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Blood-Brain Barrier (BBB)

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

Challenge

BBB prevents therapeutics from entering the brain:

  • ~98% of small molecule drugs
  • ~100% of large molecule drugs1
  • Relatively high peripheral levels of drug results in side effects
  • Poor success rate due to reliance on ineffective or non-selective delivery
  • Ubiquitous mechanisms
  • Potentially toxic carriers or directing vectors
  • Technologies with inherent limitations: stability or dose route preference

Solution

  • Discovering a “carrier” to deliver therapeutic treatments across the BBB
  • Opportunity to extend patent life of existing drug therapies
  • Revitalize dormant candidates
  • Assist development of new therapies for currently untreatable diseases
  • Repurposing existing drugs

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

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
  • LPC-drug conjugates have high potential for oral delivery as LPC are naturally absorbed by the gut
  • 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

Travecta Development Platform Medicinal Chemistry

Travecta Development Platform Proprietary Assays and Know-How