From:  Exploratory proteomic and bioinformatics analysis unveils epitope pairing between IGHV3-64 and K-Ras for polyclonal drug conjugation in colorectal cancer

 Overview of FDA-approved chemotherapeutic agents used in colorectal cancer (CRC).

ChemotherapiesMechanisms and clinical use in CRC
Irinotecan (IRN)

  • Topoisomerase I inhibitor

  • Inhibits DNA replication and repair in rapidly dividing cancer cells → induces apoptosis

  • Used to overcome tumor resistance

Oxaliplatin (OXA)

  • Platinum-based agent

  • Forms DNA crosslinks → disrupts DNA synthesis and triggers apoptosis

  • Helps to improve survival outcomes, especially in combination regimens

5-Fluorouracil (5-FU)

  • Pyrimidine analog

  • Inhibits thymidylate synthase → disrupts DNA synthesis

  • Incorporates into RNA → interferes with RNA processing and function

  • Helps to enhance overall treatment efficacy

Leucovorin (LEU) (folinic acid)

  • Stabilizes 5-FU binding to thymidylate synthase → enhances 5-FU activity

  • Used to improve therapeutic response

Lonsurf (trifluridine-tipiracil) (FTD-TPI)

  • Trifluridine: nucleoside analog → inhibits DNA synthesis

  • Tipiracil: inhibits trifluridine degradation → increases its bioavailability

  • Used to extend survival in metastatic/refractory CRC

Capecitabine (CAP)

  • Oral prodrug of 5-FU

  • Activated in tumor tissue by thymidine phosphorylase

  • Designed to enhance the targeted efficacy of 5-FU

Return to article view

This table summarizes commonly used FDA-approved chemotherapies for CRC, highlighting their primary mechanisms of action and established clinical roles. These agents form the backbone of standard treatment regimens across different disease stages and are frequently used alone or in combination to improve therapeutic efficacy, overcome resistance, and extend patient survival.