Definition

An orally bioavailable inhibitor of C-C-chemokine receptor 8 (CCR8), with potential immunomodulating and antineoplastic activities. Upon oral administration, CCR8 inhibitor IPG7236 targets, binds to and blocks the activity of CCR8 on CCR8-positive tumor-infiltrating regulatory T cells (Tregs) in the tumor microenvironment (TME) and prevents chemokine ligand 1 (CCL1)-CCR8-mediated signaling. This may reactivate antitumor immune responses. CCR8 is specifically expressed by tumor-infiltrating Tregs in multiple types of cancer and plays a key role in immunosuppression, proliferation, resistance, migration and angiogenesis. High expression is correlated with poor prognosis.