Sosman J A, Flaherty L E, Liu P Y, Fletcher W, Thompson J A, Hantel A, Sondak V
Loyola University Stritch School of Medicine, Maywood IL, USA.
Invest New Drugs. 1995;13(1):83-7. doi: 10.1007/BF02614226.
Piroxantrone is one of the anthrapyrazoles developed in an effort to combine the broad antitumor activity of the anthracyclines with decreased myocardial toxicity. It has shown activity in metastatic melanoma during phase I trials. The Southwest Oncology Group (SWOG) conducted a phase II trial in disseminated malignant melanoma with piroxantrone administered at 150 mg/m2 intravenously over 1 h every 21 days, based upon the phase I experience. Forty-six eligible patients were registered to the trial and 44 were evaluable for response. Two partial responses, Wayne of 6 and 9 months duration were observed for an overall response rate of 5% (95% confidence interval 1%-15%). Thirty-six of 46 eligible patients have died with an estimated median survival of 5 months (95% confidence interval 3-8 months). Toxicities were tolerable with granulocytopenia being the predominant toxicity. Based upon the observed response rate, it is concluded that piroxantrone administered at this dose and schedule has detectable but minimal activity, and does not warrant further investigation in this disease.
吡罗昔酮是为了将蒽环类药物的广泛抗肿瘤活性与降低的心肌毒性相结合而研发的蒽吡唑类药物之一。在I期试验中，它已显示出对转移性黑色素瘤的活性。西南肿瘤协作组（SWOG）根据I期试验经验，开展了一项II期试验，对播散性恶性黑色素瘤患者每21天静脉注射吡罗昔酮150 mg/m²，持续1小时。46例符合条件的患者登记参加了该试验，44例可评估疗效。观察到2例部分缓解，缓解期分别为6个月和9个月，总缓解率为5%（95%置信区间1%-15%）。46例符合条件的患者中有36例死亡，估计中位生存期为5个月（95%置信区间3-8个月）。毒性是可耐受的，粒细胞减少是主要毒性。基于观察到的缓解率，得出结论：按此剂量和方案给药的吡罗昔酮具有可检测到的但极小的活性，不支持在该疾病中进行进一步研究。
