Trial Watch: experimental TLR7/TLR8 agonists for oncological indications

Resiquimod (R848) and motolimod (VTX-2337) are second-generation experimental derivatives of imiquimod, an imidazoquinoline with immunostimulatory properties originally approved by the US Food and Drug Administration for the topical treatment of actinic keratosis and genital warts more than 20 years...

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Bibliographic Details
Published in:Oncoimmunology 2020-01, Vol.9 (1), p.1796002-1796002
Main Authors: Frega, Giorgio, Wu, Qi, Le Naour, Julie, Vacchelli, Erika, Galluzzi, Lorenzo, Kroemer, Guido, Kepp, Oliver
Format: Article
Language:English
Subjects:
Cancer immunotherapy
CGAS
danger signaling
immune checkpoint blockers
immunogenic cell death
Review
type I interferon
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Summary:Resiquimod (R848) and motolimod (VTX-2337) are second-generation experimental derivatives of imiquimod, an imidazoquinoline with immunostimulatory properties originally approved by the US Food and Drug Administration for the topical treatment of actinic keratosis and genital warts more than 20 years ago. Both resiquimod and motolimod operate as agonists of Toll-like receptor 7 (TLR7) and/or TLR8, in thus far delivering adjuvant-like signals to antigen-presenting cells (APCs). In line with such an activity, these compounds are currently investigated as immunostimulatory agents for the treatment of various malignancies, especially in combination with peptide-based, dendritic cell-based, cancer cell lysate-based, or DNA-based vaccines. Here, we summarize preclinical and clinical evidence recently collected to support the development of resiquimod and motolimod and other TLR7/TLR8 agonists as anticancer agents.
ISSN:2162-4011
2162-402X
2162-402X
DOI:10.1080/2162402X.2020.1796002