Folate receptor (FR) can be used as a therapeutic target because of its expression on different epithelial cancers, such as ovarian, nonsmall cell lung, endometrial, and breast cancer. Assessing FR expression in tumors may help to identify patients who can benefit from FR-targeted therapeutics, such as vintafolide and farletuzumab. Different methods exist to detect FR expression. Tissue sampling has limited clinical utility, mainly because it requires an invasive procedure. 99m Tc-etarfolatide, a 99m Tc-labeled folate conjugate, is in latephase trials in Europe and the United States. It allows noninvasive, whole-body imaging of the FR. This review focuses on this FRimaging agent and how it may be used to direct FR-targeted therapy.