Viallet J, Stewart D, Shepherd F, Ayoub J, Cormier Y, DiPietro N, Steward W
Department of Oncology, McGill University, Montreal, Canada.
Lung Cancer. 1996 Nov;15(3):367-73. doi: 10.1016/0169-5002(95)00600-1.
Tallimustine binds to the minor groove of DNA where it alkylates the N3 position of adenine and may interfere with gene transcription. We conducted a phase II trial of Tallimustine given at a dose of 750 micrograms/m2 intravenously every 4 weeks in patients with small cell lung cancer progressing or relapsing following cisplatin or carboplatin-based chemotherapy. We treated 14 eligible patients with a performance status 0, 1 or 2, bi-dimensionally measurable disease and adequate end-organ function. The main toxicity was neutropenia with a median granulocyte count of 0.1 x 10(9) per liter (range 0-3.9) and four patients (27%) developing febrile neutropenia. In addition, most patients (93%) experienced lethargy. No objective responses were seen. A mixed response was seen in one patient and three others had stable disease for a median of 3.7 months. We conclude that Tallimustine is an ineffective agent in previously treated small cell lung cancer.
他利莫司汀与DNA的小沟结合，在腺嘌呤的N3位置进行烷基化反应，并可能干扰基因转录。我们开展了一项II期试验，对接受过基于顺铂或卡铂化疗后病情进展或复发的小细胞肺癌患者，每4周静脉注射一次他利莫司汀，剂量为750微克/平方米。我们治疗了14例符合条件的患者，其体能状态为0、1或2，疾病可进行二维测量，且终末器官功能良好。主要毒性为中性粒细胞减少，中性粒细胞计数中位数为每升0.1×10⁹（范围0 - 3.9），4例患者（27%）发生发热性中性粒细胞减少。此外，大多数患者（93%）出现嗜睡。未观察到客观缓解。1例患者出现混合反应，另外3例患者病情稳定，中位时间为3.7个月。我们得出结论，他利莫司汀在既往接受过治疗的小细胞肺癌中是一种无效的药物。
