第一阶段实验小说的哺乳动物雷帕霉素靶抑制剂deforolimus (AP23573;mk - 8669)进行静脉注射每日5天每两周的晚期恶性肿瘤患者。

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Mita Mita MM, AC,楚QS Rowinsky EK,羁绊GJ, Goldston M, Patnaik,马修斯L,卡特举广告,Mays T,诺尔斯H,里维拉VM, Kreisberg J, Bedrosian CL, Tolcher哦

第一阶段实验小说的哺乳动物雷帕霉素靶抑制剂deforolimus (AP23573;mk - 8669)进行静脉注射每日5天每两周的晚期恶性肿瘤患者。

肿瘤防治杂志。2008年1月20日,26 (3):361 - 7。doi: 10.1200 / JCO.2007.12.0345。

PubMed ID

18202410 (在PubMed

]

文摘

目的:这个阶段我审判确定安全,耐受性,药物动力学和药效学deforolimus(以前称为AP23573;mk - 8669), nonprodrug雷帕霉素模拟,在先进的固体恶性肿瘤患者。患者和方法:患者治疗使用加速滴定法设计与序贯平剂deforolimus升级管理30分钟静脉输液连续5天每天一次每2周(QDx5)在28天为一个周期。安全、药代动力学、药效学和肿瘤反应进行评估。结果:32例收到至少一个剂量的deforolimus (3 - 28 mg / d)。三个dose-limiting毒性三年级口腔溃疡的事件被报道。最大耐受剂量(MTD)为18.75 mg / d。常见的治疗相关的不良事件包括可逆的口腔溃疡和皮疹。遗传损伤间隙增加剂量。药效学分析表明哺乳动物雷帕霉素靶抑制剂量水平。 Four patients (one each with non-small-cell lung cancer, mixed mullerian tumor [carcinosarcoma], renal cell carcinoma, and Ewing sarcoma) experienced confirmed partial responses, and three additional patients had minor tumor regressions. CONCLUSION: The MTD of this phase I trial using an accelerated titration design was determined to be 18.75 mg/d. Deforolimus was well tolerated and showed encouraging antitumor activity across a broad range of malignancies when administered intravenously on the QDx5 schedule. On the basis of these overall results, a dose of 12.5 mg/d is being evaluated in phase II trials.

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药物

Ridaforolimus