This review article discusses PET agents, other than (18)F-FDG, with the potential to monitor the response to therapy before, during, or after therapeutic intervention. This review deals primarily with non-(18)F-FDG PET tracers that are in the final stages of preclinical development or in the early stages of clinical application for monitoring the therapeutic response. Four sections related to the nature of the tracers are included: radiotracers of DNA synthesis, such as the 2 most promising agents, the thymidine analogs 3'-(18)F-fluoro-3'-deoxythymidine and (18)F-1-(2'-deoxy-2'-fluoro-beta-d-arabinofuranosyl)thymine; agents for PET imaging of hypoxia within tumors, such as (60/62/64)Cu-labeled diacetyl-bis(N(4)-methylthiosemicarbazone) and (18)F-fluoromisonidazole; amino acids for PET imaging, including the most popular such agent, l-[methyl-(11)C]methionine; and agents for the imaging of tumor expression of androgen and estrogen receptors, such as 16beta-(18)F-fluoro-5alpha-dihydrotestosterone and 16alpha-(18)F-fluoro-17beta-estradiol, respectively.