Adoption of Transferrin receptor for BBB crossing pathway

Adoption of Transferrin receptor for BBB crossing pathway

Our blood-brain barrier (BBB) ​​solution, BrainAccess®, is a second-generation drug delivery system for the central nervous system. This platform transports oligonucleotide and other drug modalities across the BBB using the transferrin receptor (TfR) transcytosis route.

Brain Access® Mechanism

The characteristics of our polymer micelle DDS using navigator molecules for TfR are:

  • No need for glycemic control
  • Almost the same size with or without the contents of the micelle
  • High transport efficiency per navigator molecule because many drugs can be encapsulated in micelles
  • Due to high transport efficiency, lower BrainAccess® dose is required to achive equivalent efficacy, and better safety can be expected.
  • High transport efficiency can provide cost advantage (because of the higher molecular weight of drug that can be delivered to one ligand)

With our “Brain Access®”, we realize brain DDS using the TfR pathway and enable effective and safe brain delivery, thereby providing a treatment method for unmet needs for CNS diseases. This is our mission.

Integration of Brain Access® (combination of TfR ligand & micelle technology)

When micelles equipped with a TfR ligand were administered to mice, a clear difference was observed in the distribution within the brain compared to administration of non-micellar TfR antibody.

Either fluorescently labeled antibodies or micelles were administered to mice, and 1 hour later the brain distribution was examined. TfR antibody was localized to the cerebral capillary endothelial cells. In contrast, TfR ligand-micelles were also distributed within the brain parenchyma. This unique prototype demonstrates the efficacy of combining a TfR ligand and micelle technology.

Anti-TfR Antibody

Trapped in Brain Microvascular Endothelial Cells

anti-TfR Fab’-installed Micelle

Broad Distribution in Brain Parenchyma

Superior expansion capability of the Brain Access® platform

Brain Access® has excellent platform extensibility, and we are expanding modality and developing functional ligands(navigation molecure). This makes it possible to meet a wide range of modality CNS delivery needs and customizations such as site-specific delivery.