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.