Class: Monoclonal antibody
- Injection, lyophilized powder for solution 120 mg
- Injection, lyophilized powder for solution 400 mg
Blocks the binding of soluble human B lymphocyte stimulator protein (BLyS), a B-cell survival factor, to its receptors on B cells, which inhibits the survival of B cells, including reactive B cells, and reduces the differentiation of B cells into immunoglobulin-producing plasma cells.
C max is 313 mcg/mL and AUC 0-∞ is 3,083 days•mcg/mL.
V ss is 5.29 L.
Terminal half-life is 19.4 days and systemic Cl is 215 mL/day.
Special PopulationsRenal Function Impairment
Increases in creatinine and proteinuria (more than 2 g/day) increased belimumab Cl, but these effects were within the expected range of variability.Hepatic Function Impairment
Pharmacokinetics have not been studied. Baseline ALT and AST levels did not significantly influence belimumab pharmacokinetics.Elderly
Limited pharmacokinetic data are available.Children
Pharmacokinetics have not been assessed.Gender
Pharmacokinetics are not affected by gender.Race
Pharmacokinetics are not affected by race. Response rate for the primary end point were lower for black patients.
Indications and Usage
For the treatment of adults with active, autoantibody-positive SLE who are receiving standard therapy.
Patients who have had anaphylaxis with belimumab.
Dosage and AdministrationSystemic Lupus Erythematosus
IV 10 mg/kg at 2-wk intervals for the first 3 doses and at 4-wk intervals thereafter. Consider administering premedication for prophylaxis against infusion reactions and hypersensitivity reactions.
- For IV infusion only. Do not administer as an IV push or bolus. Administer over a period of 1 h. The infusion rate may be slowed or interrupted if the patient develops an infusion reaction. The infusion must be discontinued immediately if the patient experiences a serious hypersensitivity reaction.
- Allow belimumab vial to stand 10 to 15 min to reach room temperature before reconstitution and dilution.
- Reconstitute the 120 mg vial with 1.5 mL sterile water for injection. Reconstitute the 400 mg vial with 4.8 mL sterile water for injection. The stream of sterile water should be directed toward the side of the vial to minimize foaming. Gently swirl the vial for 60 sec. Allow the vial to sit at room temperature during reconstitution, gently swirling the vial for 60 sec every 5 min until the powder is dissolved. Do not shake. Reconstitution is typically complete within 10 to 15 min after the sterile water has been added, but it may take up to 30 min. The reconstituted solution will contain a concentration of 80 mg/mL belimumab.
- If a mechanical reconstitution device (swirler) is used to reconstitute belimumab, it should not exceed 500 rpm and the vial swirled for no longer than 30 min.
- Once reconstitution is complete, the solution should be opalescent and colorless to pale yellow, and without particles. Small air bubbles, however, are expected and acceptable.
- Dilute the reconstituted product to 250 mL in sodium chloride 0.9% injection. Gently invert the bag or bottle to mix the solution.
- Belimumab should not be infused concomitantly in the same IV line with other agents. Dextrose IV solutions are incompatible with belimumab.
Store vials between 2° and 8°C (36° and 46°F). Vials should be protected from light and stored in the original carton until use. Do not freeze. Avoid exposure to heat. The reconstituted solution, if not used immediately, should be stored protected from direct sunlight at 2° to 8°C (36° to 46°F). Any unused solution in the vials must be discarded. Solutions diluted in normal saline may be stored at 2° to 8°C (36° to 46°F) or room temperature. The total time from reconstitution to completion of infusion should not exceed 8 h.
None well documented.
Insomnia (7%); depression, migraine (5%).
Nausea (15%); diarrhea (12%); viral gastroenteritis (3%).
Bronchitis, nasopharyngitis (9%); pharyngitis (5%).
Pyrexia (10%); pain in extremity (6%); cystitis, leukopenia (4%).
Monitor patients closely for the development of infusion and/or hypersensitivity reactions. Carefully monitor patients who develop a new infection while undergoing treatment.
Category C .
Safety and efficacy not established.
Use with caution.
Special Risk Patients
Use with caution in black patients.
The development of antibelimumab antibodies has occurred.
Serious infusion reactions, including bradycardia, headache, hypotension, myalgia, rash, and urticaria, have occurred.
Has been reported.
Has occurred. Etiologies included infection, CV disease, and suicide.
Primarily depression-related events, suicide, insomnia, and anxiety have been reported. It is unknown if belimumab is associated with an increased risk for these events.
Serious and fatal infections have been reported. Use with caution in patients with chronic infections; patients receiving any therapy for chronic infections should not receive belimumab.
None well documented.
- Give patients the Medication Guide for belimumab and provide them an opportunity to read it prior to each treatment session. It is important that the patient's overall health be assessed at each infusion visit and any questions resulting from the patient's reading of the Medication Guide be discussed.
- Advise patients that more patients receiving belimumab in the main clinical trials died than did patients receiving placebo treatment.
- Advise patients that belimumab may decrease their ability to fight infections. Ask patients if they have a history of chronic infections and if they are currently on any therapy for an infection. Instruct patients to tell their health care provider if they develop signs or symptoms of an infection.
- Educate patients on the signs and symptoms of anaphylaxis, including wheezing, difficulty breathing, peri-oral or lingual edema, and rash. Instruct patients to immediately tell their health care provider if they experience symptoms of an allergic reaction during or after the administration.
- Instruct patients to contact their health care provider if they experience new or worsening depression, suicidal thoughts, or other mood changes.
- Inform patients not to receive live vaccines while taking belimumab. Response to vaccinations could be impaired by belimumab.
- Inform patients that belimumab has not been studied in pregnant or breast-feeding women, so the effects of belimumab on pregnant women or breast-feeding infants are not known. Instruct patients to tell their health care provider if they are pregnant, become pregnant, or are thinking about becoming pregnant. Instruct patients to tell their health care provider if they plan to breast-feed their infant.
- Advise women of childbearing potential to use adequate contraception during treatment with belimumab and for at least 4 mo after final treatment.
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