Tumor Immunotherapy Using A(2A) Adenosine Receptor Antagonists

The A(2A) adenosine receptor (A(2A)AR) plays critical roles in human physiology and pathophysiology, which makes it an important drug target. Previous drug-discovery efforts targeting the A(2A)AR have been focused on the use of A(2A)AR antagonists for the treatment of Parkinson’s disease. More recently, the A(2A)AR has attracted additional attention for its roles in immuno-oncology, and a number of A(2A)AR antagonists are currently used as lead compounds for antitumor drugs in both preclinical models and clinical trials. This review surveys recent advances in the development of A(2A)AR antagonists for cancer immunotherapy. The therapeutic potential of representative A(2A)AR antagonists is discussed based on both animal efficacy studies and clinical data.