The hydroxynaphthoquinone 566C80 represents a new class of drugs with activity against Pneumocystis carinii, the cause of a life-threatening pneumonitis in patients with the acquired immunodeficiency syndrome (AIDS) as well as in other immunocompromised hosts. Results of animal studies have shown potent activity in the treatment and prevention of P. carinii pneumonitis. A phase I clinical trial in men infected with the human immunodeficiency virus (HIV) showed safety in doses ranging from 100 to 3000 mg per day and linear increases in plasma concentrations with doses of up to 750 mg per day. In an open phase I/II trial, 27 of 34 patients (79%) with AIDS were treated successfully for mild and moderate P. carinii pneumonia. Results of additional studies will be forthcoming soon and 566C80 has recently received treatment approval as an investigational new drug by the Food and Drug Administration (FDA). Although promising as a new anti-P. carinii drug, 566C80 can not yet be designated a therapeutic priority.