Trial Watch: experimental TLR7/TLR8 agonists for oncological indications.

Abstract

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.

• Authors: Giorgio Frega, Qi Wu, Julie Le Naour, Erika Vacchelli, Lorenzo Galluzzi, Guido Kroemer, Oliver Kepp
• Journal: Oncoimmunology (Oncoimmunology) Vol. 9 Issue 1 Pg. 1796002 (07 21 2020) ISSN: 2162-4011 [Print] United States
• PMID: 32934889 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Review)
• Copyright: © 2020 The Author(s). Published with license by Taylor & Francis Group, LLC.

Chemical References

• Adjuvants, Immunologic
• Antineoplastic Agents
• Toll-Like Receptor 7
• Toll-Like Receptor 8
• Imiquimod

Topics

• Adjuvants, Immunologic (pharmacology)
• Antineoplastic Agents (pharmacology)
• Imiquimod
• Toll-Like Receptor 7
• Toll-Like Receptor 8
• United States