人参三醇-3,6-二琥珀酸酯钠I期临床耐受性研究  

A phase I trial for evaluating the tolerance of disodium panaxatriol 3,6-succinate

作　　者：孙燕[1] 王华庆[1] 阎昭[1] 宋拯[1] 张会来[1] 刘贤明[1] 李维[1] 

机构地区：[1]天津医科大学附属肿瘤医院内一科,天津市肿瘤防治重点实验室,天津300060

出　　处：《中国新药杂志》2008年第3期241-243,共3页Chinese Journal of New Drugs

摘　　要：目的：评价抗肿瘤新药人参三醇-3,6-二琥珀酸酯钠的人体安全性,观察毒副反应并确定人体安全耐受剂量。方法：采用改良的Fibonacci方法进行剂量递增。选择30例健康受试者和9例肿瘤患者。21例健康受试者进行7个剂量组单次给药试验（20,40,70,100,140,190,240 mg）;9例健康受试者进行3个剂量组（70,100,140 mg）连续给药30 d的试验,9例肿瘤患者进行100 mg连续给药30 d试验。结果：21例健康受试者单次给药试验未观察到不良反应;9例健康受试者和9例肿瘤患者连续给药30 d试验主要的不良反应为乏力、体内热感、咽痛和大便干燥等。结论：人参三醇-3,6-二琥珀酸酯钠毒性反应轻,患者耐受性好。推荐Ⅱ期临床使用剂量及方法为70-100 mg·d^-1,静脉滴注,连用30 d。Objective：To evaluate the safety of a new anticancer drug, disodium panaxatriol 3,6-succinate, in human by determining its maximally tolerated dose. Methods：Dose escalation was performed by modified Fibonacci sequence in 30 healthy volunteers and 9 cancer patients. Single doses （20, 40, 70, 100, 140, 190, 240 mg） of disodium panaxatriol 3,6-succinate were intravenously infused in 21 healthy volunteers once daily until to MTD. Multiple doses were successively given for 30 d in 9 healthy volunteers （70, 100, 140 mg） and 9 cancer patients （100 mg）. Results： No adverse reactions were observed after single doses in 21 healthy volunteers. The major adverse reaction after 30 d multiple doses included hypodynamia, pharyngalgia, dryness-heat and sedes drying in 9 healthy volunteers and 9 cancer patients. Conclusion： The toxicity of disodium panaxatriol 3,6-succinate is mild, and subjects can be well tolerated. The recommended dose regimen for phase Ⅱtrial is 70 - 100 mg·d^-1 , intravenous infusion, once daily for 30 d.

关 键 词：人参三醇-3 6-二琥珀酸酯钠 Ⅰ期临床试验 耐受性 

分 类 号：R969.4[医药卫生—药理学] R979.1[医药卫生—药学]