belimumab

A monoclonal antibody produced by recombinant DNA technique that specifically binds to B-lymphocyte stimulator protein, thereby inactivating it.

Therapeutic effects:

↓survival of B cells, including autoreactive ones and ↓ differentiation into immunoglobulin-producing plasma cells. Result is ↓ disease activity with lessened damage/improvement in mucocutaneous, musculoskeletal, and immunologic manifestations of systemic lupus erythematosus.
Improvement in or stabilization of renal function in lupus nephritis.

Pharmacokinetics ⬆ ⬇

Absorption: 74% absorbed after SUBQ administration; IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Unknown.

Half-Life: 19.4 days.

Time/Action Profile ⬆ ⬇

(↓ in activated B cells)

ROUTE	ONSET	PEAK	DURATION
IV or SUBQ	8 wk	unknown	52 wk‡

‡With continuous treatment.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Receiving therapy for chronic infection.

Use Cautiously in:

Infections (consider temporary withdrawal for acute infections, treat aggressively);
Concurrent use of immunosuppressant therapy or impaired immune function (↑ risk of progressive multifocal leukoencephalopathy [PML]);
Previous history of depression or suicidal ideation (may worsen);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Safety not established in breastfeeding;
Rep: Women of reproductive potential;
Pedi: Children <5 yr (safety and effectiveness not established);
Geri: Older adults may be more sensitive to drug effects.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: rash

GI: diarrhea, nausea

GU: cystitis

Hemat: leukopenia

MS: extremity pain, myalgia

Neuro: depression, insomnia, migraine, anxiety, fatigue, PML, SUICIDAL IDEATION/BEHAVIOR

Misc: fever, infusion reactions, ANAPHYLAXIS, facial edema, INFECTION

Interactions ⬆ ⬇

Drug-drug:

↑risk of adverse reactions and ↓ immune response to live vaccines; should not be given concurrently.
↑risk of serious infections and postinjection systemic reactions when used with rituximab.

Route/Dosage ⬆ ⬇

Systemic Lupus Erythematosus

IV (Adults and Children ≥5 yr): 10 mg/kg every 2 wk for 3 doses; then 10 mg/kg every 4 wk.
SUBQ (Adults and Children ≥5 yr and ≥40 kg): 200 mg once weekly; if transitioning from IV therapy, give 1st SUBQ dose 1–4 wk after last IV dose.
SUBQ (Children ≥5 yr and 15–<40 kg): 200 mg every 2 wk; if transitioning from IV therapy, give 1st SUBQ dose 1–4 wk after last IV dose.

Lupus Nephritis

IV (Adults and Children ≥5 yr): 10 mg/kg every 2 wk for 3 doses; then 10 mg/kg every 4 wk.
SUBQ (Adults and Children ≥5 yr and ≥40 kg): 400 mg (given as two 200-mg injections) once weekly for 4 wk; then 200 mg once weekly. May transition from IV therapy after completing 1st two IV doses; give 1st 200 mg SUBQ dose 1–2 wk after last IV dose.
SUBQ (Children ≥5 yr and 15–<40 kg): 200 mg once weekly for 4 wk; then 200 mg every 2 wk; if transitioning from IV therapy, give 1st SUBQ dose 1–2 wk after last IV dose; then continue with 200 mg every 2 wk.

Availability ⬆ ⬇

Lyophilized powder for IV injection: 120 mg/vial; 400 mg/vial
Solution for SUBQ injection (prefilled syringes and autoinjectors): 200 mg/mL

Assessment ⬆ ⬇

Monitor for signs of anaphylaxis (hypotension, angioedema, urticaria, rash, pruritus, wheezing, dyspnea, facial edema) during and following injection. Medications (antihistamines, corticosteroids, epinephrine) and equipment should be readily available. If anaphylaxis or other severe allergic reaction occurs, discontinue belimumab immediately.
Monitor for infusion reactions (headache, nausea, skin reactions, bradycardia, myalgia, rash, urticaria, hypotension). If infusion reaction occurs, infusion rate may be slowed or interrupted.
Assess for signs of infection, including tuberculosis, prior to injection. If active infection is present, do not initiate belimumab. If serious infection occurs during therapy, monitor, treat as indicated, and consider holding belimumab until infection controlled.
Assess for signs of PML (hemiparesis, apathy, confusion, cognitive deficiencies, ataxia) periodically during therapy.

Implementation ⬆ ⬇

Consider premedication for prophylaxis against infusion and hypersensitivity reaction.
SUBQ: Allow autoinjector or prefilled syringe to sit at room temperature for 30 min prior to injection. Solution is clear to opalescent and colorless to pale yellow; do not use if discolored or contains particulates. Inject into abdomen or thigh; rotate sites each week. Avoid areas of tenderness, bruising, redness, or induration. Do not freeze or shake. Avoid exposure to heat. May store at room temperature for ≤12 hr if protected from sunlight.

IV Administration:

Intermittent Infusion: Allow to stand 10–15 min at room temperature. Reconstitution: Using a 21–25-gauge needle, reconstitute 120-mg vial with 1.5 mL and 400-mg vial with 4.8 mL of sterile water for injection by directing stream toward side of vial to minimize foaming. Swirl gently for 60 sec. Allow vial to sit at room temperature during reconstitution, swirling gently for 60 sec every 5 min until powder is dissolved. Do not shake. Reconstitution usually takes 10–15 min but may take up to 30 min. Protect from sunlight. Solution is opalescent and colorless to pale yellow and without particles. Small bubbles are expected and acceptable. Concentration: 80 mg/mL. Diluent: 0.9% NaCl, 0.45% NaCl or LR. Remove volume of patient’s dose from a 250-mL infusion bag and discard. Replace with required amount of reconstituted solution. Gently invert bag to mix. Do not administer if discolored or contains particulates. Discard unused solution in vial. If not used immediately, refrigerate or store at room temperature and protect from light. Total time from reconstitution to completion of infusion should not exceed 8 hr.
Rate: Rate: Infuse over 1 hr; may slow or interrupt rate if infusion reaction occurs.
Y-Site Incompatibility: Do not administer other drugs through same IV line.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient or caregiver in correct technique for SUBQ injection, care, and disposal of equipment. Inject on the same day each week. Inject missed dose as soon as remembered; then resume on usual day or start a new weekly schedule from the day missed dose was administered. Do not inject two doses on same day.
Caution patient to notify health care provider immediately if signs of infection (fever; sweating; chills; muscle aches; cough; shortness of breath; blood in phlegm; weight loss; warm, red, or painful skin or sores; diarrhea or stomach pain; burning on urination; urinary frequency; feeling tired), PML, severe rash, or swollen face occurs.
Advise patient and caregiver to notify health care provider immediately for signs of suicidality, attempts to die by suicide, new or worse depression or anxiety, agitation or restlessness, panic attacks, insomnia, new or worse irritability, aggressiveness, acting on dangerous impulses, mania, other changes in mood or behavior, or symptoms of serotonin syndrome.
Caution patient to avoid receiving live vaccines for 30 days before and during belimumab therapy.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
Rep: Advise women of reproductive potential to use effective contraception during and for ≥4 mo after final dose and to notify health care provider if breastfeeding. Encourage pregnant patients to enroll in pregnancy registry by calling 1-877-311-8972 or visiting https://mothertobaby.org/ongoing-study/benlysta-belimumab/.

Evaluation/Desired Outcomes ⬆ ⬇

Improvement in mucocutaneous, musculoskeletal, and immunologic disease activity in patients with systemic lupus erythematosus.
Improvement in or stabilization of renal function in lupus nephritis.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0409- Hospira, Inc.
- 0409-9966-
  - 0409-9966-01- 192 VIAL in 1 PACKAGE (0409-9966-01) / 5 mL in 1 VIAL (0409-9966-11)

49401- GlaxoSmithKline LLC
- 49401-088- BENLYSTA
  - 49401-088-02- 1 SYRINGE in 1 CARTON (49401-088-02) / 1 mL in 1 SYRINGE (49401-088-01)

49401- GlaxoSmithKline LLC
- 49401-088- BENLYSTA
  - 49401-088-35- 4 SYRINGE in 1 CARTON (49401-088-35) / 1 mL in 1 SYRINGE (49401-088-01)

49401- GlaxoSmithKline LLC
- 49401-088- BENLYSTA
  - 49401-088-47- 4 SYRINGE in 1 CARTON (49401-088-47) / 1 mL in 1 SYRINGE (49401-088-42)

49401- GlaxoSmithKline LLC
- 49401-088- BENLYSTA
  - 49401-088-50- 1 SYRINGE in 1 CARTON (49401-088-50) / 1 mL in 1 SYRINGE (49401-088-42)

49401- GlaxoSmithKline LLC
- 49401-088- BENLYSTA
  - 49401-088-61- 1 SYRINGE in 1 CARTON (49401-088-61) / 1 mL in 1 SYRINGE

49401- GlaxoSmithKline LLC
- 49401-101- BENLYSTA
  - 49401-101-01- 1 VIAL in 1 CARTON (49401-101-01) / 1.5 mL in 1 VIAL

49401- GlaxoSmithKline LLC
- 49401-102- BENLYSTA
  - 49401-102-01- 1 VIAL in 1 CARTON (49401-102-01) / 5 mL in 1 VIAL

71124- SAMSUNG BIOLOGICS Co., Ltd.
- 71124-0025-
  - 71124-0025-0- 16 kg in 1 BAG (71124-0025-0)

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Pronunciation ⬇

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