242138-07-4

Basic information

• Product Name: OMALIZUMAB
• Synonyms: OMALIZUMAB;Xolair
• CAS NO: 242138-07-4
• Molecular Weight: 0
• Mol File: 242138-07-4.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: OMALIZUMAB(CAS DataBase Reference)
• NIST Chemistry Reference: OMALIZUMAB(242138-07-4)
• EPA Substance Registry System: OMALIZUMAB(242138-07-4)

Safety Data

• Hazardous Substances Data: 242138-07-4(Hazardous Substances Data)

Usage

Description

Omalizumab, also known as Xolair, is a recombinant humanized monoclonal antibody engineered to treat allergic asthma. It is a construct of murine IgG1k monoclonal antibody that specifically binds to free, circulating serum IgE, thereby inhibiting the binding of IgE to the high-affinity IgE-receptor (FcεRI) on the surface of mast cells and basophils. This interaction leads to a reduction in the release of mediators responsible for the allergic response. Omalizumab is produced through a Chinese hamster ovary cell suspension culture in a nutrient medium containing gentamicin and is administered subcutaneously every 2 or 4 weeks.

Uses

Used in Pharmaceutical Industry:
Omalizumab is used as a therapeutic agent for the treatment of atopic diseases, particularly allergic asthma and rhinitis. It functions by forming complexes with free IgE, reducing the degree of release of mediators of the allergic response and providing relief from symptoms.
Used in Asthma Treatment:
Omalizumab is used as an add-on therapy for patients with inhaled corticosteroid-dependent (ICS) asthma. It has been shown to significantly reduce steroid dosage and the frequency of exacerbations during steroid withdrawal phase, allowing more patients to discontinue their ICS use compared to the placebo group.
Used in Allergy Management:
Omalizumab is used as a treatment option for patients with moderate to severe allergic rhinitis, helping to alleviate symptoms and improve the quality of life for those affected by this condition.
Brand Name:
Xolair (Genentech)

Originator

Genentech (US)

Mechanism of action

Additional amino acid sequences have been incorporated into the antibody so that a humanized product resulted that only differs by 5% nonhuman amino acid residues. In vitro, omalizumab has been shown to complex with free IgE, forming trimers consisting of a 2:1 complex of IgE to omalizumab or a 1:2 complex of IgE to omalizumab. In addition, larger complexes also are formed, consisting of a 3:3 ratio of each. Omalizumab does not bind to IgE already bound to mast cells and, therefore, does not cause the degranulation that might be expected from such interaction. Thus, omalizumab effectively neutralizes free IgE and, aside from the obvious decrease of available IgE, also causes the down-regulation of FcεRI receptors on the mast cell surface, resulting in a decrease of IgE bound to the mast cell.

Pharmacokinetics

The bioavailability after subcutaneous administration is 62%, with slow absorption resulting in peak serum levels in 7 to 8 days from a single dose. Steady-state plasma concentration is reached in 14 to 29 days with multiple dosing regimens. The elimination of omalizumab is not clearly understood; however, studies have determined that intact IgE is excreted via the bile and that omalizumab:IgE complexes are cleared faster than uncomplexed omalizumab and slower than free IgE. This means that over time, total IgE concentrations (free and complexed IgE) increase, because the complex is cleared more slowly. The metabolism of omalizumab is not known, and the clearance of the complex is similar to the liver elimination of another immunoglobulin, IgG. The reticuloendothelial system degrades IgG, and it is believed that the same process occurs for the omalizumab:IgE complex.

Clinical Use

The clinical role for omalizumab is in the treatment of allergic asthma. It is approved for the treatment of adults and adolescents 12 years of age and older whose symptoms are not controlled with inhaled glucocorticoids and who have a positive skin test for airborne allergens.