Our Technology

About Our Technology

Our Science

 

 

 

 

Identifying MFSD2A as the Transporter at the Blood-brain barrier

 

 

 

 

Breakthrough Discovery / Advantage of MSFD2A Transport

The Mfsd2a transporter

  • A naturally occurring physiological transport mechanism
  • Proven to transport lipids when they are linked to a Lyso-Phosphatidyl-Cholines (LPC) head group across the BBB
  • Proven Efficiency of BBB delivery
  • MFSD2A transporter present in brain, eye and gut
  • Targeted brain delivery will reduce peripheral drug load and improve Risk/Benefit Ratio
  • Significantly enhance oral bioavailability

The Blood-Brain Barrier Challenge

Blood-Brain Barrier (BBB)

Protective barrier of the Central Nervous System (CNS) to prevent toxic compounds entering the brain from the circulatory system

Challenge

  • BBB prevents > 98% of small molecule drugs from entering the brain
  • Relatively high peripheral drug concentrations results in side effects
  • Poor success rate due to reliance on ineffective or non-selective delivery

Solution

Utilization of the newly discovered Mfsd2a transporter to deliver therapeutics across the BBB

  • Revitalize dormant candidates
  • Repurposing of existing drugs
  • Assist in the development of new therapies for currently untreatable diseases

Travecta Platform: Delivery Technology

Travecta’s novel Drug Delivery Technology uses proprietary vectors to more effectively deliver therapeutics to the CNS
  • Modify rate/selectivity of transport process
  • Target sub-cellular compartments
  • Modulate overall pharmacology of the drug conjugate:ADME*
  • Improve transport kinetics of drug conjugates with MFSD2a
  • Optimize fatty chain for drug transport in conjunction with Head Group
 
  • Broaden scope of application to wider range of pharmaceuticals
  • Develop linker systems with predicable and tunable off-rates:chemical/enzymatic cleavages
  • Optimize size, shape, polarity and position of attachment on the drug
  • Ideal position of attachment to the fatty chain

Travecta Platform: Validation Tools

Step 1
Cell Culture

In vitro transport of Drug conjugates

  • Human derived HEK293 cells overexpressing MFSD2a, including MFSD2a mutant constructs as controls
  • Neural stem cells that naturally express MFSD2a
  • Mutant neural stem cells that are genetically deficient in MFSD2a
Step 2
Mouse Models

In vivo transport of Drug conjugates

  • Wild type vs. MFSD2a Knock Out mice
Step 3
In Vivo Models

In vivo distribution of Drug conjugates

  • Oral bioavailability
  • Brain delivery
  • Radiolabeling

 

Proprietary assays and know-how allow for rapid confirmation of BBB transport