NUCALA
  • NUCALA

  • QTY 1 • 100 MG • VIAL • Near 77381

MEPOLIZUMAB (me poe LIZ ue mab) is a monoclonal antibody. It treats severe asthma. It is used with other drugs for asthma. It also treats other conditions that have a high level of eosinophils (a type of white blood cell) called hypereosinophilic syndrome (HES) or Churg-Strauss Syndrome. This medicine is also used to treat adults with sinus inflammation with nasal polyps.

NUCALA Pediatric Monographs
  • General Administration Information
    For storage information, see the specific product information within the How Supplied section.

    Route-Specific Administration

    Injectable Administration
    -Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit. The solution should be clear to opalescent and colorless to pale yellow or pale brown.
    -Mepolizumab vials should be reconstituted and administered by a healthcare professional.
    -The mepolizumab injection prefilled autoinjector and the prefilled syringe are only for use in pediatric patients aged 12 years and older. Either may be administered by a caregiver if the healthcare provider determines it is appropriate.
    -For a 300 mg dose, administer as 3 separate 100-mg injections at least 5 cm (approximately 2 inches) apart.
    -Monitoring of patients after administration of biologic agents is recommended.
    Subcutaneous Administration
    Mepolizumab for Injection Vial

    Reconstitution
    -Reconstitute with 1.2 mL Sterile Water for Injection, preferably using a 2- or 3-mL syringe and a 21-gauge needle. The final concentration will be 100 mg/mL (144 mg/vial). There will be overfill in the vial.
    -Direct the stream of diluent vertically into the center of the lyophilized powder. Gently swirl the vial for 10 seconds at 15-second intervals until the powder is dissolved. Do not shake the reconstituted solution, as this may lead to foaming or precipitation. Reconstitution is usually complete within 5 minutes but may take additional time.
    -If a mechanical reconstitution device (swirler) is used, swirl at 450 rpm for no longer than 10 minutes. Alternatively, swirling at 1,000 rpm for no longer than 5 minutes is acceptable.
    -The solution should be clear to opalescent and colorless to pale yellow or pale brown and essentially particle-free. Small air bubbles are expected and acceptable.
    -Do not mix with other medications.
    -Storage: If not used immediately, store below 30 degrees C (86 degrees F), but do not freeze. Discard if not used within 8 hours of reconstitution.

    Subcutaneous Administration from the Vial

    -Administer the dose into the upper arm, thigh, or abdomen; a 1-mL polypropylene syringe fitted with a disposable 21- to 27-gauge x 0.5-inch (13-mm) needle is preferred for subcutaneous administration.
    -For a 100 mg dose, remove 1 mL (100 mg) of the reconstituted solution from the vial.
    -For a 40 mg dose, remove 0.4 mL (40 mg) of the reconstituted solution from the vial.
    -Each vial should be used for a single patient, and any remainder of the contents should be discarded.

    Mepolizumab Injection Prefilled Autoinjector and Prefilled Syringe
    -Provide proper training in subcutaneous injection technique and on the preparation and administration of mepolizumab injection prior to use according to the "Instructions for Use".
    -Do not use the prefilled autoinjector or prefilled syringe if it is dropped on a hard surface or if it looks damaged.
    -Remove the prefilled autoinjector or prefilled syringe from the refrigerator and allow it to sit at room temperature for approximately 30 minutes prior to injection. Do NOT warm mepolizumab in any other way.
    -Administer the subcutaneous injection into the thigh or abdomen, avoiding the 5 cm (2 inches) around the navel. The upper arm can also be used if a caregiver administers the subcutaneous injection. If multiple injections are needed, ensure injection sites are separated by at least 5 cm (2 inches). Never give injections into areas where the skin is tender, bruised, red, or hard.
    -If a dose is missed, administer a dose as soon as possible. Thereafter, the patient can resume dosing on the usual day of administration. If the next dose is already due, then administer as planned.
    -Do not use the prefilled syringe or autoinjector more than 1 time. Throw away the autoinjector or prefilled syringe in an FDA-cleared sharps disposal container after injection.
    -Storage: Store unopened autoinjectors or prefilled syringes in the original carton in the refrigerator between 2 and 8 degrees C (36 and 46 degrees F); do not freeze. Protect from light. Do not shake. Keep away from heat. If needed, an unopened carton can be stored outside the refrigerator at up to 30 degrees C (86 degrees F) for up to 7 days. Dispose of the injection properly if it is left out of the refrigerator in the unopened carton for more than 7 days. The prefilled autoinjector must be used within 8 hours after it is removed from the carton. Discard properly if it is not used within 8 hours.

    The adverse reaction profile for patients aged 6 to 11 years was similar to that observed in patients aged 12 years and older.

    In patients with severe asthma, systemic non-allergic reactions were reported by 2% of mepolizumab-treated patients, compared to 3% of those receiving placebo. The most commonly reported manifestations included rash, flushing, and myalgia. Fatigue (5%), back pain (5%), and muscle cramps/spasms (3%) were also reported. Asthenia and musculoskeletal pain were reported in 3% or more of patients receiving intravenous mepolizumab 75 mg (not an approved dosage or route). Arthralgia (6%) was reported during adult trials for chronic rhinosinusitis with nasal polyps.

    Headache (19%) was 1 of the most common adverse reactions reported during mepolizumab clinical trials for severe asthma. Dizziness (3% or more) was reported during a 52-week dose-ranging and exacerbation-reduction trial of intravenous mepolizumab 75 mg (not an approved dosage or route).

    Upper abdominal pain was reported in 3% of actively treated patients during clinical trials for severe asthma. Abdominal pain, gastroenteritis, dental pain (toothache), nausea, and vomiting were reported in 3% or more of patients receiving intravenous mepolizumab 75 mg (not an approved dosage or route). Oropharyngeal pain (8%), upper abdominal pain (3%), and diarrhea (3%) were reported in adult trials for chronic rhinosinusitis.

    Opportunistic herpes zoster infections have occurred in patients receiving mepolizumab; consider varicella vaccination prior to starting therapy if medically appropriate. In controlled trials, 2 serious adverse reactions of herpes zoster occurred in patients receiving subcutaneous mepolizumab (n = 263) compared to none in patients receiving placebo (n = 257). In addition, 3 cases of herpes zoster occurred in patients treated with intravenous mepolizumab 75 mg (n = 153) during a 52-week dose-ranging and exacerbation-reduction trial, compared to 2 cases in those receiving placebo (n = 155); of note, mepolizumab is not indicated for intravenous use and should only be given by the subcutaneous route. Additional cases of herpes zoster have been reported in long-term open-label extension studies. Other infectious and/or respiratory events including influenza (3%), urinary tract infection (3%), fever (3%), and nasal dryness (3%) were reported during clinical trials. Allergic rhinitis, bronchitis, cystitis, dyspnea, ear infection, gastroenteritis, lower respiratory tract infection, nasal congestion, pharyngitis, nasopharyngitis, fever, viral infection, and viral respiratory tract infection were reported in 3% or more of patients receiving intravenous mepolizumab 75 mg (not an approved dosage or route).

    Hypersensitivity reactions (e.g., anaphylaxis, angioedema, bronchospasm, hypotension, urticaria, rash) have occurred after mepolizumab administration. Such reactions generally occur within hours of administration, but may have a delayed onset (i.e., days). Discontinue mepolizumab and institute appropriate treatment if a hypersensitivity reaction occurs. In patients with severe asthma, systemic allergic/hypersensitivity reactions were reported by 1% of actively treated patients compared to 2% in the placebo group; these reactions included rash (3% or more), pruritus (3%), headache, and myalgia. Urticaria, erythema, flushing, fatigue, hypertension, warm sensation in trunk and neck, cold extremities, and shortness of breath were reported as manifestations of hypersensitivity in clinical trials specific to adults. Eczema (3%) and multifocal skin reaction was also reported during clinical trials.

    An injection site reaction (e.g., pain, erythema, swelling, itching, burning) occurred in 2% to 15% of patients receiving subcutaneous mepolizumab during clinical trials.

    Antibody formation occurred in 6% or less of patients who received subcutaneous mepolizumab in clinical trials. Neutralizing antibodies were detected in 1 patient who had severe asthma. The clinical relevance of the presence of anti-mepolizumab antibodies is unknown. Antibodies increased the clearance of mepolizumab by about 20%. There was no evidence of a correlation between anti-mepolizumab antibody titers and change in eosinophil concentration.

    Mepolizumab is contraindicated in patients with a history of hypersensitivity to mepolizumab or excipients in the formulation. Use with caution in patients with hamster protein hypersensitivity, as the drug is produced in Chinese hamster ovary cells. Hypersensitivity reactions (e.g., angioedema, bronchospasm, hypotension, urticaria, rash) have occurred after mepolizumab administration. Such reactions generally occur within hours of administration, but may have a delayed onset (i.e., days). If a hypersensitivity reaction occurs, discontinue the drug and institute appropriate treatment.

    Mepolizumab should not be used to treat acute bronchospasm or status asthmaticus. Patients should seek medical advice if their asthma remains uncontrolled or worsens after mepolizumab initiation. Short-acting beta-agonists, such as albuterol, should be available for rescue therapy.

    Do not discontinue systemic or inhaled corticosteroid therapy abruptly upon mepolizumab initiation. Corticosteroid withdrawal and dosage reduction, if appropriate, should be done gradually under the direct supervision of a physician. Reduction in corticosteroid dose may be associated with systemic withdrawal symptoms and/or unmask conditions previously suppressed by systemic corticosteroid therapy.

    In pre-marketing clinical trials, 2 cases of serious herpes infection (herpes zoster) occurred in patients who received mepolizumab compared to none in the placebo group. Nine hundred ninety-eight (998) subjects have received mepolizumab in ongoing open-label extension studies, during which additional cases of herpes zoster have been reported. If medically appropriate, consider varicella vaccination prior to treatment initiation.

    Treat patients with a pre-existing helminth infection prior to initiating therapy with mepolizumab. If a patient becomes infected while receiving mepolizumab therapy and does not respond to anti-helminth treatment, discontinue mepolizumab therapy until the infection resolves. Mepolizumab reduces the production and survival of eosinophils, which may be involved in the immunological response to some helminth infections. Although it is not known whether if mepolizumab will influence the body's response against parasitic infections, caution is warranted. Patients with known parasitic infections were excluded from clinical trials.

    Description: Mepolizumab is a subcutaneous humanized interleukin-5 receptor alpha-directed cytolytic monoclonal antibody (IgG1, kappa) indicated for add-on maintenance treatment of severe asthma with an eosinophilic phenotype and for treatment of hypereosinophilic syndrome (HES). This biologic therapy is directed against interleukin (IL)-5, which is known to play an important role in regulating the function of eosinophils, an inflammatory cell responsible for airway inflammation in some types of asthma. Use of mepolizumab in patients with severe asthma (eosinophilic phenotype) led to fewer exacerbations requiring hospitalization and/or emergency department care and a longer time to the first exacerbation, compared to those who received placebo. Clinical trial data indicated that mepolizumab use may also lead to a decrease in dosage of oral maintenance corticosteroids, while maintaining asthma control, for these patients. GINA recommends use in patients aged 6 years and older with severe eosinophilic asthma not controlled with usual therapies; GINA notes that their recommendations for ages 6 to 11 years were limited to data from one small uncontrolled study. The NAEPP includes add-on mepolizumab therapy as a consideration in pediatric patients 12 years and older with severe persistent asthma after confirmatory phenotyping. However, the NAEPP has withheld specific recommendations for the use of newer biologics for patients with severe asthma (NAEPP steps 5 and 6) pending further clinical study assessments of the role of biologics in patients with specific phenotypes and/or endotypes. Mepolizumab is FDA-approved for asthma in patients 6 years and older and for HES is patients 12 years and older.

    For asthma maintenance add-on therapy in patients with severe asthma (eosinophilic phenotype):
    Subcutaneous dosage:
    Children 6 to 11 years: 40 mg subcutaneously once every 4 weeks.
    Children and Adolescents 12 to 17 years: 100 mg subcutaneously once every 4 weeks.

    For the treatment of hypereosinophilic syndrome (HES) present for at least 6 months without an identifiable non-hematologic secondary cause:
    NOTE: Mepolizumab has been designated by the FDA as an orphan drug for the first-line treatment in patients with HES.
    Subcutaneous dosage:
    Children and Adolescents 12 to 17 years: 300 mg subcutaneously every 4 weeks; administer as 3 separate 100-mg injections at least 5 cm (approximately 2 inches) apart.

    Maximum Dosage Limits:
    -Neonates
    Safety and efficacy have not been established.
    -Infants
    Safety and efficacy have not been established.
    -Children
    1 to 5 years: Safety and efficacy have not been established.
    6 to 11 years: 40 mg subcutaneously every 4 weeks for asthma; safety and efficacy for hypereosinophilic syndrome have not been established.
    12 years: 100 mg subcutaneously every 4 weeks for asthma; 300 mg subcutaneously every 4 weeks for hypereosinophilic syndrome.
    -Adolescents
    100 mg subcutaneously every 4 weeks for asthma; 300 mg subcutaneously every 4 weeks for hypereosinophilic syndrome.

    Patients with Hepatic Impairment Dosing
    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Patients with Renal Impairment Dosing
    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    *non-FDA-approved indication

    Monograph content under development

    Mechanism of Action: Mepolizumab is a fully-humanized monoclonal antibody (IgG1 kappa) that targets human interleukin (IL)-5. Inflammation is a major component in the pathogenesis of asthma and hypereosinophilic syndrome; many cell types (e.g., eosinophils) and mediators (e.g., cytokines) are involved in inflammation. IL-5 is the major cytokine responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils. Mepolizumab selectively binds to IL-5, blocking it from binding to the alpha chain of the IL-5 receptor complex located on the eosinophil cell surface. This, in turn, inhibits IL-5 signaling and reduces the production and survival of eosinophils. Other undefined mechanisms of action may also play a role.

    Pharmacokinetics: Mepolizumab is administered by subcutaneous injection. The central volume of distribution (Vd) of mepolizumab in adult patients with asthma is approximately 3.6 L for a 70-kg individual. Mepolizumab is a humanized IgG1 monoclonal antibody, and degradation occurs via proteolytic enzymes that are widely distributed throughout the body and not restricted to hepatic tissue. Apparent systemic clearance in adult and adolescent patients is estimated to be 0.28 L/day for a 70-kg individual. Mean terminal half-life in adult patients ranges from 16 to 22 days.

    Affected cytochrome P450 isoenzymes and drug transporters: none


    -Route-Specific Pharmacokinetics
    Subcutaneous Route
    After subcutaneous administration in the upper arm, the bioavailability of mepolizumab in adult and adolescent patients with asthma was approximately 80%. After repeated subcutaneous administration once every 4 weeks, there was approximately a 2-fold accumulation at steady state.


    -Special Populations
    Pediatrics
    There is no significant effect of age on mepolizumab clearance in patients 12 years and older. In a pharmacokinetic study in patients aged 6 to 11 years with severe asthma, simulation of a 40 mg subcutaneous dose every 4 weeks in children aged 6 to 11 years, irrespective of body weight, resulted in predicted exposures similar to that observed in adults and adolescents.

    Hepatic Impairment
    Mepolizumab is degraded by widely distributed proteolytic enzymes, not restricted to hepatic tissue. Changes in hepatic function are not expected to affect elimination; however, no clinical trials have been conducted to investigate the effect of hepatic impairment on mepolizumab pharmacokinetics.

    Renal Impairment
    Mepolizumab is not cleared renally. Based on population pharmacokinetic analyses, mepolizumab clearance was comparable between patients with a CrCl 50 to 80 mL/minute and those with normal renal function. There is limited data in patients with a CrCl less than 50 mL/minute; however, changes in renal function are not expected to affect mepolizumab pharmacokinetics.

    Gender Differences
    There is no significant effect of gender on mepolizumab clearance.

    Ethnic Differences
    There is no significant effect of race on mepolizumab clearance.

DISCLAIMER: This drug information content is provided for informational purposes only and is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Patients should always consult their physician with any questions regarding a medical condition and to obtain medical advice and treatment. Drug information is sourced from GSDD (Gold Standard Drug Database ) provided by Elsevier.

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