A comprehensive review of 5-fluorouracil and leucovorin in patients with metastatic colorectal carcinoma

Cancer. 1997 Oct 1;80(7):1179-87. doi: 10.1002/(sici)1097-0142(19971001)80:7<1179::aid-cncr1>3.0.co;2-g.


Background: Colorectal carcinoma is the third leading cause of cancer-related death. The primary treatment for patients with metastatic colorectal carcinoma is systemic chemotherapy with 5-fluorouracil (5-FU) and leucovorin (LV), a biomodulator of 5-FU that has been shown to enhance its activity. Optimal dosing and administration strategies remain to be determined.

Methods: This article is a review of recent studies reporting on the use of high dose and low dose LV as a biomodulator of 5-FU in patients with advanced colorectal carcinoma.

Results: Studies of LV plus 5-FU demonstrated response rates of 7-58% in patients who had not received prior chemotherapy. A survival advantage was recorded in some trials. LV plus 5-FU produces mild and transient hematologic toxicity. The most common toxicities from LV plus 5-FU were gastrointestinal and schedule-dependent, but generally resolved within a few days.

Conclusions: The combination of LV and 5-FU provides a favorable treatment regimen for patients with metastatic colorectal carcinoma. Growing evidence suggests that altering the dose and schedule of both LV and 5-FU can impact positively on the response rate. However, controversy remains regarding the optimal dosing regimen. Therefore, continued study of LV plus 5-FU is urged and a favorable impact on survival is requisite before definitive conclusions are drawn, particularly in relation to LV dosage.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / pathology*
  • Drug Administration Schedule
  • Fluorouracil / administration & dosage*
  • Fluorouracil / adverse effects
  • Humans
  • Immunologic Factors / therapeutic use
  • Leucovorin / administration & dosage*
  • Leucovorin / adverse effects
  • Lymphatic Metastasis


  • Immunologic Factors
  • Leucovorin
  • Fluorouracil