The pathogenic wood-decaying fungus Irpex lacteus belongs to Basidiomycota. This mushroom causes a white rot and occurs on numerous hardwood trees, growing on dead branches of either dead or living trees as well as on dead standing trunks or fallen trunks and branches. The geographic distribution of I. lacteus is restricted to the Northern Hemisphere, including Europe, Asia, North Africa, and is widely distributed in North America. I. lacteus is also reported as an endophyte and also reported to cause infections in humans. I. lacteus is one of the main sources of a wide range of bioactive class of compounds such as sterol, terpenoid, sesquiterpene, tremulane, glucoside, furan, polyketide, indole, naphthalene, lactone and others. Many of the metabolites of I. lacteus possess antimicrobial, anticancer, anti-inflammatory, anti-Alzheimer's, antifeedant, and anti-quorum sensing activities. This chapter uncovers the bioactive metabolites of different species of I. lacteus with their source of origin and biological activities.