Abstract: With the development of medicinal and organic chemistry, more and more classical and non-classical bioisosteres are used in the design of novel drugs.Bicyclo1.1.1 pentane (BCP), as a bioisostere of benzene, t-butyl and alkyne moieties,has recently received extensive attention from medicinal and organic chemists.This paper briefly reviews its application in drug design to provide reference for drug discovery researchers.