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Small Molecule Agonist of TLR 7/8 Targeting Immunomodulator and Vaccine Adjuvant

Technology #20110214

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ImmunomodulatorToll-like Receptor
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Researchers
David Ferguson, PhD
Professor, Director of Graduate Studies, Medicinal Chemistry
External Link (www.pharmacy.umn.edu)
Courtney Aldrich, PhD
Associate Professor, Medicinal Chemistry
External Link (www.pharmacy.umn.edu)
John Ohlfest, PhD
Managed By
Kevin Anderson
Technology Licensing Officer 612-624-8293
Patent Protection

US Patent Pending 20140212442

Toll-like Receptor 7/8 Agonist as a Immunomodulator

Immunomodulation is the use of a specific substance to affect the immune system, and is commonly used in many developing therapies. However, current immunomodulators have been found to be suboptimal in their control, specificity, and flexibility components. A small molecule agonist of toll-like receptor 7/8 (TLR 7/8) has been identified to act as an immune response modifier. This TLR agonist has a unique structure that permits biomolecule conjugation and administration ease. In vitro and in vivo studies have revealed that this small molecule triggers a more desirable ratio of pro-inflammatory and anti-inflammatory molecules, including unique induction of interleukin-1beta in human monocyte-derived dendritic cells, a unique mechanism of action for drug development.

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Applications Include Cancer Therapy, Vaccine Adjuvant and Dermatology Treatment

This technology could have a variety of applications including cancer therapy, vaccine adjuvant (cancer and infectious), and dermatology treatments. This unique immunomodulator also has the potential to increase efficacy and strength of immune response given its more desired cytokine profile and ability to induce rapid T cell differentiation. Existing technologies do not demonstrate these key features and broad treatment applications.

BENEFITS OF TOLL-LIKE RECEPTOR 7/8 AGONIST:

  • IL-1beta induction in human dendritic cells- a unique mechanism of action for drug development
  • Improved/modified physical properties- potentially increased efficacy and strength of immune response
  • More rapid differentiation of T cells within several days after antigen challenge
  • Simple bioconjugate system- easy preparation in a clinical setting without the need for special reagents or equipment
  • Development as a single agent or codevelopment with oncology and dermatology treatments
  • Potential as preferred adjuvant for vaccine delivery

Phase of Development Several derivative examples prepared, characterized and tested in vivo.