title: A novel antimetabolite: TAS-102 for metastatic colorectal cancer.
abstract: TAS-102 is a new oral anti-tumor drug, composed of a thymidine-based nucleoside analog (trifluridine: FTD) and a thymidine phosphorylase inhibitor (tipiracil hydrochloride: TPI). TAS-102 has been shown to significantly improve overall survival and progression-free survival in patients with refractory metastatic colorectal cancer (mCRC) in placebo-controlled randomized phase II and III trials. The current review summarizes mechanisms of action, pharmacokinetics/dynamics and preclinical and clinical data of TAS-102 in colorectal cancer. TAS-102 is a new salvage-line treatment option for patients with mCRC. TAS-102 is well tolerated and has great potential in future clinical drug combination therapies.
authors.affiliation: a Department of Gastroenterological Surgery, Graduate School of Medical Sciences , Kumamoto University , Kumamoto , Japan.|b Division of Medical Oncology, Norris Comprehensive Cancer Center , University of Southern California , Los Angeles , CA , USA.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Miyamoto
authors.affiliation: b Division of Medical Oncology, Norris Comprehensive Cancer Center , University of Southern California , Los Angeles , CA , USA.
authors.forename: Heinz-Josef
authors.initials: HJ
authors.lastname: Lenz
authors.affiliation: a Department of Gastroenterological Surgery, Graduate School of Medical Sciences , Kumamoto University , Kumamoto , Japan.
authors.forename: Hideo
authors.initials: H
authors.lastname: Baba
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D015179:Colorectal Neoplasms / Q000188:drug therapy* / Q000473:pathology; D018572:Disease-Free Survival; D004338:Drug Combinations; D006801:Humans; D009362:Neoplasm Metastasis; D011759:Pyrrolidines; D016032:Randomized Controlled Trials as Topic; D015996:Survival Rate; D013941:Thymine; D014271:Trifluridine / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D014498:Uracil / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D004338:Drug Combinations; D011759:Pyrrolidines; C000613803:trifluridine tipiracil drug combination; D014498:Uracil; D013941:Thymine; D014271:Trifluridine
keywords: TAS-102; chemotherapy; intolerant; metastatic colorectal cancer; phase III; refractory; salvage line