Bramwell V H, Eisenhauer E A, Blackstein M, Boos G, Knowling M, Jolivet J, Bogues W
London Regional Cancer Centre, Ontario, Canada.
Ann Oncol. 1995 Oct;6(8):847-9. doi: 10.1093/oxfordjournals.annonc.a059329.
New drugs are needed for treatment of unresectable or metastatic soft tissue sarcoma. Topotecan, a semisynthetic derivative of the alkaloid, camptothecin, exerts its cytotoxic effect through inhibition of topoisomerase I.
Thirty-two adult patients with locally advanced or metastatic soft tissue sarcoma entered this phase II study of topotecan, administered at 1.5 mg/m2/day IV x 5 days every 3 weeks. All had measurable disease and none had received previous chemotherapy.
There were 3 partial responses (10.3%; 95% CI 2.2-27.4%) in 29 evaluable patients. Grade 3 or 4 neutropenia occurred in 25 patients, and there was a 17% incidence of infection/neutropenic fever leading to one toxic death.
Topotecan, in this dose and schedule, has low activity in adult soft tissue sarcoma.
治疗无法切除或转移性软组织肉瘤需要新的药物。拓扑替康是生物碱喜树碱的半合成衍生物，通过抑制拓扑异构酶I发挥其细胞毒性作用。
32例局部晚期或转移性软组织肉瘤成年患者进入了这项拓扑替康的II期研究，每3周静脉注射1.5mg/m²/天，共5天。所有患者均有可测量的疾病，且之前均未接受过化疗。
29例可评估患者中有3例部分缓解（10.3%；95%置信区间2.2-27.4%）。25例患者出现3级或4级中性粒细胞减少，感染/中性粒细胞减少性发热的发生率为17%，导致1例毒性死亡。
按此剂量和给药方案，拓扑替康在成人软组织肉瘤中的活性较低。
