To provide a comprehensive review of intravesical treatment options for non-muscle-invasive bladder cancer, we performed a search of the PubMed database for articles between 1980 and 2006 that reported on intravesical agents for treating this disease. Data were compiled and analyzed, emphasizing findings from large multicenter trials, studies providing reproducible results, data that could be confirmed by cross-referencing the literature, and phase I or II studies for pertinent novel agents. A critical analysis of evidence shows that: 1) treatment with Bacillus Calmette-Guérin (BCG), including a maintenance schedule (with or without interferon-alpha), is the most effective therapy for limiting recurrence, is the only therapy that reduces the incidence of progression, and overall is superior to chemotherapy; 2) mitomycin C, gemcitabine, anthracyclines, and thiotepa provide similar benefits for preventing recurrence in patients with minimal effect on progression; and 3) using chemotherapeutic agents immediately after transurethral resection (when use of BCG is contraindicated because of the risk for systemic absorption) reduces the recurrence rate by up to 50% and seems to be the ideal method of chemotherapy. Although various clinical factors dictate which agent is most appropriate for an individual patient, the current literature supports a single perioperative dose of intravesical mitomycin C followed, in appropriate cases, by induction and maintenance therapy with intravesical BCG.