Omalizumab
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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).7 IgE promotes the release of inflammatory mediators from mast cells and basophils during allergic and inflammatory reactions. By binding to IgE and neutralizing it, omalizumab reduces free IgE levels and prevents IgE from binding to its receptors on immune cells.1
Omalizumab was first approved in the US in 2003 3 and in Europe in 2005.7 It is used to treat a range of immune and inflammatory conditions, including allergies, urticaria, and asthma.3
- 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.6,7 - add-on maintenance treatment of chronic rhinosinusitis with nasal polyps (CRSwNP) in adults with inadequate response to nasal corticosteroids.6,7 - 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 to be used in conjunction with food allergen avoidance.6 - the treatment of adults and adolescents 12 years of age and older with chronic spontaneous urticaria (CSU) who remain symptomatic despite H1 antihistamine treatment.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
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
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
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.6
- Mechanism of action
IgE antibodies have been implicated in several immune-mediated diseases, including allergic hypersensitivity reactions and asthma. IgE binds to the high-affinity IgE receptor Fc-epsilon-RI typically found on inflammatory cells such as eosinophils, mast cells, and basophils.1,3 IgE binding to Fc-epsilon-RI initiates a downstream cascade that releases pro-inflammatory mediators.1
Omalizumab is an IgE-neutralizing antibody: It selectively binds to the C-epsilon-3 locus of IgE, the domain at which IgE binds to Fc-epsilon-RI to mediate its actions. Omalizumab works to lower circulating free IgE levels and prevent IgE from interacting with Fc-epsilon-RI,3 which can also lead to the reduced expression of Fc-epsilon-RI.4
Target Actions Organism AImmunoglobulin heavy constant epsilon antibodyneutralizerHumans - 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.6
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.6
- Volume of distribution
In patients with asthma, the apparent volume of distribution was 78 ± 32 mL/kg following subcutaneous administration.6
- Protein binding
Not Available
- Metabolism
Omalizumab is degraded in the reticuloendothelial system and endothelial cells.3
- 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.6
- 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.6
- 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).7
- Adverse Effects
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- Toxicity
The intravenous LD50 in monkeys is 200 mg/kg.8
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.7
- 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 Omlyclo Injection, solution 150 mg Subcutaneous Celltrion Healthcare Hungary Kft. 2024-07-10 Not applicable EU Omlyclo Injection, solution 75 mg Subcutaneous Celltrion Healthcare Hungary Kft. 2024-07-10 Not applicable EU Omlyclo Injection, solution 150 mg Subcutaneous Celltrion Healthcare Hungary Kft. 2024-07-10 Not applicable EU Omlyclo Injection, solution 150 mg Subcutaneous Celltrion Healthcare Hungary Kft. 2024-07-10 Not applicable EU Xolair Injection, solution 300 mg Subcutaneous Novartis Europharm Limited 2023-11-28 Not applicable EU
Categories
- ATC Codes
- R03DX05 — Omalizumab
- Drug Categories
- Agents to Treat Airway Disease
- 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]
- 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]
- Kumar C, Zito PM: Omalizumab. . [Article]
- Okayama Y, Matsumoto H, Odajima H, Takahagi S, Hide M, Okubo K: Roles of omalizumab in various allergic diseases. Allergol Int. 2020 Apr;69(2):167-177. doi: 10.1016/j.alit.2020.01.004. Epub 2020 Feb 14. [Article]
- Pelaia C, Calabrese C, Terracciano R, de Blasio F, Vatrella A, Pelaia G: Omalizumab, the first available antibody for biological treatment of severe asthma: more than a decade of real-life effectiveness. Ther Adv Respir Dis. 2018 Jan-Dec;12:1753466618810192. doi: 10.1177/1753466618810192. [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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Allergic Rhinitis (AR) 1 somestatus stop reason just information to hide Not Available Completed Not Available Asthma 4 somestatus stop reason just information to hide Not Available Completed Not Available Asthma in Children / Food; Allergy, Anaphylactic Shock 1 somestatus stop reason just information to hide Not Available Completed Not Available Asthma, Allergic 2 somestatus stop reason just information to hide Not Available Completed Basic Science Allergic Reaction 1 somestatus stop reason just information to hide
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/2mL Injection, solution Subcutaneous 300 mg Injection, solution Subcutaneous 75 mg Powder 150 mg/1vial Powder, for solution Subcutaneous 150 mg / vial Solution Subcutaneous 150 mg / mL Solution Subcutaneous 150 mg / 1 mL Solution Subcutaneous 300 mg / 2 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 Solution Subcutaneous 150 mg/ml Injection, powder, lyophilized, for solution Subcutaneous 75 mg Solution Subcutaneous 75 mg/0.5ml 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
- AntibodyNeutralizer
- General Function
- Constant region of immunoglobulin heavy chains. Immunoglobulins, also known as antibodies, are membrane-bound or secreted glycoproteins produced by B lymphocytes. In the recognition phase of humoral immunity, the membrane-bound immunoglobulins serve as receptors which, upon binding of a specific antigen, trigger the clonal expansion and differentiation of B lymphocytes into immunoglobulins-secreting plasma cells. Secreted immunoglobulins mediate the effector phase of humoral immunity, which results in the elimination of bound antigens (PubMed:20176268, PubMed:22158414). The antigen binding site is formed by the variable domain of one heavy chain, together with that of its associated light chain. Thus, each immunoglobulin has two antigen binding sites with remarkable affinity for a particular antigen. The variable domains are assembled by a process called V-(D)-J rearrangement and can then be subjected to somatic hypermutations which, after exposure to antigen and selection, allow affinity maturation for a particular antigen (PubMed:17576170, PubMed:20176268)
- Specific Function
- antigen binding
- Gene Name
- IGHE
- Uniprot ID
- P01854
- Uniprot Name
- Immunoglobulin heavy constant epsilon
- Molecular Weight
- 59538.685 Da
References
- Pelaia C, Calabrese C, Terracciano R, de Blasio F, Vatrella A, Pelaia G: Omalizumab, the first available antibody for biological treatment of severe asthma: more than a decade of real-life effectiveness. Ther Adv Respir Dis. 2018 Jan-Dec;12:1753466618810192. doi: 10.1177/1753466618810192. [Article]
- 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]
- FDA Approved Drug Products: XOLAIR (omalizumab) injection, for subcutaneous use (February 2024) [Link]
Drug created at June 13, 2005 13:24 / Updated at August 02, 2024 07:21