Purpose: Pyrazoloacridine (PZA) is an acridine derivative selected for clinical development because of broad preclinical antitumor activity and solid tumor selectivity. Phase I evaluations with PZA have demonstrated predictable toxicity and suggested clinical efficacy. A phase II trial in patients with previously untreated advanced colorectal cancer was conducted.
Methods: PZA was administered at a dose of 750 mg/m2 intravenously over 3 h every 21 days to patients who received a total of 31 courses of PZA.
Results: In 15 patients evaluable for response, no responses were observed (0% response rate, 95% confidence interval 0-22%). Toxicity to PZA consisted of myelosuppression and neurotoxicity that was treatment-limiting in several instances.
Conclusion: PZA at this dose and schedule of administration is inactive in patients with colorectal cancer.