Efficacy, pharmacokinetic and pharmacodynamic profile of belimumab for systemic lupus erythematosus

Abstract

Introduction: Systemic lupus erythematosus (SLE) is a severe autoimmune disease and a sizeable proportion of patients remain refractory to currently available immunosuppressive agents. The burden of uncontrolled disease is significant as disease flare and persistent inflammation lead to long-term damage accrual and increased morbidity. Belimumab, a humanized monoclonal antibody that inhibits B-lymphocyte stimulator (BLyS), is the first drug to be approved by the US FDA for the treatment of SLE in 50 years.

Areas covered: In this review, we provide an overview of novel therapeutic agents under development for the treatment of SLE, a description of the pharmacodynamic and pharmacokinetic properties of belimumab, evidence of efficacy of belimumab as demonstrated in clinical trials, safety and tolerability data and a summary of ongoing clinical trials of belimumab in SLE. This information was amassed following a comprehensive MEDLINE and Cochrane library search. Ongoing clinical trial information was obtained from ClinicalTrials.gov.

Expert opinion: Two, large Phase III trials have demonstrated the clinical efficacy of belimumab in musculoskeletal, mucocutaneous, haematologic and constitutional features of SLE. Patients with severe disease manifestations such as lupus nephritis and CNS disease were excluded from these trials and hence the role of belimumab in the overall management of SLE has yet to be established. Studies in lupus nephritis are ongoing.

Keywords:

• belimumab
• B-lymphocyte stimulator
• systemic lupus erythematosus

Declaration of interest

DP D’Cruz reports participation in advisory boards and consultancies for Human Genome Sciences and Roche and has received consulting fees and/or has participated in clinical trials for GlaxoSmithKline, Bristol Myers Squibb, TEVA, Merck Serono and Eli-Lilly. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.