The oral A2AR inhibitor CPI-444 in combination with immune checkpoint blockades, such as antibodies against programmed death 1 (PD-1) or cytotoxic T-lymphocyte-associated protein-4 (CTLA-4), generated synergistic antitumor effects and significant tumor regression and led to memory antitumor immune responses in preclinical studies (82). The gene discussed is ADORA2A; the disease is neoplasm.