Inhibiting or knocking out A2AR in preclinical models led to tumor regression, spurring the development of the oral A2AR antagonist CPI-444 (ciforadenant), currently in a phase 1/1b trial of 336 patients, alone and in combination with atezolizumab in the treatment of various metastatic solid tumors, including mCRPC (NCT02655822). Here, ADORA2A is linked to neoplasm.