TAS-102 in gastric cancer: Development and perspectives of a new biochemically modulated fluroropyrimidine drug combination. (August 2020)

• Record Type: Journal Article
• Authors: Roviello, Giandomenico; Fancelli, Sara; Gatta Michelet, Marta Rita; Aprile, Giuseppe; Nobili, Stefania; Roviello, Franco; Cianchi, Fabio; Mini, Enrico; Lavacchi, Daniele
• Is Part Of: Critical reviews in oncology/hematology. Volume 152(2020)
• Publication Date: 2020-08
• Subjects: AE adverse event -- AUC area under the concentration-time curve -- BSC best supportive care -- Cmax maximum plasma concentration -- CR complete response -- CrCl creatinine clearance -- DCR disease control rate -- DLT dose-limiting toxicity -- DPD dihydropyrimidine dehydrogenase -- EGFR epidermal growth factor receptor -- FDA Food and Drug Administration -- TFT trifluridine -- G grade -- HER2 human epidermal growth factor receptor 2 -- MMR mismatch repair -- MoAb monoclonal antibody -- MTD maximum tolerated dose -- Nal-IRI nanoliposomal irinotecan -- OS overall survival -- ORR overall response rate -- PD progressive disease -- PFS progression-free survival -- PR partial response -- SD stable disease -- TKI tyrosine kinase inhibitor -- Tmax times to maximum plasma concentration -- TPI tipiracil hydrochloride -- TP thymidine phosphorylase -- TS thymidylate synthase -- VEGFR-2 vascular endothelial growth factor receptor 2 -- 5-FU 5-fluorouracil; Gastric cancer -- Chemotherapy -- Third line -- TAS-102; Oncology -- Periodicals; Hematology -- Periodicals; 616.994
• DOI: 10.1016/j.critrevonc.2020.102987
• Languages: English
• ISSNs: 1040-8428

Abstract

Abstract: TAS-102 is a preconstituted drug combination comprising an oral fluoropyrimidine (trifluridine, TFT) and a potent inhibitor of thymidine phosphorylase (tipiracil hydrochloride, TPI). TFT/TPI has recently received Food and Drug Administration (FDA) approval also for the treatment of gastric cancer after at least two lines of chemotherapy. The approval was based on a large phase 3 trial (TAGS), in which TAS-102 showed a 31 % decrease in the risk of death compared with placebo. Here, we review the pharmacological properties, clinical development and potential future directions of TAS-102 in gastric cancer.