Zalupski M M, Shields A F, Philip P A, Kraut M, LoRusso P, Heilbrun L K, Vaitkevicius V
Division of Hematology and Oncology, Karmanos Cancer Institute, Wayne State University, Detroit, MI, USA.
Invest New Drugs. 1998;16(1):93-6. doi: 10.1023/a:1006087114621.
Pyrazoloacridine (PZA) is an acridine derivative selected for clinical development because of broad pre-clinical 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 pancreatic cancer was conducted.
PZA was administered at a dose of 750 mg/m2 intravenously over 3 hours every 21 days. Seventeen patients were treated receiving a total of 46 courses of PZA.
Of the 15 patients evaluable for response, no responses were observed (0% response rate, 95% confidence interval 0-22%). Major toxicities directly attributable to PZA included moderate neutropenia and mild neurotoxicity.
PZA at this dose and schedule of administration was inactive in patients with pancreatic carcinoma.
吡唑并吖啶（PZA）是一种吖啶衍生物，因其广泛的临床前抗肿瘤活性和实体瘤选择性而被选用于临床开发。PZA的I期评估已证明其毒性可预测并显示出临床疗效。对先前未经治疗的晚期胰腺癌患者进行了II期试验。
PZA以750mg/m²的剂量每21天静脉输注3小时。17例患者接受治疗，共接受46个疗程的PZA。
在15例可评估反应的患者中，未观察到反应（缓解率0%，95%置信区间0-22%）。直接归因于PZA的主要毒性包括中度中性粒细胞减少和轻度神经毒性。
该剂量和给药方案的PZA对胰腺癌患者无活性。
