Complement inhibition as a therapeutic strategy in retinal disorders

Expert Opin Biol Ther. 2019 Apr;19(4):335-342. doi: 10.1080/14712598.2019.1575358. Epub 2019 Feb 11.

Abstract

Introduction: Dry age-related macular degeneration (AMD) and Stargardt Macular Dystrophy (STGD1) result in vision loss due to progressive atrophy of the macula and lack of effective treatments. Numerous studies have implicated complement-associated inflammation as a contributor to both diseases.

Areas covered: The complement factor D inhibitor, lampalizumab, failed to halt geographic atrophy (GA) progression in phase 3 studies. The complement factor 3 (C3) inhibitor, APL-2, has shown potential to reduce GA growth in a phase 2 trial, supporting advancement to phase 3 trials. The intravenous complement factor 5 (C5) inhibitor, eculizumab, failed to halt GA progression in a phase 2 study. Another C5 inhibitor, avacincaptad pegol, is delivered by intravitreal injection, and will be studied for safety and preliminary signs of efficacy for AMD and STGD1 patients in phase 2 trials. LFG316 (C5 inhibitor) and CLG561 (properdin inhibitor) failed to halt GA progression in phase 2 studies. A phase 1 trial is evaluating the effects of combining LFG316 and CL561. Complement inhibition by gene therapy will be explored in the phase 1 trial of HMR59 in AMD patients.

Expert opinion: While complement inhibition has not yet demonstrated the ability to halt GA progression in a phase 3 trial, further study is warranted.

Keywords: APL-2; CL561; Complement; LFG316; Stargardt macular dystrophy; age-related macular degeneration; avacincaptad pegol; eculizumab; geographic atrophy; lampalizumab.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal, Humanized / therapeutic use*
  • Clinical Trials as Topic
  • Complement C3 / immunology
  • Complement C5 / immunology
  • Complement Factor D / immunology
  • Genetic Therapy
  • Geographic Atrophy / drug therapy*
  • Geographic Atrophy / pathology
  • Geographic Atrophy / therapy
  • Humans
  • Immunoglobulin Fab Fragments / therapeutic use*
  • Stargardt Disease / drug therapy*
  • Stargardt Disease / pathology
  • Stargardt Disease / therapy

Substances

  • Antibodies, Monoclonal, Humanized
  • Complement C3
  • Complement C5
  • Immunoglobulin Fab Fragments
  • eculizumab
  • Complement Factor D
  • lampalizumab