S1P1-targeted PET tracers

Tech ID: T-016151

Technology Description

Researchers at Washington University in St. Louis have developed sphingosine 1-phosphate receptor 1 (S1P1)-specific PET tracers. Sphingosine 1-phosphate receptors are G-protein coupled receptors, with five subtypes denoted S1P1-5, that have key functions in immune, inflammatory and cardiovascular systems. The expression of S1P1 can be used as a marker for MS, cardiovascular disease and other inflammatory disorders. Therefore, the ability to track S1P1 expression would be beneficial for identifying the disease, monitoring disease progression and assessing therapeutic efficacy. PET imaging is a non-invasive strategy to do this. However, previously developed S1P1-targeted PET tracers had several disadvantages including a requirement for in vivo phosphorylation and low specificity for S1P1. Thus, there is still a great need for viable S1P1-targeted PET tracers. To help meet this need and overcome the disadvantages, the inventors have developed these compounds. The compounds have high affinity and selectivity for S1P1, do not require in vivo phosphorylation and are not subject to metabolic loss of the radionuclide. This technology provides S1P1-targeted PET tracers that can be used to track S1P1-associated disease progression and monitor therapeutic efficacy.

Stage of Research

PET radioactivity and imaging capabilities have been validated in vivo using animal models. Additionally, the e-IND application of 11CS1P1 for human use had been approved by FDA on Dec. 9, 2019.

Related technology

The inventors have also developed sphingosine 1-phosphate receptor 2- specific PET tracers. See Washington University technology T-018580 for more information.

Applications

  • PET tracers for S1P1-associated conditions including MS, cardiovascular disease and neuroinflammatory disease
    • Track disease progression
    • Track therapeutic efficacy
  • Potential for therapeutic development
  • Research tool- investigation into S1P1 role in disease pathogenesis

Key Advantages

  • Solves an unmet need- provides a means to track S1P1-associated disease progression and therapeutic efficacy
  • High specificity for S1P1
  • Does not require in vivo phosphorylation
  • Not subject to metabolic loss of radionuclide
  • Capable of penetrating the blood brain barrier
  • High yield from starting material

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