Office for Technology Commercialization

Immunomodulators and Immunomodulator Conjugates

Technology #20160274-20160275-20110214

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David Ferguson, PhD
Professor, Medicinal Chemistry
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Courtney Aldrich, PhD
Associate Professor, Medicinal Chemistry; Center for Drug Design
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John Ohlfest, PhD
Managed By
Kevin Anderson
Technology Licensing Officer 612-624-8293
Patent Protection

US Patent Pending 20170217960
US Patent 9,034,336
Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8
ACS Medicinal Chemistry Letters, 2017, 8 (11), pp 1148–1152
Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction
ACS Medicinal Chemistry Letters, 2012, 3 (6), pp 501–504

Commercially Viable Small Molecule TLR7/8-Targeting Immunomodulator and Vaccine Adjuvant

Novel small molecule agonists of toll-like receptors 7 and 8 (TLR7 and TLR8) act as immune response modifiers and have potential immunomodulatory activity. These newly synthesized imquidazolequinoline-based compounds trigger a more desirable ratio of pro- to anti-inflammatory cytokines and therefore appear to have a potentially new mechanism of action compared to other known TLR7/8 immunomodulators. These drugs could be used for a variety of applications including cancer treatment, vaccine adjuvants and skin conditions (e.g., warts, herpes, and more). One of the compounds also shows unique biological activity relative to other compounds in this class.

More Specific and Unique Immune Response

Toll-like receptors play a crucial role in host defense, inflammation and immune response, and significant efforts have gone into development of potent TLR agonists. Adjuvants help antigens elicit an early, high and long-lasting immune response, allowing more robust responses to vaccines and reducing vaccine production costs. TLR 7 and 8 are key targets for the design of small molecule immunomodulators for use as vaccine adjuvants and anticancer/antiviral agents. However, while some of the compounds in this class of adjuvants induce pro-inflammatory cytokines, important for priming a robust immune response associated with anti-tumor and anti-viral activity in animals, they concurrently induce high levels of anti-inflammatory cytokines resulting in treatment failures. These compounds, with potentially different activity, could make the immune response more specific and unique compared to other products currently known. Furthermore, these new compounds offer a more desirable ratio of pro-inflammatory and anti-inflammatory molecules along with a unique induction of IL-1β in that could result in a strong antibody response.


  • TLR7/8 immunomodulators
  • Imquidazolequinoline-based compounds
  • Stimulate human adaptive immune response
  • Vaccine adjuvants could augment innate immune response against inflammatory, microbial and/or viral diseases as well as cancer
  • Immune response modifiers with potential immunomodulatory activity
  • Desirable ratio of pro- to anti-inflammatory cytokines
  • May enable a more specific and unique immune response


  • TLR7/8 immunomodulators
  • Bioconjugates
  • Autoimmune and infectious diseases
  • Vaccines, vaccine adjuvants
  • Cancer treatment
  • Asthma
  • Respiratory conditions
  • Food and skin allergies
  • Skin conditions (e.g., warts, herpes, etc.)

Phase of Development - In Vivo/animal studies

Interested in Licensing?
The University relies on industry partners to scale up technologies to large enough production capacity for commercial purposes. The license is available for this technology and would be for the sale, manufacture or use of products claimed by the issued patents. Please contact Kevin Anderson to share your business needs and technical interest in this technology and if you are interested in licensing the technology for further research and development.