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Trifluridine/tipiracil in metastatic colorectal cancer: a guide to its use

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Abstract

Trifluridine/tipiracil (Lonsurf®; also known as TAS-102), an oral antimetabolite agent, is a welcome addition to the options available to treat metastatic colorectal cancer in patients who are refractory to, or are not considered candidates for, currently available therapies. This novel fixed-dose formulation combines trifluridine, which inhibits cell proliferation after being incorporated into DNA via phosphorylation, with tipiracil, which increases systemic exposure to trifluridine by potently inhibiting thymidine phosphorylase. In clinical trials, the addition of trifluridine/tipiracil (35 mg/m2 twice daily on days 1–5 and 8–12 of each 28-day cycle) to best supportive care significantly improved overall survival, progression-free survival and disease control relative to placebo. Adverse events associated with trifluridine/tipiracil can generally be managed with dose modification and/or supportive measures.

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Acknowledgements

This manuscript is updated from Drugs 2016;76(14):1392–1402 [37] and was reviewed by: B. Royer, Department of Pharmacology and Toxicology, Centre Hospitalier Régional Universitaire de Besançon, Besançon, France; S.V. Sakpal, Department of Surgery, Medical College of Wisconsin, Milwaukee, WI, USA; R.G. Watson, Alexion Pharmaceuticals, Inc., Lexington, MA, USA; K.-H. Yeh, Graduate Institute of Oncology, National Taiwan University College of Medicine, Taipei, Taiwan; A. Zanboni, Medical Oncology Department, Fondazione Poliambulanza, Brescia, Italy. During the peer review process, the manufacturer of trifluridine/tipiracil was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand

    Katherine A. Lyseng-Williamson, Celeste B. Burness & Sean T. Duggan

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  1. Katherine A. Lyseng-Williamson
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Correspondence to Katherine A. Lyseng-Williamson.

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The preparation of this review was not supported by any external funding.

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KA. Lyseng-Williamson, C.B. Burness and S.T. Duggan are/were salaried employees of Adis/Springer, are responsible for the article content and declare no relevant conflicts of interest.

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Lyseng-Williamson, K.A., Burness, C.B. & Duggan, S.T. Trifluridine/tipiracil in metastatic colorectal cancer: a guide to its use. Drugs Ther Perspect 33, 110–118 (2017). https://doi.org/10.1007/s40267-017-0385-y

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