Over the past few years, several studies have proved the potential role of diagnostic procedures in patients with treated prostate cancer who develop biochemical relapse. Notably, no precise indications exist regarding the use of emerging modalities such as positron emission tomography/computerized tomography (PET/CT) scanning with radiolabeled choline. However, the literature suggests that the main and most important application of choline PET/CT at present is in disease restaging in cases of biochemical relapse for the detection of local, lymph node-related or distant recurrence. In this setting, it is well known that prostate-specific antigen (PSA) values play a significant role in the follow-up of these patients. This short review aims at summarizing the results of the most relevant published studies with particular interest directed towards a better understanding of the relationship between PSA kinetics and choline PET/CT detection rate and the potential use of PSA kinetics for an optimal selection of patients who may benefit most from this diagnostic procedure particularly at an early stage of biochemical recurrence.