Phase I Clinical Study of Three Times a Day Oral Administration of TAS-102 in Patients with Solid Tumors

作者：Michael James Overman, Scott Kopetz, Gauri Varadhachary, Masakazu Fukushima, Keizo Kuwata, Akira Mita, Robert A. Wolff, Paulo M. Hoff, Henry Q. Xiong, James L. Abbruzzese · 发表于：Cancer Investigation · 年份：2008 · DOI：10.1080/07357900802087242 · 被引用次数：64 · 研究领域：Colorectal Cancer Treatments and Studies、Chronic Lymphocytic Leukemia Research、Biochemical and Molecular Research

TAS-102 is a novel formulation of the fluorinated pyrimidine analogue trifluorothymidine (FTD) with an inhibitor of thymidine phosphorylase. The purpose of this study was to determine the MTD and DLT for TAS-102 administered three times a day on days 1-5 and 8-12 every 4 weeks. Fifteen patients were enrolled with two patients experiencing dose-limiting fatigue and granulocytopenia at the first dose level (80 mg/m2/day). Granulocytopenia was the primary toxicity: 7 patients experienced grade 3 or 4 granulocytopenia with the first course. No responses were noted, but nine patients demonstrated prolonged stable disease in this heavily pretreated 5-FU refractory population.