Over the last 10 years, trilostane, a competitive inhibitor of steroid synthesis, is being widely used for the treatment of canine hyperadrenocorticism. Trilostane causes a significant but reversible decrease in cortisol production and a concomitant improvement in clinical signs in most dogs with this common condition. Side effects, though infrequent, can be serious: dogs treated with this drug require regular monitoring. This review summarizes current knowledge of the use of this drug with particular emphasis on its efficacy, safety, adverse reactions, and effects on endocrine parameters. Brief mention is made of its other uses in dogs and other species.