Improved Efficacy in a Fabry Disease Model Using a Systemic mRNA Liver Depot System as Compared to Enzyme Replacement Therapy

Mol Ther. 2019 Apr 10;27(4):878-889. doi: 10.1016/j.ymthe.2019.03.001. Epub 2019 Mar 6.

Abstract

Fabry disease is a lysosomal storage disorder caused by the deficiency of α-galactosidase A. Enzyme deficiency results in a progressive decline in renal and cardiac function, leading to cardiomyopathy and end-stage renal disease. Current treatments available, including enzyme replacement therapies, have provided significant benefit to patients; however, unmet medical needs remain. mRNA therapy, with drug-like properties, has the unique ability to produce therapeutic proteins endogenously. Here we describe the sustained delivery of therapeutic human α-galactosidase protein in vivo via nanoparticle-formulated mRNA in mouse and non-human primate, with a demonstration of efficacy through clinically relevant biomarker reduction in a mouse Fabry disease model. Multi-component nanoparticles formulated with lipids and lipid-like materials were developed for the delivery of mRNA encoding human α-galactosidase protein. Upon delivery of human GLA mRNA to mice, serum GLA protein levels reached as high as ∼1,330-fold over normal physiological values.

Keywords: Fabry; delivery; enzyme replacement therapy; lipid nanoparticle; mRNA.

MeSH terms

  • Animals
  • Callithrix
  • Disease Models, Animal
  • Drug Compounding / methods
  • Drug Delivery Systems / methods
  • Enzyme Replacement Therapy / methods*
  • Fabry Disease / drug therapy*
  • Female
  • Gene Knockout Techniques
  • Humans
  • Kidney / drug effects
  • Kidney / metabolism
  • Lipids / chemistry
  • Liver / drug effects*
  • Liver / metabolism*
  • Male
  • Mice
  • Mice, Knockout
  • Nanoparticles / administration & dosage
  • RNA, Messenger / administration & dosage
  • RNA, Messenger / genetics*
  • Treatment Outcome
  • alpha-Galactosidase / administration & dosage
  • alpha-Galactosidase / biosynthesis
  • alpha-Galactosidase / genetics

Substances

  • Lipids
  • RNA, Messenger
  • GLA protein, human
  • alpha-Galactosidase