Abstract Geniposide, a water‐soluble iridoid glycoside, has multiple pharmacological activities such as hypoglycemic, anticancer, anti‐inflammatory, neuroprotective, cardiac protection, and so on. However, geniposide has the disadvantages of poor fat solubility, short half‐life, and low bioavailability, which makes it unable to play a better role in clinical practice. At present, there is no systematic report on the biological activities and structural modification of geniposide and its derivatives at home and abroad. Through extensive literature research, structural modification and biological activities of geniposide and its derivatives were reported in this paper, providing a research basis for the development of new geniposide drugs in the future.