Sentinel node navigation surgery (SNNS) using a radiolabeled compound consists of imaging with a camera and/or detection with a probe followed by injection. The lymph nodes can be clearly visualized and sentinel nodes can be detected in the operating room because of the high sensitivity of this method. This paper describes the characteristics of 99mTc-labeled compounds including conventional ones that are used for liver/spleen and lymph scintigraphy and new ones developed specifically for SNNS. Radiopharamaceuticals for SNNS should be selected based on the type of cancer, injection site, and detecting modality.