Single-agent TLR7 agonist treatment of advanced primary or metastatic liver cancers induces local inflammation of the TME by reprogramming myeloid cells. Combination therapies may be needed to increase the relocation of antitumor CD8 T effector cells to the TME and unlock the full potential of the local immune stimulatory effect.
This defined the lowest pharmacologically active dose as 3 mg.The prodrug entered the clinic in 2020 in patients with primary or secondary liver cancers. Clear pharmacodynamic, transient and dose-dependent cytokine induction was observed at prodrug doses >1 mg.