Phase I clinical study of three times a day oral administration of TAS-102 in patients with solid tumors.

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Overman MJ, Kopetz S, Varadhachary G, Fukushima M, Kuwata K, Mita A, Wolff RA, Hoff P, Xiong H, Abbruzzese JL

Phase I clinical study of three times a day oral administration of TAS-102 in patients with solid tumors.

Cancer Invest. 2008 Oct;26(8):794-9. doi: 10.1080/07357900802087242.

PubMed ID

18798063 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Trifluridine	DNA	Nucleotide	Humans	Yes	Other/unknown	Details
Trifluridine	Thymidylate synthase	Protein	Humans	Yes	Inhibitor	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Trifluridine	Thymidine phosphorylase	Protein	Humans	Unknown	Substrate	Details