nsc-366140 and Rectal-Neoplasms

To perform a phase II trial of pyrazoloacridine (PZA), a novel DNA intercalator, in patients with metastatic colorectal carcinoma and no previous therapy.. PZA was administered at a dose of 750 mg/m2 intravenously over 3 h every 21 days. Pharmacokinetic studies to determine PZA plasma concentrations were performed.. No responses were seen in 14 response-evaluable patients. Patients received a median of two cycles of PZA (range 1-6). Toxicity included neutropenia and neurologic side-effects, which were > or = grade III in 73% and 14%, respectively. High plasma concentrations of PZA (Cmax) correlated with low neutrophil counts (P = 0.04).. PZA is inactive at this dose and schedule in colorectal cancer, and produces moderately severe toxicity.

Topics: Acridines; Adult; Aged; Antineoplastic Agents; Colonic Neoplasms; Female; Humans; Intercalating Agents; Male; Middle Aged; Neoplasm Metastasis; Nervous System Diseases; Neutropenia; Pyrazoles; Rectal Neoplasms