Fungi cause various severe diseases of food such as rice blast, which led to the infamous Bengal famine in 1943. These are usually called food spoilers, as they damage raw and cooked food as well as grains. But fungi are also useful because of the production of antibiotics such as cephalosporin, penicillin, cyclosporine, and statins. The beneficial effects include the production of numerous enzymes (lipase, ligninolytic enzymes, cellulase), pigments (anthraquinone, betalains), and alkaloids (ergot). Other benefits include cheese making; nematode control; aromas or flavors; edible fungi; a source of potassium, selenium, niacin, riboflavin, vitamin D, and proteins; and the prevention or treatment of various diseases including cancer, hypertension, Alzheimer’s, viral diseases, Parkinson’s, and diseases caused by various microbes as well as fungi. The vast bioactivities of fungi are because of the production of metabolites, which possess different structural backbones such as aromatic and aliphatic hydrocarbons, esters, ketones, organic acids, alcohols, aldehydes and mono-, sesqui-, and di-terpenes. This chapter provides an elaborate view of the biomedical applications of fungal biometabolites and prospects for their future development. © 2021 Elsevier B.V. All rights reserved.