Xolair150 mg/vial

Xolair is a recombinant humanized monoclonal antibody that targets immunoglobulin E (IgE) and is used across several IgE-mediated allergic conditions. Its approved and evidence-supported uses include:

Established / Approved Indications

• Moderate-to-severe persistent allergic asthma (age 6 years and above) with a positive skin test or in vitro reactivity to a perennial aeroallergen, in patients whose symptoms are inadequately controlled with inhaled corticosteroids.
• Chronic idiopathic (spontaneous) urticaria (CIU/CSU) (age 12 years and above) in patients who remain symptomatic despite H1-antihistamine treatment.
• Chronic rhinosinusitis with nasal polyps (CRSwNP) (age 18 years and above), as add-on maintenance treatment.
• IgE-mediated food allergy (age 1 year and above), to reduce the risk and severity of allergic reactions, including anaphylaxis, that may occur with accidental exposure to one or more foods. Xolair does not treat an acute allergic reaction and must be used together with continued food allergen avoidance.

Not an Indicated Use

Xolair is not indicated for the relief of acute bronchospasm or status asthmaticus, and is not a rescue medication.

Each formulation of Omalizumab contains omalizumab, a recombinant DNA-derived humanized IgG1 kappa monoclonal antibody produced in a Chinese hamster ovary cell suspension culture, as the sole active ingredient.

• Prefilled syringe / autoinjector: Omalizumab 75 mg/0.5 mL or 150 mg/mL solution for subcutaneous injection.
• Lyophilized powder for injection: Omalizumab 150 mg per single-use vial, reconstituted before use.

Common excipients include L-histidine, L-histidine hydrochloride, polysorbate 20, and sucrose.

Xolair is a biologic (large-molecule) medicine belonging to the anti-IgE monoclonal antibody class. It is given by subcutaneous injection and works by binding free immunoglobulin E (IgE) in the blood, interrupting the allergic cascade that drives conditions such as allergic asthma, chronic spontaneous urticaria, chronic rhinosinusitis with nasal polyps, and IgE-mediated food allergy.

Xolair is administered under medical supervision, typically every 2 or 4 weeks, and is intended for long-term, add-on management of allergic disease rather than for immediate symptom relief.

Anti-IgE monoclonal antibody (biologic immunomodulator); Xolair is classified as a selective IgE-blocking agent used in allergic/immunologic disease.

Omalizumab is a recombinant humanized monoclonal antibody (IgG1 kappa) that selectively binds to free circulating immunoglobulin E (IgE), including at the same site on IgE that would otherwise bind to the high-affinity IgE receptor (FcεRI) on mast cells and basophils.

• By binding free IgE, Omalizumab lowers free serum IgE levels and prevents IgE from attaching to effector cells.
• Omalizumab does not bind IgE already fixed to mast cells or basophils, so it does not trigger degranulation or an allergic reaction itself.
• Over time, reduced free IgE leads to down-regulation of FcεRI receptor expression on basophils and mast cells, further blunting the IgE-mediated allergic inflammatory response.
• This mechanism reduces the frequency and severity of allergic symptoms in IgE-driven conditions such as allergic asthma, chronic spontaneous urticaria, chronic rhinosinusitis with nasal polyps, and IgE-mediated food allergy.

Omalizumab is administered subcutaneously; peak serum concentrations are typically reached over several days, and clinical effects on free IgE and symptoms accumulate over weeks of repeated dosing.

Xolair is given only by subcutaneous injection, typically into the upper arm or thigh, and must never be given intravenously or intramuscularly.

• Injection sites should be rotated with each dose.
• Xolair should not be injected into skin that is red, bruised, tender, hard, or affected by psoriasis or other active skin disease.
• Doses greater than 150 mg are typically split between two or more injection sites.
• Xolair must be administered in a setting equipped to manage anaphylaxis, with the patient observed for an appropriate period after each injection (see Precautions and Warnings).

Formal drug-drug interaction studies with Xolair have not been conducted, and no clinically significant pharmacokinetic drug interactions have been established. The following points are clinically relevant when Xolair is used alongside other therapies:

• Allergen immunotherapy: Xolair has been used concomitantly with allergen immunotherapy in some patients, but data defining the safety of starting immunotherapy during Xolair treatment are limited; initiate immunotherapy with caution and physician oversight.
• Inhaled/systemic corticosteroids: Xolair is not a substitute for corticosteroids; any reduction in corticosteroid dose during Xolair therapy should be gradual and physician-supervised (see Precautions and Warnings).
• Other immunosuppressants/biologics: Concurrent use with other immunomodulatory or immunosuppressive biologic therapy has not been systematically studied; combined use should be individualized by the treating physician.

Most patients tolerate Xolair reasonably well; adverse effects range from common and mild to rare but serious reactions.

Common Side Effects

• Injection-site reactions (pain, swelling, redness, itching, bruising)
• Headache
• Upper respiratory tract infection
• Sinusitis
• Joint pain (arthralgia)
• Fatigue
• Dizziness

Serious but Less Common Side Effects

• Anaphylaxis (see boxed warning under Precautions and Warnings)
• Serum-sickness-like reactions (fever, joint pain/swelling, rash, lymphadenopathy), typically 1–5 days after an injection
• Malignancy (numerically higher rate observed in some early trials; a causal relationship has not been established — see Precautions and Warnings)
• Cardiovascular and cerebrovascular events have been reported in some observational data, though a causal link to Xolair has not been established

Patients should seek immediate medical attention for any signs of a severe allergic reaction after receiving Xolair.

Pregnancy: Data on the use of Xolair in human pregnancy are limited. Pregnancy registry data have suggested a numerically higher rate of low birth weight among infants born to mothers treated with Xolair, but confounding by underlying asthma severity has not been excluded, and a causal relationship has not been established. Xolair is a large IgG-class molecule known to cross the placenta, particularly in the second and third trimesters. Xolair should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus, and only under the guidance of a physician.

Lactation: Limited data indicate that Xolair is present in human milk in small amounts; available data have not shown an increased rate of infections in breastfed infants of mothers using Xolair. The decision to continue Xolair during breastfeeding should be made by a physician, weighing the mother's clinical need against any potential risk to the infant.

Boxed Warning: Anaphylaxis

Anaphylaxis — presenting as bronchospasm, hypotension, syncope, urticaria, and/or angioedema of the throat or tongue — has occurred after administration of Xolair, including after the very first dose and, in some cases, more than a year after starting treatment. Xolair should be administered only in a healthcare setting by personnel prepared to manage anaphylaxis, with epinephrine and other emergency measures readily available, and patients should be observed for an appropriate period after each injection.

Other Warnings and Precautions

• Malignancy: A numerically higher rate of malignancy was observed in some early clinical trials of Xolair compared with control; a causal relationship has not been established. Long-term monitoring is advised.
• Not for acute symptoms: Xolair is not indicated for treatment of acute bronchospasm, status asthmaticus, or acute allergic emergencies, and must not be used as a rescue therapy.
• Parasitic (helminth) infection: IgE may play a role in the immune response to certain parasitic infections. Patients at high risk of geohelminth infection (e.g., those living in or travelling to endemic areas) should be monitored during Xolair treatment; if a patient fails to respond to anti-parasitic treatment, discontinuation of Xolair should be considered.
• Corticosteroid reduction: Corticosteroid doses should not be abruptly stopped upon starting Xolair; any reduction should be gradual and supervised by a physician.
• Fever, arthralgia, and rash occurring days after an injection may indicate a serum-sickness-like reaction and should be reported to a physician promptly.

Clinical experience with overdose of Xolair is limited, and no specific toxicity syndrome has been established for doses above the recommended range. If an overdose of Xolair is suspected, or if a severe or allergic reaction occurs, seek immediate medical attention or contact emergency services / a poison control center rather than attempting home treatment. The patient should be monitored clinically, and supportive care given as needed.

Store Xolair refrigerated at 2°C to 8°C (36°F to 46°F) in its original carton, protected from light. Do not freeze. Do not shake the syringe, autoinjector, or vial. If refrigeration is not available, consult the product packaging or a pharmacist for permitted room-temperature storage limits before use. Keep out of reach of children.

• Renal impairment: No formal dose adjustment of Xolair has been established; limited data are available in patients with significant renal impairment, so use with caution and physician monitoring.
• Hepatic impairment: No formal dose adjustment of Xolair has been established; limited data are available in patients with significant hepatic impairment, so use with caution and physician monitoring.
• Elderly patients: Clinical trial data on Xolair in patients over 65 years are limited; no specific dose adjustment is established, but response and tolerability should be monitored.
• Pediatric patients: Approved age thresholds vary by indication (see Pediatric Uses); Xolair is not established as safe and effective below the approved age for each specific indication.
• Pregnancy and lactation: See Pregnancy and Lactation section.

Treatment duration with Xolair is individualized by the treating physician based on indication and clinical response. For allergic asthma, response is typically assessed after approximately 12–16 weeks of therapy; if there is no clear improvement in asthma control, continuation of Xolair should be reconsidered. For chronic idiopathic urticaria, chronic rhinosinusitis with nasal polyps, and IgE-mediated food allergy, Xolair is generally used as a long-term, ongoing add-on therapy for as long as clinical benefit is demonstrated and the physician determines continued treatment is appropriate. Periodic physician review is required, and Xolair should not be stopped or restarted without medical advice.

The lyophilized (freeze-dried) powder vial form of Xolair (150 mg/vial) must be reconstituted before use:

• Reconstitute with 1.4 mL of Sterile Water for Injection.
• Allow the vial to sit and gently swirl (do not shake) until the powder is fully dissolved; this can take up to 15–20 minutes and may result in a viscous, slightly opalescent solution.
• Once reconstituted, use within 8 hours if kept refrigerated (2–8°C) or within 4 hours if kept at room temperature.

Prefilled syringe and autoinjector presentations of Xolair are supplied ready-to-use and do not require reconstitution.

Monoclonal antibodies; Anti-IgE agents; Biologic immunomodulators used in allergic disease. Omalizumab is the prototype anti-IgE monoclonal antibody in clinical use.

Omalizumab works by selectively binding to free immunoglobulin E (IgE) in the bloodstream, at the same region of the IgE molecule that would otherwise attach to the high-affinity IgE receptor (FcεRI) on mast cells and basophils. By capturing free IgE before it can bind to these effector cells, Omalizumab lowers free serum IgE levels and, over repeated dosing, leads to down-regulation of FcεRI receptors on mast cells and basophils — reducing the release of histamine and other inflammatory mediators that drive allergic asthma, chronic urticaria, nasal polyps, and IgE-mediated food allergy reactions. Omalizumab does not bind IgE already attached to cells, so it does not itself cause mast cell or basophil activation.

Approved pediatric use of Xolair depends on the indication:

• Allergic asthma: Approved from age 6 years and above; safety and efficacy in children younger than 6 years have not been established.
• IgE-mediated food allergy: Approved from age 1 year and above; safety and efficacy below age 1 have not been established.
• Chronic idiopathic (spontaneous) urticaria: Approved from age 12 years and above; safety and efficacy in children younger than 12 have not been established.
• Chronic rhinosinusitis with nasal polyps: Approved only in adults (age 18 years and above); safety and efficacy in children have not been established.

Xolair should only be used in pediatric patients within these approved age ranges and under close physician supervision.