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TLR Agonists

TLR agonist licensing opportunities from 3M

Discover the Potential of Immunotherapeutics

As science continues to elucidate the complex controls governing immune responsiveness, we can expect to see an increasing role for TLR agonists. With a variety of molecules at various stages of development, 3M is your go-to partner to expand your portfolio with licensing opportunities in this new and exciting arena.

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Explore 3M TLR Agonists

We offer a wide variety of molecules at different stages of development, for use in a range of vaccine and non-vaccine therapeutics:

Dermatology | Cancer | Vaccine Adjuvants | Allergic Rhinitis

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For Use in Dermatology

3M produced the very first TLR7 agonist product, Aldara (imiquimod 5% cream). Aldara was approved in 1997 for the topical treatment of external genital warts, actinic keratosis, and basal cell carcinoma. Since then, 3M has synthesized well over 10,000 distinct molecules that act either as selective TLR7, selective TLR8, or as TLR7/8 agonists. These agonists have potential utility against a broad spectrum of diseases, including a variety of dermatologic indications.

Potential benefits of second generation topical compounds:

852 TLR agonist 852

  • More potent, more selective TLR7 agonist
  • Easier to formulate than imiquimod
  • Potential for better efficacy
  • Less off-target effects than imiquimod
  • Longer patent life
  • Currently in Phase I for dermatology application

S-34240 TLR agonist S-34240

  • More potent and easier to formulate than imiquimod
  • Molecule can be sterilized, offering broader utility than Aldara
  • Currently in preclinical development
  • Long patent life

3M-052 (injectible) Injectible TLR agonist 3M-052

  • Potent TLR7/8 agonist
  • Stays at the site upon injection (unlike other TLR 7 agonists) reducing systemic side effect
  • Potential to eliminate tumors after 2-3 doses
  • GLP Toxicology studies underway

854A TLR agonist 854A

  • TLR7/8 agonist
  • POC with TLR7/8 agonist shows better efficacy in AK and warts than Aldara

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For Treatment of Head and Neck Cancer Injectible TLR agonist 3M-052

Current treatments for head and neck cancer are effective only for 40-50% of recipients. They have major side-effects (pain from feeding tubes, difficulty swallowing, rash, cardiac arrest), and 60% of patients are still dying.

TLR agonist 3M-052 changes everything. It’s not just a treatment. This next- generation immunotherapy could lead to a cure with far fewer side effects than standard surgical and radiation treatments.

How it works
Our product stimulates the body’s own immune system to kill the tumor and inhibit recurrence. Initially indicated for patients who can’t receive surgery, we believe 3M-052 will eventually replace surgery as the standard of care.

  • Patented distinct molecule in the IRM family
  • Similar to Aldara, the only TLR agonist approved to topically treat cancer
  • Once a week injection for solid tumors
  • Remains at injection site and stimulates immune system to attack and destroy tumors
  • Currently in preclinical development

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For Use as Vaccine Adjuvants
3M-052 is the next generation of TLR 7/8 agonists for vaccine adjuvant use. Novel chemistry results in prolonged retention of adjuvants with antigen at administration site, resulting in increased cell-mediated immunity and decreased systemic cytokine production associated with adverse effects.

Bottom line: 3M-052 is less toxic and more effective. Injectible TLR agonist 3M-052

  • Liposomal or oil-in-water formulation acts as an effective adjuvant to:
    • Enhance immunoglobulin production to various antigens, including Influenza hemagglutinin (HA) and Hepatitis-B virus surface antigen (HBsA)
    • Skew antibody responses towards a Th1 response with multiple antigens
  • More effective than resiquimod at enhancing immune responses over a wide range of doses
  • Consistent results observed with multiple antigens and multiple formulations
  • Active in both mouse and non-human primate models

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For Use in Allergic Rhinitis
854 is a TLR 7/8 agonist that has been formulated in an aqueous pump system for treatment of allergic rhinitis. Allergic rhinitis is considered to be a Th2-mediated disease process, and 854A has been shown to inhibit many aspects of the Th2 immune response.

TLR 7/8 agonists, like 854A, are known to: TLR agonist 854A

  • Inhibit IgE production and Th2 cytokine release
  • Inhibit eosinophil recruitment and activation
  • Inhibit mucus production and plasma extravasation in the nose

Topical delivery to the nose inhibits various aspects of allergic rhinitis without high levels of systemic drug exposure.

Get Started
3M has a variety of molecules to be licensed for a broad range of vaccine adjuvants and non-vaccine therapeutics. For details and to discuss your TLR agonist licensing opportunities, talk to your local 3M representative, or contact us online for more information.

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Related Posters, Presentations and Publications

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