TAS-102 – a new option in the treatment of patients with advanced colorectal cancer after failure or intolerance to other therapies Review article
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Published:
Mar 31, 2020
Keywords:
metastatic colorectal cancer, refractory, fluoropyrimidines, TAS-102
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Abstract
Colorectal cancer is the second cause of death from malignant cancer, following lung cancer. Approximately 35–45% of patients with colorectal cancer will develop distant metastases over time. Palliative systemic treatment remains the standard for non-operative distant metastases. TAS-102 is a novel orally administered antineoplasmatic thymidine-based nucleoside analog which represents an approved option for the treatment of advanced metastatic colorectal cancer in patients who are refractory, or are not considered canditates for, currently available therapies.
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How to Cite
1.
Skalij P, Tokajuk P, Wojtukiewicz MZ. TAS-102 – a new option in the treatment of patients with advanced colorectal cancer after failure or intolerance to other therapies. OncoReview [Internet]. 2020Mar.31 [cited 2024Nov.22];10(1(37):8-14. Available from: https://journalsmededu.pl/index.php/OncoReview/article/view/1076
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Section
CARDIO-ONCOLOGY
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Copyright: © Medical Education sp. z o.o. This is an Open Access article distributed under the terms of the Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). License (https://creativecommons.org/licenses/by-nc/4.0/), allowing third parties to copy and redistribute the material in any medium or format and to remix, transform, and build upon the material, provided the original work is properly cited and states its license.
Address reprint requests to: Medical Education, Marcin Kuźma (marcin.kuzma@mededu.pl)
References
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9. Wyatt MD, Wilson DM 3rd. Participation of DNA repair in the response to 5-fluorouracil. Cell Mol Life Sci. 2009; 66: 788-99.
10. Glazer RI, Lloyd LS. Association of cell lethality with incorporation of 5-fluorouracil and 5-fluorouridine into nuclear RNA in human colon carcinoma cells in culture. Mol Pharmacol. 1982; 21: 468-73.
11. Aschele C, Sobrero A, Faderan MA et al. Novel mechanism(s) of resistance to 5-fluorouracil in human colon cancer (HCT-8) sublines following exposure to two different clinically relevant dose schedules. Cancer Res. 1992; 52: 1855-64.
12. Wilson PM, Danenberg PV, Johnston PG et al. Standing the test of time: targeting thymidylate biosynthesis in cancer therapy. Nat Rev Clin Oncol. 2014; 11: 282-98.
13. Lenz HJ, Stintzing S, Loupakis F. TAS-102, a novel antitumor agent: a review of the mechanism of action. Cancer Treat Rev. 2015; 41: 777-83.
14. Dexter DL, Wolberg WH, Ansfield FJ et al. The clinical pharmacology of 5-trifluoromethyl-2’-deoxyuridine. Cancer Res. 1972; 32: 247-53.
15. Temmink OH, Emura T, de Bruin M et al. Therapeutic potential of the dual-targeted TAS-102 formulation in the treatment of gastrointestinal malignancies. Cancer Sci. 2007; 98: 779-89.
16. Eckstein JW, Foster PG, Finer-Moore J et al. Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2’-deoxyuridine 5’-monophosphate. Biochemistry. 1994; 33: 15086-94.
17. Temmink OH, Comijn EM, Fukushima M et al. Intracellular thymidylate synthase inhibition by trifluorothymidine in FM3A cells. Nucleosides Nucleotides Nucleic Acids. 2004; 23: 1491-4.
18. Heidelberger C, Boohar J, Kampschroer B. Fluorinated pyrimidines. XXIV. In vivo metabolism of 5-trifluoromethyluracil-2-C-14 and 5-trifluoromethyl-2’-deoxyuridine-2-C-14. Cancer Res. 1965; 25: 377-81.
19. Oguchi K, Sakamoto K, Kazuno H et al. TAS-102 treatment results in high trifluridine incorporation into DNA with pyrimidine metabolic pathway markedly up-regulated in cancer. Eur J Cancer. 2014; 50(suppl. 6): Abstract 27.
20. Suzuki N, Emura T, Fukushima M. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011; 39: 263-70.
21. Suzuki N, Emura T, Fukushima M. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011; 39: 263-70.
22. Moghaddam A, Zhang HT, Fan TP et al. Thymidine phosphorylase is angiogenic and promotes tumour growth. Proc Natl Acad Sci USA. 1995; 92: 998-1002.
23. Hotchkiss KA, Ashton AW, Schwartz EL. Thymidine phosphorylase and 2-deoxyribose stimulate human endothelial cell migration by specific activation of the integrins alpha 5 beta 1 and alpha V beta 3. J Biol Chem. 2003; 278: 19272-9.
24. Takao S, Akiyama SI, Nakajo A et al. Suppression of metastasis by thymidine phosphorylase inhibitor. Cancer Res. 2000; 60: 5345-8.
25. Matsushita S, Nitanda T, Furukawa T et al. The effect of a thymidine phosphorylase inhibitor on angiogenesis and apoptosis in tumors. Cancer Res. 1999; 59: 1911-6.
26. Dexter DL, Wolberg WH, Ansfield FJ et al. The clinical pharmacology of 5-trifluoromethyl-2’-deoxyuridine. Cancer Res. 1972; 32: 247-53.
27. Emura T, Suzuki N, Fujioka A et al. Potentiation of the antitumor activity of alpha, alpha, alpha-trifluorothymidine by the co-administration of an inhibitor of thymidine phosphorylase at a suitable molar ratio in vivo. Int J Oncol. 2005; 27: 449-55.
28. Fukushima M, Suzuki N, Emura T et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of a ntitumor 2’-deoxyribonucleosides. Biochem Pharmacol. 2000; 59: 1227-36.
29. Yoshino T, Mizunuma N, Yamazaki K et al. TAS-102 monotherapy for pretreated metastatic colorectal cancer: a double-blind, randomised, placebo-controlled Phase 2 trial. Lancet Oncol. 2012; 13(10): 993-1001.
30. Mayer RJ, Van Cutsem E, Falcone A et al. Randomized trial of TAS-102 for refractory metastatic colorectal cancer. N Engl J Med. 2015; 372(20): 1909-19.
31. Van Cutsem E, Mayer RJ, Laurent S et al. The subgroups of the Phase III RECOURSE trial of trifluridine/tipiracil (TAS-102) versus placebo with best supportive care in patients with metastatic colorectal cancer. Eur J Cancer. 2018; 90: 63-72.
32. Xu J, Kim TW, Shen L et al. Results of a randomized, double-blind, placebo-controlled, Phase III trial of trifluridine/tipiracil (TAS-102) monotherapy in Asian patients With previously treated metastatic colorectal cancer: the TERRA study. J Clin Oncol. 2018; 36(4): 350-8.
33. Kwakman JJM, Vink G, Vestjens JH et al. Feasibility and effectiveness of trifluridine/tipiracil in metastatic colorectal cancer: real-life data from The Netherlands. Int J Clin Oncol. 2018; 23:482-9.
34. Cremolini C, Rossini D, Martinelli E et al. Trifluridine/tipiracil (TAS-102) in refractory metastatic colorectal cancer: a multicenter register in the frame of the Italian compassionate use program. Oncologist. 2018; 23:1178-87.
35. Pietrantonio F, Miceli R, Rimassa L et al. Estimating 12-week death probability in patients with refractory metastatic colorectal cancer: The Colon Life nomogram. Ann Oncol. 2017; 28: 555-61.
36. Cremolini C, Rossini D, Martinelli E et al. Trifluridine/tipiracil (TAS-102) in refractory metastatic colorectal cancer: a multicenter register in the frame of the Italian compassionate use program. Oncologist. 2018; 23: 1178-87.
2. Cromheecke M, de Jong KP, Hoekstra HJ. Current treatment for colorectal cancer metastatic to the liver. Eur J Surg Oncol. 1999; 25: 451-63.
3. Hochster HS, Grothey A, Hart L et al. Improved time to treatment failure with an intermittent oxaliplatin strategy: Results of concept. Ann Oncol. 2014; 25: 1172-8.
4. Yoshino T, Arnold D, Taniguchi H et al. Pan-Asian adapted ESMO consensus guidelines for the management of patients with metastatic colorectal cancer: A JSMO-ESMO initiative endorsed by CSCO, KACO, MOS, SSO and TOS. Ann Oncol. 2018; 29: 44-70.
5. Vogel A, Hofheinz RD, Kubicka S et al. Treatment decisions in metastatic colorectal cancer – Beyond first and second line combination therapies. Cancer Treat Rev. 2017; 59: 54-60.
6. Wilson PM, Danenberg PV, Johnston PG et al. Standing the test of time: targeting thymidylate biosynthesis in cancer therapy. Nat Rev Clin Oncol. 2014; 11: 282-98.
7. Rahman L, Voeller D, Rahman M et al. Thymidylate synthase as an oncogene: a novel role for an essential DNA synthesis enzyme. Cancer Cell. 2004; 5: 341-51.
8. Longley DB, Harkin DP, Johnston PG. 5-fluorouracil: mechanisms of action and clinical strategies. Nat Rev Cancer. 2003; 3: 330-8.
9. Wyatt MD, Wilson DM 3rd. Participation of DNA repair in the response to 5-fluorouracil. Cell Mol Life Sci. 2009; 66: 788-99.
10. Glazer RI, Lloyd LS. Association of cell lethality with incorporation of 5-fluorouracil and 5-fluorouridine into nuclear RNA in human colon carcinoma cells in culture. Mol Pharmacol. 1982; 21: 468-73.
11. Aschele C, Sobrero A, Faderan MA et al. Novel mechanism(s) of resistance to 5-fluorouracil in human colon cancer (HCT-8) sublines following exposure to two different clinically relevant dose schedules. Cancer Res. 1992; 52: 1855-64.
12. Wilson PM, Danenberg PV, Johnston PG et al. Standing the test of time: targeting thymidylate biosynthesis in cancer therapy. Nat Rev Clin Oncol. 2014; 11: 282-98.
13. Lenz HJ, Stintzing S, Loupakis F. TAS-102, a novel antitumor agent: a review of the mechanism of action. Cancer Treat Rev. 2015; 41: 777-83.
14. Dexter DL, Wolberg WH, Ansfield FJ et al. The clinical pharmacology of 5-trifluoromethyl-2’-deoxyuridine. Cancer Res. 1972; 32: 247-53.
15. Temmink OH, Emura T, de Bruin M et al. Therapeutic potential of the dual-targeted TAS-102 formulation in the treatment of gastrointestinal malignancies. Cancer Sci. 2007; 98: 779-89.
16. Eckstein JW, Foster PG, Finer-Moore J et al. Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2’-deoxyuridine 5’-monophosphate. Biochemistry. 1994; 33: 15086-94.
17. Temmink OH, Comijn EM, Fukushima M et al. Intracellular thymidylate synthase inhibition by trifluorothymidine in FM3A cells. Nucleosides Nucleotides Nucleic Acids. 2004; 23: 1491-4.
18. Heidelberger C, Boohar J, Kampschroer B. Fluorinated pyrimidines. XXIV. In vivo metabolism of 5-trifluoromethyluracil-2-C-14 and 5-trifluoromethyl-2’-deoxyuridine-2-C-14. Cancer Res. 1965; 25: 377-81.
19. Oguchi K, Sakamoto K, Kazuno H et al. TAS-102 treatment results in high trifluridine incorporation into DNA with pyrimidine metabolic pathway markedly up-regulated in cancer. Eur J Cancer. 2014; 50(suppl. 6): Abstract 27.
20. Suzuki N, Emura T, Fukushima M. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011; 39: 263-70.
21. Suzuki N, Emura T, Fukushima M. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011; 39: 263-70.
22. Moghaddam A, Zhang HT, Fan TP et al. Thymidine phosphorylase is angiogenic and promotes tumour growth. Proc Natl Acad Sci USA. 1995; 92: 998-1002.
23. Hotchkiss KA, Ashton AW, Schwartz EL. Thymidine phosphorylase and 2-deoxyribose stimulate human endothelial cell migration by specific activation of the integrins alpha 5 beta 1 and alpha V beta 3. J Biol Chem. 2003; 278: 19272-9.
24. Takao S, Akiyama SI, Nakajo A et al. Suppression of metastasis by thymidine phosphorylase inhibitor. Cancer Res. 2000; 60: 5345-8.
25. Matsushita S, Nitanda T, Furukawa T et al. The effect of a thymidine phosphorylase inhibitor on angiogenesis and apoptosis in tumors. Cancer Res. 1999; 59: 1911-6.
26. Dexter DL, Wolberg WH, Ansfield FJ et al. The clinical pharmacology of 5-trifluoromethyl-2’-deoxyuridine. Cancer Res. 1972; 32: 247-53.
27. Emura T, Suzuki N, Fujioka A et al. Potentiation of the antitumor activity of alpha, alpha, alpha-trifluorothymidine by the co-administration of an inhibitor of thymidine phosphorylase at a suitable molar ratio in vivo. Int J Oncol. 2005; 27: 449-55.
28. Fukushima M, Suzuki N, Emura T et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of a ntitumor 2’-deoxyribonucleosides. Biochem Pharmacol. 2000; 59: 1227-36.
29. Yoshino T, Mizunuma N, Yamazaki K et al. TAS-102 monotherapy for pretreated metastatic colorectal cancer: a double-blind, randomised, placebo-controlled Phase 2 trial. Lancet Oncol. 2012; 13(10): 993-1001.
30. Mayer RJ, Van Cutsem E, Falcone A et al. Randomized trial of TAS-102 for refractory metastatic colorectal cancer. N Engl J Med. 2015; 372(20): 1909-19.
31. Van Cutsem E, Mayer RJ, Laurent S et al. The subgroups of the Phase III RECOURSE trial of trifluridine/tipiracil (TAS-102) versus placebo with best supportive care in patients with metastatic colorectal cancer. Eur J Cancer. 2018; 90: 63-72.
32. Xu J, Kim TW, Shen L et al. Results of a randomized, double-blind, placebo-controlled, Phase III trial of trifluridine/tipiracil (TAS-102) monotherapy in Asian patients With previously treated metastatic colorectal cancer: the TERRA study. J Clin Oncol. 2018; 36(4): 350-8.
33. Kwakman JJM, Vink G, Vestjens JH et al. Feasibility and effectiveness of trifluridine/tipiracil in metastatic colorectal cancer: real-life data from The Netherlands. Int J Clin Oncol. 2018; 23:482-9.
34. Cremolini C, Rossini D, Martinelli E et al. Trifluridine/tipiracil (TAS-102) in refractory metastatic colorectal cancer: a multicenter register in the frame of the Italian compassionate use program. Oncologist. 2018; 23:1178-87.
35. Pietrantonio F, Miceli R, Rimassa L et al. Estimating 12-week death probability in patients with refractory metastatic colorectal cancer: The Colon Life nomogram. Ann Oncol. 2017; 28: 555-61.
36. Cremolini C, Rossini D, Martinelli E et al. Trifluridine/tipiracil (TAS-102) in refractory metastatic colorectal cancer: a multicenter register in the frame of the Italian compassionate use program. Oncologist. 2018; 23: 1178-87.