Introduction：Basic information about Omalizumab CAS 242138-07-4, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Omalizumab Basic information
| Product Name: | Omalizumab |
| Synonyms: | OMALIZUMAB;Xolair;Immunoglobulin G1,anti-(human immunoglobulin E Fc region) (human-mouse monoclonal E25 clonepSVIE25 g-chain), disulfide withhuman-mouse monoclonal E25 clone pSVIE25 k-chain, dimer (9CI);Research Grade Omalizumab(DHJ92701);humanized,asthma,IgE,CD40,allergic,IL-4,IL-6,FcγRIIb,Olizumab,Inhibitor,immunoglobulin,FcεRI,rhuMab-E25,Omalizumab,inhibit;Omalizumab (anti-IgE);Research Grade Omalizumab;Omalizumab - buffer solution |
| CAS: | 242138-07-4 |
| MF: | |
| MW: | 0 |
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| Mol File: | Mol File |
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Omalizumab Chemical Properties
| form | Solid |
| color | White to light yellow |
Safety Information
| Hazardous Substances Data | 242138-07-4(Hazardous Substances Data) |
Omalizumab Usage And Synthesis
| Description | Omalizumab is a recombinant humanized construct of murine IgG1k monoclonalantibody introduced for the treatment of allergic asthma. It formscomplexes with free, circulating serum IgE, which results in the inhibition of bindingof IgE to the high-affinity IgE-receptor (FCeRI) on the surface of mast cells andbasophils. Reduction in surface-bound IgE on FceRI-bearing cells limits the degreeof release of mediators of the allergic response. Omalizumab is produced by aChinese hamster ovary cell suspension culture in a nutrient medium containing theantibiotic gentamicin. The recommended dosage is 150–375 mg administeredsubcutaneously every 2 or 4 weeks. Omalizumab has an average absolutebioavailability of 62% and an average terminal half-life of 26 days. Following asingle SC dose, omalizumab is absorbed slowly, reaching peak serum concentrationsafter 7–8 days. However, serum levels of free IgE begin to decline in a dosedependentmanner within an hour after the first injection and typically lead to ＞96%reduction in free IgE concentrations. The omalizumab-IgE complexes have a longer half-life and are eliminated more slowly than free IgE. After 16 weeks of dosing,total serum IgE (free plus bound IgE) is five times higher than pretreatment levels.Clearance of the omalizumab-IgE complexes occurs via the Fcg receptorsreticuloendothelial system. The efficacy and safety of omalizumab in the treatmentof inhaled corticosteroid-dependent (ICS) asthma was evaluated in a 28-week doubleblinded,placebo-controlled clinical study, which entailed co-administration of ICSfor 16 weeks, followed by a gradual reduction in ICS dose over 12 weeks. Asignificant reduction in steroid dose with fewer exacerbations during steroidwithdrawal phase was noted and more subjects receiving omalizumab were able todiscontinue their ICS than in the placebo group (39.6 vs 19.1%, respectively;p ＜0.001). Omalizumab was well tolerated and the most common adverse effectswere arthralgia, generalized pain, leg pain, and injection-site reactions. |
| Originator | Genentech (US) |
| Uses | Treatment of atopic disease (asthma; rhinitis) (monoclonal antibody). |
| Brand name | Xolair (Genentech). |
| Mechanism of action | Additional amino acidsequences have been incorporated into the antibody so that a humanized product resulted thatonly differs by 5% nonhuman amino acid residues.In vitro, omalizumab has been shown to complex with free IgE, forming trimers consisting of a 2:1complex of IgE to omalizumab or a 1:2 complex of IgE to omalizumab. In addition, largercomplexes also are formed, consisting of a 3:3 ratio of each. Omalizumab does notbind to IgE already bound to mast cells and, therefore, does not cause the degranulation thatmight 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 FcεRIreceptors 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 isreached in 14 to 29 days with multiple dosing regimens. The elimination of omalizumab is notclearly understood; however, studies have determined that intact IgE is excreted via the bile andthat omalizumab:IgE complexes are cleared faster than uncomplexed omalizumab and slower thanfree 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, andthe 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 forthe omalizumab:IgE complex. |
| Clinical Use | The clinical role for omalizumab is in the treatment of allergic asthma. It is approved for thetreatment of adults and adolescents 12 years of age and older whose symptoms are notcontrolled with inhaled glucocorticoids and who have a positive skin test for airborne allergens. |
Omalizumab Preparation Products And Raw materials
