The proteasome inhibitior bortezomib depletes plasma cells and ameliorates clinical manifestations of refractory systemic lupus erythematosus

Ann Rheum Dis. 2015 Jul;74(7):1474-8. doi: 10.1136/annrheumdis-2014-206016. Epub 2015 Feb 20.

Abstract

Objectives: To investigate whether bortezomib, a proteasome inhibitor approved for treatment of multiple myeloma, induces clinically relevant plasma cell (PC) depletion in patients with active, refractory systemic lupus erythematosus (SLE).

Methods: Twelve patients received a median of two (range 1-4) 21-day cycles of intravenous bortezomib (1.3 mg/m(2)) with the coadministration of dexamethasone (20 mg) for active SLE. Disease activity was assessed using the SLEDAI-2K score. Serum concentrations of anti-double-stranded DNA (anti-dsDNA) and vaccine-induced protective antibodies were monitored. Flow cytometry was performed to analyse peripheral blood B-cells, PCs and Siglec-1 expression on monocytes as surrogate marker for type-I interferon (IFN) activity.

Results: Upon proteasome inhibition, disease activity significantly declined and remained stable for 6 months on maintenance therapies. Nineteen treatment-emergent adverse events occurred and, although mostly mild to moderate, resulted in treatment discontinuation in seven patients. Serum antibody levels significantly declined, with greater reductions in anti-dsDNA (∼60%) than vaccine-induced protective antibody titres (∼30%). Bortezomib significantly reduced the numbers of peripheral blood and bone marrow PCs (∼50%), but their numbers increased between cycles. Siglec-1 expression on monocytes significantly declined.

Conclusions: These findings identify proteasome inhibitors as a putative therapeutic option for patients with refractory SLE by targeting PCs and type-I IFN activity, but our results must be confirmed in controlled trials.

Keywords: Autoimmune Diseases; Autoimmunity; B cells; Systemic Lupus Erythematosus; Treatment.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intravenous
  • Adult
  • Antibodies / blood
  • Boronic Acids / administration & dosage
  • Boronic Acids / pharmacology*
  • Boronic Acids / therapeutic use*
  • Bortezomib
  • DNA / immunology
  • Dexamethasone / administration & dosage
  • Dexamethasone / therapeutic use
  • Drug Therapy, Combination
  • Female
  • Germany
  • Humans
  • Interferon Type I / metabolism
  • Lupus Erythematosus, Systemic / drug therapy*
  • Lupus Erythematosus, Systemic / immunology
  • Lupus Erythematosus, Systemic / metabolism
  • Male
  • Plasma Cells / drug effects*
  • Plasma Cells / pathology
  • Proteasome Inhibitors / administration & dosage
  • Proteasome Inhibitors / pharmacology*
  • Proteasome Inhibitors / therapeutic use*
  • Pyrazines / administration & dosage
  • Pyrazines / pharmacology*
  • Pyrazines / therapeutic use*
  • Severity of Illness Index
  • Treatment Outcome

Substances

  • Antibodies
  • Boronic Acids
  • Interferon Type I
  • Proteasome Inhibitors
  • Pyrazines
  • Bortezomib
  • Dexamethasone
  • DNA