Omalizumab

• CAS Number: 242138-07-4

Omalizumab (trade name Xolair ®, manufactured by Novartis) is a recombinant humanized monoclonal antibody against immunoglobulin E ( anti-IgE ) for the treatment of severe allergic asthma. He binds and neutralizes the anti-antibody which are responsible for triggering the allergic reaction antibody IgE-type. The preparation is carried out in a cell line of the Chinese hamster ovary ( CHO) cells.

Indication

In the U.S. it is be prescribed for the treatment of moderate to severe persistent allergic asthma since July 2003, in Germany the drug was only approved for the treatment of severe allergic asthma in October 2005. The application should only take place when patients despite treatment with a long-acting β2 -sympathomimetic combined with high-dose inhaled glucocorticoids have more severe asthma attacks a year. Currently, in the United States about 50 000 treated in France in 3500 and Germany in 1500 patients with this medication. Since September 2009 Omalizumab is approved in the EU for the treatment of children aged 6 years.

Although there is not yet approved for the treatment, has been shown in several studies that omalizumab also highly effective in the urticaria shows which could often be treated by the current treatment options are unsatisfactory.

Dosage

Every 2-4 weeks 75-375 mg subcutaneously as a function of body weight and total IgE, which is to be determined beforehand.

If a favorable response does not reach even after 16 weeks of use, therapy should be discontinued with omalizumab.

Mechanism of Action

Omalizumab binds to as " anti-antibody " to free IgE, forming complexes that are ineffective in the cascade of allergy trigger. The binding of the IgE to mast cells is reduced and the release -promoting allergy mediators ( histamine and leukotrienes ) decreases. Of the application, the concentration of free IgE is reduced by over 90%.

Side effects

Local reactions

Side effects are minimal pain increased compared to placebo, but significantly increased severe reactions at the injection site such as swelling, skin rashes, itching but also described a headache.

Allergies, anaphylaxis

Of particular note are life-threatening anaphylactic reactions observed in part more than 24 hours after injection, both after the first, and after subsequent applications ( even after more than one year). The overall incidence is estimated on the basis of ADR reports in the U.S. to 0.2%. These symptoms can use within minutes, hours or days after the injection of omalizumab: 35% of reactions occurred up to 30 minutes after injection, into 14 % are between 6 and 12 hours, after all, still in 5% of cases in the range of 1-4 days. 39% in the reaction appeared during the first dose, 19 % in the second and 10% at the third dose, and the remaining 32% at later time points. A replay of the application of the active ingredient after anaphylaxis is particularly dangerous. In 18 of 23 people reexponierten again occur partly severe anaphylactic symptoms.

Possible symptoms of such anaphylaxis are bronchospasm, hypotension, syncope ( sudden onset, short lasting loss of consciousness), urticaria, angioedema, respiratory distress, generalized itching and Others After a recommendation by the Food and Drug Administration ( Food and Drug Administration of the USA) to the patient until at least be monitored two hours after the injection by a doctor. The causes of anaphylactic and anaphylactoid (late) reactions are still unclear, concrete long-term studies are still missing.

Malignant tumors

Another serious adverse effect of omalizumab is the increased observation of the development of malignant tumors of various types during therapy. In a summary report to the FDA in November 2009, a warning relating to increased tumor formation in comparison is shown to placebo: 0.5 % versus 0.2 %, corresponding to 6.3 tumors versus 3.3 per 1000 patient-years.

Other side effects

An additional side effects were partially pronounced changes in blood count to ( thrombocytopenia ) and hair loss. The infection rate of worms ( helminths ) increased because IgE is involved in the defense of worm infections.

Other Information

One vial of 150 mg in Germany costs about 530 €.