omalizumab has not been determined. Single intravenous doses up to 4000 mg have been administered to patients without evidence of dose-limiting toxicities. The highest cumulative dose administered to patients was 44,000 mg over a 20-week period and this dose did not result in any untoward acute effects. If an overdose is suspected, the patient should be monitored for any abnormal signs or symptoms. Medical treatment should be sought and instituted appropriately.8
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Omalizumab is combined with Abciximab. Adalimumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Adalimumab. Aducanumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Alemtuzumab. Alirocumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Alirocumab. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Xolair Injection, solution 75 mg Subcutaneous Novartis Europharm Limited 2023-11-28 Not applicable EU 
Xolair Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU Xolair Injection, solution 75 mg Subcutaneous Novartis Europharm Limited 2023-11-28 Not applicable EU Xolair Injection, solution 300 mg Subcutaneous Novartis Europharm Limited 2023-11-28 Not applicable EU Xolair Solution 75 mg / 0.5 mL Subcutaneous Novartis 2017-06-28 Not applicable Canada 
Categories
- ATC Codes
- R03DX05 — Omalizumab
- Drug Categories
- Agents to Treat Airway Disease
- Allergens
- Amino Acids, Peptides, and Proteins
- Anti-Allergic Agents
- Anti-Asthmatic Agents
- Anti-IgE
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antigens
- Biological Factors
- Blood Proteins
- Decreased IgE Activity
- Globulins
- IgE-directed Antibody Interactions
- Immunoglobulins
- Immunoproteins
- Proteins
- Respiratory Agents, Miscellaneous
- Respiratory System Agents
- Serum Globulins
- 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
- 2P471X1Z11
- CAS number
- 242138-07-4
References
- General References
- Jensen RK, Plum M, Tjerrild L, Jakob T, Spillner E, Andersen GR: Structure of the omalizumab Fab. Acta Crystallogr F Struct Biol Commun. 2015 Apr;71(Pt 4):419-26. doi: 10.1107/S2053230X15004100. Epub 2015 Mar 20. [Article]
- Miller CW, Krishnaswamy N, Johnston C, Krishnaswamy G: Severe asthma and the omalizumab option. Clin Mol Allergy. 2008 May 20;6:4. doi: 10.1186/1476-7961-6-4. [Article]
- Godse K, Mehta A, Patil S, Gautam M, Nadkarni N: Omalizumab-A Review. Indian J Dermatol. 2015 Jul-Aug;60(4):381-4. doi: 10.4103/0019-5154.160490. [Article]
- Kaplan AP, Joseph K, Maykut RJ, Geba GP, Zeldin RK: Treatment of chronic autoimmune urticaria with omalizumab. J Allergy Clin Immunol. 2008 Sep;122(3):569-73. doi: 10.1016/j.jaci.2008.07.006. [Article]
- Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X. [Article]
- Kumar C, Zito PM: Omalizumab. . [Article]
- FDA Approved Drug Products: XOLAIR (omalizumab) injection, for subcutaneous use (February 2024) [Link]
- EMA Approved Drug Products: Xolair (omalizumab) Subcutaneous Injection [Link]
- Genentech: XOLAIR (omalizumab) MSDS [Link]
- External Links
- UniProt
- P01857
- Genbank
- J00228
- PubChem Substance
- 46507002
- 302379
- ChEMBL
- CHEMBL1201589
- Therapeutic Targets Database
- DAP000387
- PharmGKB
- PA164752253
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Omalizumab
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Not Available Atopic Dermatitis 1 4 Completed Basic Science Asthma 1 4 Completed Diagnostic Asthma, Allergic 1 4 Completed Treatment Allergic Rhinitis (AR) / Asthma / Atopic Dermatitis 1 4 Completed Treatment Aspirin Sensitivity 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Genentech Inc.
- Novartis AG
- Dosage Forms
Form Route Strength Injection Subcutaneous 150 MG Injection, powder, for solution Subcutaneous 150 MG Injection, powder, for solution Subcutaneous 75 MG Injection, solution Parenteral; Subcutaneous 150 MG Injection, solution Parenteral; Subcutaneous 300 mg Injection, solution Parenteral; Subcutaneous 75 MG Injection, solution Subcutaneous 150 mg/1.2mL Injection, solution Subcutaneous 300 mg Injection, solution Subcutaneous 300 mg/2mL Injection, solution Subcutaneous 75 mg Powder 150 mg/1vial Powder, for solution Subcutaneous 150 mg / vial Solution Subcutaneous 150 mg / mL Solution Subcutaneous 75 mg / 0.5 mL Solution Subcutaneous 75.000 mg Solution Subcutaneous 150 mg Solution Subcutaneous 75 mg Injection, solution Subcutaneous 150 mg Injection, solution Subcutaneous 150 mg/ml Injection, powder, lyophilized, for solution Subcutaneous 150 mg Injection, powder, for solution Subcutaneous Injection, powder, lyophilized, for solution Subcutaneous 75 mg Injection, solution Subcutaneous 150 mg/1mL Injection, solution Subcutaneous 75 mg/0.5mL Injection, solution Subcutaneous 150 mg/1.0mL - Prices
Unit description Cost Unit Xolair 150 mg vial 715.42USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2113813 No 2005-04-12 2012-08-14 Canada CA1340233 No 1998-12-15 2015-12-15 Canada
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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
- 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. [Article]
- 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. [Article]
- Godse K, Mehta A, Patil S, Gautam M, Nadkarni N: Omalizumab-A Review. Indian J Dermatol. 2015 Jul-Aug;60(4):381-4. doi: 10.4103/0019-5154.160490. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- DuBuske LM: IgE, allergic diseases, and omalizumab. Curr Pharm Des. 2006;12(30):3929-44. [Article]
- Raunio H, Rautio A, Gullsten H, Pelkonen O: Polymorphisms of CYP2A6 and its practical consequences. Br J Clin Pharmacol. 2001 Oct;52(4):357-63. [Article]
Drug created at June 13, 2005 13:24 / Updated at April 16, 2024 15:53