Phase II trial of pyrazoloacridine as second-line therapy for patients with unresectable or metastatic transitional cell carcinoma

Invest New Drugs. 2000 Aug;18(3):247-51. doi: 10.1023/a:1006477823378.


Purpose: A phase II trial of pyrazoloacridine (PZA) was conducted to assess its activity and toxicity in patients with advanced transitional cell carcinoma (TCC) refractory to or progressing after one prior cisplatin-, carboplatin- or paclitaxel- based regimen.

Patients and methods: PZA at a dose of 750 mg/m2 was administered to 14 patients as a three-hour intravenous infusion on day 1 every 21 days. Premedication consisted of lorazepam 0.5-1.0 mg prior to each cycle to alleviate central nervous system toxicity. Reduction of subsequent doses was made for hematologic or central nervous system toxicity.

Results: Among fourteen patients evaluable for response, no responses were observed (0% response rate; 95% confidence interval 0% to 23%). The median duration of survival for all patients was 9 months with a median follow-up of 8.5 months. Toxicity to PZA included grade 3 or 4 neutropenia in 8/14 (57%) and grade 3 or 4 thrombocytopenia in 2/14 (14%). Non-hematologic toxicity was mild.

Conclusions: PZA at this dose and schedule does not have significant single-agent activity in patients with TCC who have failed one prior regimen.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase II

MeSH terms

  • Acridines / adverse effects
  • Acridines / therapeutic use*
  • Adult
  • Aged
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Transitional Cell / drug therapy*
  • Carcinoma, Transitional Cell / mortality
  • Carcinoma, Transitional Cell / secondary
  • Female
  • Humans
  • Male
  • Middle Aged
  • Pyrazoles / adverse effects
  • Pyrazoles / therapeutic use*
  • Urinary Bladder Neoplasms / drug therapy*
  • Urinary Bladder Neoplasms / mortality


  • Acridines
  • Antineoplastic Agents
  • Pyrazoles
  • NSC 366140