Suramin is a new experimental polyanionic compound that has shown evid
ence of antitumor activity in patients with hormone refractory prostat
e cancer. After a few years of Phase I and Phase II testing, much of t
he drug's toxicity pattern has been carefully characterized. Similarly
, pharmacologic studies have defined many of the drug's complex pharma
cologic properties to the extent that simple outpatient methods of dru
g administration can be easily accomplished. A pharmacologically deriv
ed, fixed outpatient schedule has been shown to be safe and effective
and is currently in active Phase III development in prostate cancer an
d will provide more definitive data regarding the role of suramin in t
he treatment of this disease. Despite these accomplishments, a number
of questions require further study, such as definition of pharmacodyna
mic correlations, effects on the hypothalamic-pituitary-adrenal and go
nadal axis, and the nature of its most common dose-limiting toxicity,
which is a syndrome of malaise and fatigue.