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. Author manuscript; available in PMC: 2023 Jul 24.
Published in final edited form as: Trends Pharmacol Sci. 2023 Feb 23;44(4):222–236. doi: 10.1016/j.tips.2023.01.003

Table 1.

Therapies used for metastatic colorectal cancer

Systemic chemotherapy
Drug Mechanism of
action		 Year of
FDA
approval
for CRC		 Use in mCRC Ref
Fluorouracil (5-FU) Inhibits formation of thymidylate from uracil 1962 All lines of therapy [97]
Irinotecan Hydrochloride Topoisomerase I inhibitor 1996 All lines of therapy [97]
Oxaliplatin Forms intrastrand DNA adducts 2002 All lines of therapy [97]
Capecitabine Pro-drug of 5-FU; inhibits formation of thymidylate from uracil 2005 All lines of therapy [97]
Trifluridine + Tipiracil (TAS-102) Nucleoside analog + thymidine phosphorylase inhibitor 2015 Third-line therapy or beyond [98]
Targeted therapy
Bevacizumab VEGF inhibitor 2004 Any line of therapy in combination with 5-FU, irinotecan, and/or oxaliplatin [2]
Cetuximab EGFR inhibitor 2004 In EGFR mutant, RAS/RAF wild-type cancers; any line of therapy in combination with 5-FU, irinotecan, and/or oxaliplatin [2]
Panitumumab EGFR inhibitor 2006 In EGFR mutant, RAS/RAF wild-type cancers; any line of therapy in combination with 5-FU, irinotecan, and/or oxaliplatin [2]
Regorafenib Multi-kinase inhibitor 2012 Second-line therapy or beyond [2]
Aflibercept VEGF-A, VEGF-B, PIGF inhibitor 2012 Second-line therapy or beyond in combination with irinotecan-based regimens [2]
Ramucirumab VEGFR2 inhibitor 2015 Second-line therapy or beyond in combination with irinotecan-based regimens [2]
Encorafenib BRAF inhibitor 2020 In BRAFV600E mutant cancers; second-line therapy in combination with cetuximab [2]
Immunotherapy
Nivolumab PD-1 inhibitor 2017 In MSIhigh or dMMR cancers [65]
Ipilimumab CTLA-4 inhibitor 2018 In MSIhigh or dMMR cancers; in combination with nivolumab [65]
Pembrolizumab PD-1 inhibitor 2020 In MSIhigh or dMMR cancers [99]
a

Abbreviations: FDA, Food and Drug Administration; mCRC, metastatic colorectal cancer; VEGF, vascular endothelial growth factor; EGFR, epidermal growth factor receptor; PIGF, placental growth factor; VEGFR2, VEGF receptor 2; PD-1, programmed death protein 1; CTLA-4, cytotoxic T-lymphocyte-associated protein 4.