FA-TLR7-1A

FA-TLR7-1A is a folate receptor beta (FRβ)-targeted Toll-like receptor 7 (TLR7) agonist conjugate developed by Purdue University. It consists of folic acid (FA) conjugated to a potent, cell-impermeable TLR7 agonist (TLR7-1A) via a hydrophilic, non-cleavable linker. FA-TLR7-1A is designed to selectively target and reprogram immunosuppressive tumor-associated macrophages (TAMs) and myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME) from an M2-like anti-inflammatory phenotype to an M1-like pro-inflammatory phenotype. By restricting activation to FRβ-expressing myeloid cells in inflamed or tumor tissues, FA-TLR7-1A avoids the systemic immune activation and toxicity associated with free TLR7 agonists. Preclinical studies have demonstrated that FA-TLR7-1A induces tumor regression, blocks metastasis, and significantly enhances the efficacy of CAR-T cell therapies and checkpoint inhibitors in solid tumor models.

Other names

FA-TLR7aFA-TLR-7aFA-TLR 7afolate-TLR7-1Afolate-TLR-7-1Afolate-TLR 7-1Afolate-targeted TLR7 agonistfolate-targeted Toll-like receptor 7 agonist