Pharmacokinetics, pharmacodynamics, short term efficacy and safety of RCT-18, a novel BLyS/APRIL fusion protein, in patients with rheumatoid arthritis

Br J Clin Pharmacol. 2016 Jul;82(1):41-52. doi: 10.1111/bcp.12908. Epub 2016 Apr 7.

Abstract

Aim: RCT-18 is a recombinant fusion protein that interferes with the selection and survival of mature B-lymphocytes by inhibiting B-lymphocyte stimulator and a proliferation-inducing ligand.

Methods: This single blind, randomized, placebo controlled, clinical pharmacological study explored the short term efficacy and safety of RCT-18 in 21 rheumatoid arthritis (RA) patients with three different dosing regimens. The pharmacological behaviour of RCT-18 was also characterized through a six level biomarker cascade approach to identify potential predictors for clinical responses.

Results: Nine out of 10 patients (>80%) experienced moderate to good EULAR response at the end of 3 months with once or twice weekly doses of 180 mg RCT-18, whereas weekly administration of 360 mg RCT-18 or placebo, however, only resulted in moderate improvement in one patient in each group. Absence of IgM-type rheumatoid factor reduction, recovery of IgM 2 weeks after drug cessation, lack of decrease in the count of CD27(+) B-lymphocytes and a DAS28 change from baseline <6 in 4-6 weeks after the treatment initiation may indicate poor clinical response. No anti-drug antibody of RCT-18 was detected. The active treatments were well tolerated, although more mild to moderate infections were reported in patients receiving RCT-18.

Conclusion: The study results support further development of RCT-18 in RA patients and provide important information for future dose selection.

Keywords: efficacy; immunogenicity; pharmacodynamics; pharmacokinetics; rheumatoid arthritis; safety.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antirheumatic Agents / administration & dosage*
  • Antirheumatic Agents / adverse effects
  • Antirheumatic Agents / pharmacokinetics
  • Arthritis, Rheumatoid / drug therapy*
  • B-Lymphocytes / immunology
  • Biomarkers / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Immunoglobulin Fc Fragments / administration & dosage*
  • Immunoglobulin Fc Fragments / adverse effects
  • Immunoglobulin M / immunology
  • Male
  • Middle Aged
  • Recombinant Fusion Proteins / administration & dosage*
  • Recombinant Fusion Proteins / adverse effects
  • Recombinant Fusion Proteins / pharmacokinetics
  • Single-Blind Method
  • Time Factors
  • Transmembrane Activator and CAML Interactor Protein / administration & dosage*
  • Transmembrane Activator and CAML Interactor Protein / adverse effects
  • Transmembrane Activator and CAML Interactor Protein / pharmacokinetics
  • Treatment Outcome
  • Young Adult

Substances

  • Antirheumatic Agents
  • Biomarkers
  • Immunoglobulin Fc Fragments
  • Immunoglobulin M
  • RCT-18 fusion protein
  • Recombinant Fusion Proteins
  • Transmembrane Activator and CAML Interactor Protein