Pharmacogenomics and translational simulations to bridge indications for an anti-interferon-α receptor antibody

Clin Pharmacol Ther. 2013 Jun;93(6):483-92. doi: 10.1038/clpt.2013.35. Epub 2013 Feb 14.

Abstract

A type I interferon (IFN) gene signature shared by systemic lupus erythematous (SLE) and systemic sclerosis (SSc) was used to evaluate an anti-type I IFN-α receptor (IFN-αR) monoclonal antibody, MEDI-546, in a phase I trial in SSc. MEDI-546 suppressed IFN signature in blood and skin of SSc patients in a dose-dependent manner. To bridge clinical indications to SLE, we developed a model incorporating (i) pharmacokinetics (PK) and pharmacodynamics (PD) in SSc patients, (ii) internalization kinetics of MEDI-546/IFN-αR complex, and (iii) the different IFN signatures between SSc and SLE. Simulations predicted that i.v. administration of MEDI-546 at 300- or 1,000-mg monthly doses could suppress IFN signature in blood to levels of healthy subjects in 53 and 68% of SLE patients, respectively. An innovative approach utilizing a novel biomarker characterized the PD of MEDI-546 by modeling and simulation and allowed rapid progression of MEDI-546 from a phase I study in SSc to a randomized, multiple-dose phase II trial.

Publication types

  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal / therapeutic use*
  • Antibodies, Monoclonal, Humanized
  • Biomarkers / blood
  • Biomarkers / metabolism
  • Clinical Trials, Phase II as Topic
  • Computer Simulation*
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Interferon-alpha / genetics
  • Interferon-alpha / metabolism*
  • Lupus Erythematosus, Systemic / drug therapy
  • Male
  • Middle Aged
  • Models, Biological
  • Pharmacogenetics*
  • Receptor, Interferon alpha-beta / immunology*
  • Receptor, Interferon alpha-beta / metabolism*
  • Scleroderma, Systemic / blood
  • Scleroderma, Systemic / drug therapy*
  • Scleroderma, Systemic / metabolism
  • Skin / metabolism

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Biomarkers
  • Interferon-alpha
  • Receptor, Interferon alpha-beta
  • anifrolumab