Lynch G, Kemeny N, Casper E
Am J Clin Oncol. 1982 Oct;5(5):541-3.
Twenty-three patients with advanced colorectal carcinoma, previously treated with chemotherapy, were entered in a phase II trial of DON (6-Diazo-5-Oxo-L-Norleucine), an antagonist of L-glutamine. One of 14 adequately treated patients had a partial response of 6 weeks duration. The dose-limiting toxicity was nausea and vomiting; 48% of patients originally entered on the study withdrew because of vomiting. Myelosuppression was minimal, with only mild thrombocytopenia noted. The dose and schedule used in this study were beyond the maximally tolerated dose for many patients; future phase II studies of DON will be difficult to complete unless schedules and doses are found which result in less nausea and vomiting.
23例先前接受过化疗的晚期结直肠癌患者进入了一项关于L-谷氨酰胺拮抗剂DON（6-重氮-5-氧代-L-正亮氨酸）的II期试验。14例接受充分治疗的患者中有1例出现了持续6周的部分缓解。剂量限制性毒性为恶心和呕吐；最初参与该研究的患者中有48%因呕吐而退出。骨髓抑制轻微，仅观察到轻度血小板减少。本研究中使用的剂量和给药方案对许多患者来说超出了最大耐受剂量；除非找到能减少恶心和呕吐的给药方案和剂量，否则未来DON的II期研究将难以完成。
