Objectives: To evaluate the efficacy of non-steroidal anti-androgen mo
notherapy in the treatment of advanced prostate cancer. Methods: The p
ertinent literature regarding the use of nilutamide, flutamide, and bi
calutamide as monotherapy in the treatment of prostate cancer has been
reviewed. Results: The clinical utility of non-steroidal antiandrogen
monotherapy is currently under investigation. As with other endocrine
therapies, this approach appears to provide effective palliation of s
ymptoms, but offers certain quality-of-life benefits, including preser
vation of libido and sexual potency, issues which may be important in
certain patients, particularly younger men. Available data indicate th
at flutamide may be as effective as orchidectomy in terms of prolongin
g progression-free survival in selected patients. Nilutamide has been
less extensively investigated, but the clinical utility of this agent,
except for use in combined therapy, would appear to be somewhat limit
ed by a high incidence of drug-related side effects. Bicalutamide, how
ever, is well tolerated as monotherapy and appears to be as effective
as castration in patients with locally advanced non-metastatic disease
. In metastatic disease, the improved subjective response and quality
of life gains with bicalutamide may outweigh the slightly inferior sur
vival. Conclusion: These promising preliminary findings, a number of i
ssues remain to be determined before non-steroidal antiandrogen monoth
erapy can be considered to be routine clinical practice. These include
optimum indication and dosage, long-term clinical efficacy and tolera
bility, and response to second-line therapy.