It has been known for centuries that mushrooms from the Basidiomycota division possess pharmacological properties and exhibit good efficacy in treating a variety of human illnesses, including cancer, inflammatory, bacterial and viral diseases. Historically, hot-water-soluble extracts from Basidiomycota were used as medicine in the Far East, where knowledge and practice of Basidiomycota use primarily started. Today, approximately 200 species of Basidiomycota have been reported to possess therapeutic values including anticancer activity. However, most of these antitumor substances have not yet been defined. In this report, we will focus on the under-appreciated Basidiomycota culinary medicinal mushroom Coprinus comatus and review its pharmaceutical potential.