FA-TLR7a

FA-TLR7a is a folate–Toll-like receptor 7 agonist conjugate designed to selectively target and activate folate receptor beta (FRβ)–expressing myeloid cells, such as tumor-associated macrophages (TAMs) and myeloid-derived suppressor cells (MDSCs) within the tumor microenvironment. The folate moiety directs the conjugate to FRβ, which is overexpressed on immunosuppressive myeloid cells in tumors, enabling localized delivery and avoiding the systemic toxicity seen with untargeted TLR7 agonists. Upon uptake, the TLR7 agonist is delivered into endosomes of myeloid cells, stimulating TLR7 signaling to reprogram TAMs/MDSCs from an immunosuppressive, tissue-regenerating M2-like phenotype towards a pro-inflammatory, tumoricidal M1-like phenotype. FA-TLR7a suppresses tumor growth, inhibits metastasis, reduces immunosuppressive cell populations, and enhances T cell infiltration and activation in preclinical models. It has been shown to significantly augment the efficacy of CAR T cell immunotherapy for solid tumors without detectable systemic immune activation or toxicity. The drug has been studied in preclinical settings using murine models, with Endocyte named as a developer in published research[1][5][3].

Other names

folate-TLR7afolate-TLR-7afolate-TLR 7afolate–toll-like receptor 7 agonistfolate-TLR7-1Afolate-TLR-7-1Afolate-TLR 7-1AFA-TLR7-1AFA-TLR-7-1AFA-TLR 7-1Afolic acid–conjugated TLR7 agonistfolate-conjugated TLR7 agonist