Benlysta (belimumab)

Immunomodulator, B-Lymphocyte Stimulator (BLyS)-Spec Inhib Intravenous Vial (Ea); Subcutaneous Auto-Injector (Ml); Subcutaneous Syringe (Ml)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Belimumab, a recombinant fully human immunoglobulin G1 lambda (IgG1 lambda) monoclonal antibody, inhibits soluble human B-lymphocyte stimulator (BLyS) and is an immunosuppressive agent.

Belimumab is a recombinant fully human immunoglobulin G1 lambda (IgG1 lambda) monoclonal antibody that specifically binds to and inhibits the biologic effects of soluble human B-lymphocyte stimulator (BLyS). BLyS is a cytokine in the tumor necrosis factor (TNF) ligand family that contributes to B-lymphocyte differentiation and survival. BLyS binds to 3 receptors on B lymphocytes: transmembrane activator and calcium modulator and cyclophilin ligand interactor (TACI), B-cell maturation antigen (BCMA), and B-cell-activating factor receptor/BLyS receptor 3 (BAFF-R/BR3).

BLyS inhibits B-cell apoptosis and stimulates differentiation of B cells into immunoglobulin-producing plasma cells. Selective inhibition of BLyS reduces the number of B cells, with preferential reduction of naive and transitional B cells. BLyS is overexpressed in patients with systemic lupus erythematosus (SLE) and other autoimmune diseases.

Belimumab inhibits the binding of soluble BLyS to its receptors on B cells, thereby inhibiting the survival of B cells, including autoreactive B cells, and reducing the differentiation of B cells into immunoglobulin-producing plasma cells.

In clinical trials in adult patients with SLE, treatment with belimumab significantly reduced circulating CD19+, CD20+, naive, and activated B cells, and the SLE B-cell subset at week 52. Memory cells increased initially and slowly declined toward baseline levels by week 52. Treatment also led to reductions in IgG and antibodies to double-stranded DNA (anti-dsDNA).

In patients with low complement levels at baseline, treatment led to increases in complement C3 and C4 as early as week 12 and these increases were sustained through week 52. In patients with active lupus nephritis, belimumab caused a decrease in serum IgG as early as week 4; subsequently, there was an increase in serum IgG levels, which was associated with decreased proteinuria. Reductions in autoantibodies, increases in complement, and reductions in circulating total B cells and B-cell subsets observed were consistent with the studies in patients with SLE.

Clinical relevance of these effects has not been definitively established.

The subcutaneous bioavailability of belimumab is approximately 74%. Peak plasma concentrations are achieved in 2.6 days following subcutaneous administration of belimumab at steady state. Steady-state concentrations are achieved from week 2 of dosing with a subcutaneous loading dose of belimumab 400 mg weekly in patients with lupus nephritis.

The average concentrations at steady state with weekly maintenance dosing of belimumab 200 mg subcutaneously are predicted to be comparable to those seen following administration of belimumab 10 mg/kg IV every 4 weeks.

The terminal half-life of IV belimumab is 19.4 days and 18.3 days with sub-Q administration. The pharmacokinetics of belimumab have not been formally studied in hepatic and renal impairment. Body weight and body mass index do not have clinically important effects on belimumab pharmacokinetics following subcutaneous administration in adults.

Since pediatric patients with lower body weight experience reduced clearance and volume of distribution of the drug, these patients are administered subcutaneous belimumab less frequently.

USES: This medication is used with other medications to treat certain types of lupus. Belimumab belongs to a class of drugs known as monoclonal antibodies. It works by decreasing the effect of a certain protein that is increased in people with active lupus.

This may help decrease some of the symptoms of lupus.

Generic name: belimumab
Pronunciation: (be-LIM-ue-mab)
Drug class: Immunomodulator, B-Lymphocyte Stimulator (BLyS)-Spec Inhib
Therapeutic class: Analgesic, Anti-inflammatory or Antipyretic

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Benlysta

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Indications

The following indications are listed for Benlysta:

  • Active Lupus Nephritis
  • Systemic Lupus Erythematosus

Also known as: Disseminated Lupus Erythematosus, Lupus Erythematosus Syndrome.

Dosing

No dosing information is available for this tab.

Drug interactions

No formal drug interaction studies have been performed with belimumab to date.

Contraindications

*History of anaphylactic reaction to belimumab.

Adverse reactions

Adverse effects reported in >=5% of patients receiving belimumab include nausea, diarrhea, pyrexia, nasopharyngitis, bronchitis, insomnia, pain in extremity, depression, migraine, pharyngitis, and injection site reactions (with subcutaneous administration).

Precautions

No enhanced messaging available.

ICD codes

CodeTypeDescription
Active lupus nephritis
M32.14ICD10CMGlomerular disease in systemic lupus erythematosus
Systemic lupus erythematosus
M32ICD10CMSystemic lupus erythematosus (SLe)
M32.0ICD10CMDrug-induced systemic lupus erythematosus
M32.1ICD10CMSystemic lupus erythematosus with organ or system involvement
M32.10ICD10CMSystemic lupus erythematosus, organ or system involvement unspecified
M32.11ICD10CMEndocarditis in systemic lupus erythematosus
M32.12ICD10CMPericarditis in systemic lupus erythematosus
M32.13ICD10CMLung involvement in systemic lupus erythematosus
M32.14ICD10CMGlomerular disease in systemic lupus erythematosus
M32.15ICD10CMTubulo-interstitial nephropathy in systemic lupus erythematosus
M32.19ICD10CMOther organ or system involvement in systemic lupus erythematosus
M32.8ICD10CMOther forms of systemic lupus erythematosus
M32.9ICD10CMSystemic lupus erythematosus, unspecified

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data