emicizumab (Rx)

Brand and Other Names:Hemlibra, emicizumab-kxwh
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, IV solution (single-dose vials)

  • 30mg/mL
  • 60mg/0.4 mL
  • 105mg/0.7 mL
  • 150mg/mL

Hemophilia A

Indicated for routine prophylaxis to prevent or reduce the frequency of bleeding episodes in adults with hemophilia A with or without factor VIII inhibitors

Loading dose: 3 mg/kg SC qWeek for the first 4 weeks

Maintenance dose

  • 1.5 mg/kg SC qWeek, OR
  • 3 mg/kg SC q2Weeks, OR
  • 6 mg/kg SC q4Weeks

Selection of maintenance dose based on healthcare provider preference with consideration of regimens that may increase patient adherence

Discontinue prophylactic use of bypassing agents 1 day before starting prophylaxis

Prophylactic use of factor VIII (FVIII) products may be continued during first week of prophylaxis

See also Administration

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-89 mL/min): Pharmacokinetics are not affected

Hepatic impairment

  • Mild-to-moderate (total bilirubin 1X to ≤3X ULN and any AST): Pharmacokinetics are not affected

Dosage Forms & Strengths

injection, IV solution (single-dose vials)

  • 30mg/mL
  • 60mg/0.4 mL
  • 105mg/0.7 mL
  • 150mg/mL

Hemophilia A

Indicated for routine prophylaxis to prevent or reduce the frequency of bleeding episodes in patients aged newborn and older with hemophilia A with or without factor VIII inhibitors

Loading dose: 3 mg/kg SC qWeek for the first 4 weeks

Maintenance dose

  • 1.5 mg/kg SC qWeek, OR
  • 3 mg/kg SC q2Weeks, OR
  • 6 mg/kg SC q4Weeks

Selection of maintenance dose based on healthcare provider preference with consideration of regimens that may increase patient adherence

Discontinue prophylactic use of bypassing agents 1 day before starting prophylaxis

Prophylactic use of factor VIII (FVIII) products may be continued during first week of prophylaxis

See also Administration

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-89 mL/min): Pharmacokinetics are not affected

Hepatic impairment

  • Mild-to-moderate (total bilirubin 1X to ≤3X ULN and any AST): Pharmacokinetics are not affected

Dosing Considerations

Self-administration is not recommended for children <7 years

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Interactions

Interaction Checker

and emicizumab

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (6)

              • axicabtagene ciloleucel

                emicizumab, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • brexucabtagene autoleucel

                emicizumab, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • ciltacabtagene autoleucel

                emicizumab, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • idecabtagene vicleucel

                emicizumab, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • lisocabtagene maraleucel

                emicizumab, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • tisagenlecleucel

                emicizumab, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              Monitor Closely (6)

              • antihemophilic factor recombinant

                antihemophilic factor recombinant, emicizumab. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of emicizumab with rFVIIa or FVIII increases possibility for hypercoagulability.

              • efgartigimod alfa

                efgartigimod alfa will decrease the level or effect of emicizumab by receptor binding competition. Use Caution/Monitor. Coadministration of efgartigimod with medications that bind to the human neonatal Fc receptor may lower systemic exposures and effectiveness of such medications. Closely monitor for reduced effectiveness of medications that bind to the human neonatal Fc receptor. If long-term use of such medications is essential, consider discontinuing efgartigimod and using alternative therapies.

              • Factor VIIa, recombinant

                Factor VIIa, recombinant, emicizumab. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of emicizumab with rFVIIa or FVIII increases possibility for hypercoagulability.

              • Factor VIII, human plasma derived

                Factor VIII, human plasma derived, emicizumab. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of emicizumab with rFVIIa or FVIII increases possibility for hypercoagulability.

              • isavuconazonium sulfate

                emicizumab and isavuconazonium sulfate both decrease immunosuppressive effects; risk of infection. Use Caution/Monitor.

              • prothrombin complex concentrate, human

                prothrombin complex concentrate, human, emicizumab. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Thrombotic microangiopathy reported when aPCC was coadministered with emicizumab. Patients presented with thrombocytopenia, microangiopathic hemolytic anemia, and acute kidney injury, without severe deficiencies in ADAMTS13 activity. Thromboembolism was also reported with coadministration.

              Minor (0)

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                Adverse Effects

                >10%

                Injection site reaction (22%)

                Headache (15%)

                Arthralgia (15%)

                Injection site erythema (11%)

                1-10%

                Pyrexia (6%)

                Diarrhea (6%)

                Injection site pruritus (4%)

                Injection site pain (4%)

                <1%

                Rhabdomyolysis

                Postmarketing Reports

                Skin and subcutaneous tissue disorders: Rash, urticaria, angioedema

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                Warnings

                Black Box Warnings

                Thrombotic microangiopathy and thromboembolism

                • Cases of thrombotic microangiopathy (TMA) and thrombotic events reported when, on average, a cumulative amount of >100 U/kg/24 hr of activated prothrombin complex concentrate (aPCC) was administered for ≥24 hr to patients receiving emicizumab-kxwh prophylaxis
                • Monitor the development of thrombotic microangiopathy and thrombotic events if aPCC is administered
                • Discontinue aPCC and suspend emicizumab-kxwh if symptoms occur

                Contraindications

                None

                Cautions

                Cases of TMA reported from clinical trials; improvement was seen within 1 week following discontinuation of aPCC (see Black Box Warnings)

                Thrombotic events reported from clinical trials when on average a cumulative amount of >100 U/kg/24 hr of aPCC was administered for ≥24 hr to patients receiving emicizumab-kxwh prophylaxis; no thrombotic event required anticoagulation therapy; evidence of improvement or resolution seen within one month following discontinuation of aPCC; consider benefits and risks of emicizumab-kxwh if aPCC must be used in patients receiving the drug or resuming prophylaxis following complete resolution of thrombotic event; monitor for development of thromboembolism when administering aPCC (see Black Box Warnings)

                Immunogenicity

                • May induce antidrug antibodies
                • Most patients with anti-emicizumab-kxwh antibodies did not experience a change in plasma concentrations or an increase in bleeding events; in uncommon cases, the presence of neutralizing antibodies with decreasing plasma concentration may be associated with loss of efficacy
                • Monitor for clinical signs of loss of efficacy (eg, increase in breakthrough bleeding events) and if observed, promptly assess the etiology, and consider a change in treatment if neutralizing antibodies are suspected

                Drug interactions overview

                • Clinical experience suggests that a drug interaction exists with emicizumab-kxwh and aPCC; due to long half-life of the drug, the potential for interaction with aPCC may persist for up to 6 months after last dose; possible for hypercoagulability with recombinant factor VIIa (rFVIIa) or Factor VIII (FVIII) with emicizumab-kxwh based on preclinical experiments
                • Drug laboratory test interactions
                  • Intrinsic pathway clotting-based laboratory tests were affected; therefore these laboratory tests should not be used in monitoring emicizumab-kxwh; due to the long half-life of the drug, effects on coagulation essays may persist for up to 6 months after last dose
                  • Results affected by emicizumab: Activated aPTT; Bethesda assays (clotting-based) for FVIII inhibitor titers; one-stage, aPTT-based, single-factor assays; aPTT-based activated protein C resistance (APC-R); and activated clotting time
                  • Results unaffected by emicizumab: Bethesda assays (bovine chromogenic) for FVIII inhibitor titers; thrombin time; one-stage, prothrombin time-based, single-factor assays; chromogenic-based single-factor assays other than FVIII; immuno-based assays (eg, ELISA, turbidimetric methods); and genetic tests of coagulation factors (eg, factor V Leiden, prothrombin 20210)
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                Pregnancy

                Pregnancy

                No data are available regarding use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage

                Unknown whether treatment can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity

                Should be used during pregnancy only if the potential benefit for the mother outweighs the risk to the fetus

                Women of childbearing potential should use contraception during treatment

                Lactation

                No information is available regarding the presence of emicizumab-kxwh in human milk, the effects on the breastfed child, or the effects on milk production

                Human IgG is known to be present in human milk

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Bispecific factor IXa- and factor X-directed antibody that bridges activated factor IX and factor X in order to restore the function of missing activated factor VIII necessary for effective hemostasis

                Absorption

                Peak plasma concentration, steady-state: 55.1 mcg/mL (1.5 mg/kg-dose); 58.3 mcg/mL (3 mg/kg-dose); 67 mcg/mL (6 mg/kg-dose)

                AUC, steady-state: 376 mcg/mL·day (1.5 mg/kg-dose); 752 mcg/mL·day (3 mg/kg-dose); 1503 mcg/mL·day (6 mg/kg-dose)

                Bioavailability, 1 mg/kg dose: 80.4-93.1%

                Observed similar pharmacokinetic profiles following SC administration in the abdomen, upper arm, and thigh

                Distribution

                Vd: 10.4L

                Excretion

                Clearance: 0.27 L/day

                Half-life: 26.9 days

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                Administration

                SC Preparation

                Visually inspect vial for particulate matter and discoloration prior to administration; solution appears colorless to slightly yellow; do not use if particulate matter is visible or product is discolored

                Do not use different vials of different concentrations when combining vials to administer prescribed dose

                SC administration

                SC use only

                Administer doses of up to 1 mL with a 1-mL syringe (graduation 0.01 mL)

                Administer doses >1 mL to ≤2 mL with a 2-mL or 3-mL syringe (graduation 0.1 mL)

                Use a transparent polypropylene or polycarbonate syringe with Luer-Lok tip, sterile, for injection only, single-use, latex-free, nonpyrogenic, and commercially available in the United States

                Rotate injection sites (upper outer arms, thighs, or any quadrant of abdomen) from previous injection

                Do not inject into moles, scars, or areas where the skin is tender, bruised, red, hard, or not intact

                Administration into the upper outer arm should only be performed by a caregiver or healthcare provider

                Discard any unused drug remaining

                Missed dose

                • Administer as soon as possible prior to day of next scheduled dose, and then resume usual weekly dosing schedule
                • Do not double doses to make up for a missed dose

                Storage

                Opened vials: Single-dose vials; discard any unused solution remaining after administering dose

                Unopened vials

                • Store in refrigerator at 2-8°C (36-46°F) in original carton to protect from light; do not freeze; do not shake
                • If necessary, unopened vials may be stored at room temperature and then returned to refrigeration; temperature should not exceed 30°C (86°F) for up to 7 days
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.