Phase II study of pyrazoloacridine in patients with advanced colorectal carcinoma

Cancer Chemother Pharmacol. 1997;40(3):225-7. doi: 10.1007/s002800050650.


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.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase II
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acridines / adverse effects
  • Acridines / therapeutic use*
  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma / drug therapy*
  • Carcinoma / secondary
  • Colorectal Neoplasms / drug therapy*
  • Drug Administration Schedule
  • Female
  • Humans
  • Leukopenia / chemically induced
  • Male
  • Middle Aged
  • Pyrazoles / adverse effects
  • Pyrazoles / therapeutic use*
  • Safety
  • Treatment Outcome


  • Acridines
  • Antineoplastic Agents
  • Pyrazoles