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Omalizumab

Pronunciation

(oh mah lye ZOO mab)

Index Terms

  • rhuMAb-E25

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Subcutaneous [preservative free]:

Xolair: 150 mg (1 ea)

Brand Names: U.S.

  • Xolair

Pharmacologic Category

  • Monoclonal Antibody, Anti-Asthmatic

Pharmacology

Asthma: Omalizumab is an IgG monoclonal antibody (recombinant DNA derived) which inhibits IgE binding to the high-affinity IgE receptor on mast cells and basophils. By decreasing bound IgE, the activation and release of mediators in the allergic response (early and late phase) is limited. Serum free IgE levels and the number of high-affinity IgE receptors are decreased. Long-term treatment in patients with allergic asthma showed a decrease in asthma exacerbations and corticosteroid usage.

Chronic idiopathic urticaria: Omalizumab binds to IgE and lowers free IgE levels. Subsequently, IgE receptors (FcεRI) on cells down-regulate. The mechanism by which these effects of omalizumab result in an improvement of chronic idiopathic urticaria symptoms is unknown.

Absorption

Slow following SubQ injection

Distribution

Vd: 78 ± 32 mL/kg

Metabolism

Degradation of IgG and omalizumab:IgE complexes by reticuloendothelial system and endothelial cells in the liver

Excretion

Primarily via hepatic degradation; intact IgG may be secreted in bile

Time to Peak

7-8 days

Half-Life Elimination

26 days (asthma patients); 24 days (chronic idiopathic urticaria patients)

Use: Labeled Indications

Asthma: Treatment of moderate to severe persistent asthma in adults and adolescents 12 years and older who have a positive skin test or in vitro reactivity to a perennial aeroallergen and whose symptoms are inadequately controlled with inhaled corticosteroids.

Guideline recommendations:

The 2007 National Asthma Education and Prevention Program asthma guidelines recommend use be considered as adjunctive therapy in patients with severe persistent asthma who have allergies and in patients with severe persistent asthma that is inadequately controlled with a combination of a high-dose inhaled corticosteroid and a long-acting beta2-agonist (NAEPP 2007).

The Global Initiative for Asthma suggests use be considered as adjunctive therapy in patients with moderate or severe allergic asthma that is uncontrolled with a combination of a medium- to high-dose inhaled corticosteroid and a long-acting beta2-agonist (GINA 2015).

Chronic idiopathic urticaria: Treatment of chronic idiopathic urticaria in adults and adolescents 12 years and older who remain symptomatic despite H1 antihistamine treatment.

Contraindications

Severe hypersensitivity reaction to omalizumab or any component of the formulation

Dosage

Asthma: Adolescents ≥12 years and Adults: SubQ: Dose and frequency based on body weight and pretreatment total IgE serum levels. Dosing should be adjusted during therapy for significant changes in body weight. Dosing should not be adjusted based on total IgE levels taken during treatment or <1 year following interruption of therapy. If therapy has been interrupted for ≥1 year, total IgE levels may be re-evaluated for dosage determination.

Pretreatment serum IgE ≥30 to 100 units/mL:

US labeling:

30 to 90 kg: 150 mg every 4 weeks

>90 to 150 kg: 300 mg every 4 weeks

Canadian labeling:

>20 to 90 kg: 150 mg every 4 weeks

>90 to 150 kg: 300 mg every 4 weeks

Pretreatment serum IgE >100 to 200 units/mL:

US labeling:

30 to 90 kg: 300 mg every 4 weeks

>90 to 150 kg: 225 mg every 2 weeks

Canadian labeling:

>20 to 40 kg: 150 mg every 4 weeks

>40 to 90 kg: 300 mg every 4 weeks

>90 to 125 kg: 225 mg every 2 weeks

>125 to 150 kg: 300 mg every 2 weeks

Pretreatment serum IgE >200 to 300 units/mL:

US labeling:

30 to 60 kg: 300 mg every 4 weeks

>60 to 90 kg: 225 mg every 2 weeks

>90 to 150 kg: 300 mg every 2 weeks

Canadian labeling:

>20 to 30 kg: 150 mg every 4 weeks

>30 to 60 kg: 300 mg every 4 weeks

>60 to 90 kg: 225 mg every 2 weeks

>90 to 125 kg: 300 mg every 2 weeks

>125 to 150 kg: 375 mg every 2 weeks

Pretreatment serum IgE >300 to 400 units/mL:

US labeling:

30 to 70 kg: 225 mg every 2 weeks

>70 to 90 kg: 300 mg every 2 weeks

>90 kg: Do not administer dose

Canadian labeling:

>20 to 40 kg: 300 mg every 4 weeks

>40 to 70 kg: 225 mg every 2 weeks

>70 to 90 kg: 300 mg every 2 weeks

>90 kg: Do not administer dose

Pretreatment serum IgE >400 to 500 units/mL:

US labeling:

30 to 70 kg: 300 mg every 2 weeks

>70 to 90 kg: 375 mg every 2 weeks

>90 kg: Do not administer dose

Canadian labeling:

>20 to 30 kg: 300 mg every 4 weeks

>30 to 50 kg: 225 mg every 2 weeks

>50 to 70 kg: 300 mg every 2 weeks

>70 to 90 kg: 375 mg every 2 weeks

>90 kg: Do not administer dose

Pretreatment serum IgE >500 to 600 units/mL:

US labeling:

30 to 60 kg: 300 mg every 2 weeks

>60 to 70 kg: 375 mg every 2 weeks

>70 kg: Do not administer dose

Canadian labeling:

>20 to 30 kg: 300 mg every 4 weeks

>30 to 40 kg: 225 mg every 2 weeks

>40 to 60 kg: 300 mg every 2 weeks

>60 to 70 kg: 375 mg every 2 weeks

>70 kg: Do not administer dose

Pretreatment serum IgE >600 to 700 units/mL:

US labeling:

30 to 60 kg: 375 mg every 2 weeks

>60 kg: Do not administer dose

Canadian labeling:

>20 to 40 kg: 225 mg every 2 weeks

>40 to 50 kg: 300 mg every 2 weeks

>50 to 60 kg: 375 mg every 2 weeks

>60 kg: Do not administer dose

Chronic idiopathic urticaria: Adolescents ≥12 years and Adults: SubQ: 150 or 300 mg every 4 weeks. Dosing is not dependent on serum IgE (free or total) level or body weight.

Dosage adjustment for toxicity:

Severe hypersensitivity reaction or anaphylaxis: Discontinue treatment.

Fever, arthralgia, and rash: Discontinue treatment if this constellation of symptoms occurs.

Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Reconstitution

Reconstitute using SWFI only; add SWFI 1.4 mL to upright vial using a 1-inch, 18-gauge needle on a 3 mL syringe and swirl gently for ~1 minute to evenly wet the powder; do not shake. Then gently swirl the upright vial for 5 to 10 seconds approximately every 5 minutes until dissolved; generally takes 15 to 20 minutes to dissolve completely. If it takes >20 minutes to dissolve completely, continue to swirl the upright vial for 5 to 10 seconds every 5 minutes until no gel-like particles are visible in the solution; do not use if contents are not completely dissolved after 40 minutes. After reconstitution, solution is somewhat viscous and will appear clear or slightly opalescent. It is acceptable if there are a few small bubbles or foam around edge of vial. Resulting solution is 150 mg per 1.2 mL. Invert the vial for 15 seconds so the solution drains toward the stopper. Remove all of the solution by inserting a new 3 mL syringe with a 1-inch, 18-gauge needle into the inverted vial. Replace the 18-gauge needle with a 25-gauge needle for subcutaneous injection, and expel any air, bubbles, or excess solution to obtain the 1.2 mL dose.

Administration

For SubQ injection only; doses >150 mg should be divided over more than one injection site (eg, 225 mg or 300 mg administered as two injections, 375 mg administered as three injections). Injections may take 5 to 10 seconds to administer (solution is slightly viscous). Administer only under direct medical supervision and observe patient for a minimum of 2 hours following administration of any dose given.

Storage

Prior to reconstitution, store under refrigeration at 2°C to 8°C (36°F to 46°F); product may be shipped at room temperature. Following reconstitution, protect from direct sunlight. May be stored for up to 8 hours if refrigerated or 4 hours if stored at room temperature ≤30°C (≤86°F).

Drug Interactions

Belimumab: Monoclonal Antibodies may enhance the adverse/toxic effect of Belimumab. Avoid combination

Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Avoid combination

Test Interactions

Total IgE levels are elevated for up to 1 year following treatment. Total serum IgE may be retested after interruption of therapy for 1 year or more.

Adverse Reactions

Asthma:

>10%: Local: Injection site reaction (45%; severe 12%; includes bruising, redness, warmth, burning, stinging, itching, hive formation, pain, indurations, mass, and inflammation). Most reactions occurred within 1 hour, lasted <8 days, and decreased in frequency with additional dosing.

1% to 10%:

Cardiovascular: Pulmonary embolism (≤3%), venous thrombosis (≤3%), myocardial infarction (2%), unstable angina pectoris (2%)

Central nervous system: Pain (7%), dizziness (3%), fatigue (3%)

Dermatologic: Dermatitis (2%), pruritus (2%)

Neuromuscular & skeletal: Arthralgia (8%), leg pain (4%), arm pain (2%), bone fracture (2%)

Otic: Otalgia (2%)

Chronic idiopathic urticaria:

>10%: Central nervous system: Headache (6% to 12%)

1% to 10%:

Cardiovascular: Peripheral edema (≥2%)

Central nervous system: Anxiety (≥2%), migraine (≥2%)

Dermatologic: Alopecia (≥2%)

Gastrointestinal: Toothache (≥2%)

Genitourinary: Urinary tract infection (≥2%)

Infection: Fungal infection (≥2%)

Local: Injection site reaction (3%)

Neuromuscular & skeletal: Arthralgia (3%), limb pain (≥2%), musculoskeletal pain (≥2%), myalgia (≥2%)

Respiratory: Nasopharyngitis (9%), sinusitis (5%), upper respiratory tract infection (3%), asthma (≥2%), oropharyngeal pain (≥2%), sinus headache (≥2%), cough (2%), viral upper respiratory tract infection (≤2%)

Miscellaneous: Fever (≥2%)

All indications: <1% (Limited to important or life-threatening): Alopecia, anaphylaxis, antibody development, arthritis, chest tightness, Churg-Strauss syndrome, lymphadenopathy, malignant neoplasm, pulmonary hypertension, syncope, thrombocytopenia, transient ischemic attacks

ALERT: U.S. Boxed Warning

Anaphylaxis:

Anaphylaxis, presenting as bronchospasm, hypotension, syncope, urticaria, and/or angioedema of the throat or tongue, has been reported to occur after administration of omalizumab. Anaphylaxis has occurred as early as after the first dose of omalizumab but also has occurred beyond 1 year after beginning regularly administered treatment. Because of the risk of anaphylaxis, observe patients closely for an appropriate period of time after omalizumab administration. Health care providers administering omalizumab should be prepared to manage anaphylaxis that can be life-threatening. Inform patients of the signs and symptoms of anaphylaxis and instruct them to seek immediate medical care if symptoms occur.

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular effects: Cerebrovascular events, including transient ischemic attack and ischemic stroke, have been reported.

• Eosinophilia and vasculitis: In rare cases, patients may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. Healthcare providers should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between omalizumab and these underlying conditions has not been established.

• Fever/arthralgia/rash: Reports of a constellation of symptoms including fever, arthritis or arthralgia, rash, and lymphadenopathy have been reported with postmarketing use (symptoms resemble those seen in patients experiencing serum sickness, although circulating immune complexes or a skin biopsy consistent with a Type III hypersensitivity reaction were not seen with these cases). Onset of symptoms generally occurred 1 to 5 days following the first or subsequent doses. Discontinue therapy in any patient reporting this constellation of signs/symptoms.

• Hypersensitivity/anaphylactoid reactions: [US Boxed Warning]: Anaphylaxis, including delayed-onset anaphylaxis, has been reported following administration; anaphylaxis may present as bronchospasm, hypotension, syncope, urticaria, and/or angioedema of the throat or tongue. Anaphylaxis has occurred after the first dose and in some cases >1 year after initiation of regular treatment. Due to the risk, patients should be observed closely for an appropriate time period after administration and should receive treatment only under direct medical supervision. Healthcare providers should be prepared to administer appropriate therapy for managing potentially life-threatening anaphylaxis. Patients should be instructed on identifying signs/symptoms of anaphylaxis and to seek immediate care if they arise. In postmarketing reports, anaphylaxis usually occurred with the first or second dose and with a time to onset of ≤60 minutes; however, reactions have been reported with subsequent doses (after 39 doses) and with a time to onset of up to 4 days after administration. A case-control study showed that patients with a history of anaphylaxis to foods, medications, or other causes were at an increased risk of anaphylaxis. Discontinue therapy following any severe reaction.

• Malignant neoplasms: Have been reported rarely with use in short-term studies; impact of long-term use is not known.

Disease-related concerns:

• Parasitic infections: Use with caution and monitor patients at high risk for parasitic (helminth) infections; risk of infection may be increased; appropriate duration of continued monitoring following therapy discontinuation has not been established.

Concurrent drug therapy issues:

• Corticosteroid therapy: Gradually taper systemic or inhaled corticosteroid therapy; do not discontinue corticosteroids abruptly following initiation of omalizumab therapy. The combined use of omalizumab and corticosteroids in patients with chronic idiopathic urticaria has not been evaluated.

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warnings/precautions:

• Appropriate use: Therapy has not been shown to alleviate acute asthma exacerbations; do not use to treat acute bronchospasm or status asthmaticus. Do not use to treat forms of urticaria other than chronic idiopathic urticaria.

• Dosing/IgE levels: Dosing for asthma is based on body weight and pretreatment total IgE serum levels. IgE levels remain elevated up to 1 year following treatment; therefore, levels taken during treatment or for up to 1 year following treatment cannot and should not be used as a dosage guide. Dosing in chronic idiopathic urticaria is not dependent on serum IgE (free or total) level or body weight.

Monitoring Parameters

Anaphylactic/hypersensitivity reactions, baseline serum total IgE; FEV1, peak flow, and/or other pulmonary function tests; monitor for signs of infection

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. IgG molecules are known to cross the placenta. A registry has been established to monitor outcomes of women exposed to omalizumab during pregnancy or within 8 weeks prior to pregnancy (http://www.xolairpregnancyregistry.com or 866-496-5247).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, dyspepsia, asthenia, pharyngitis, or rhinitis. Have patient report immediately to prescriber signs of infection, paresthesia, osteodynia, dyspnea, severe injection site irritation, angina, pain, syncope, dyspnea, edema, or hemoptysis (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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