Levofolinate and
fluorouracil regimen (l-
leucovorin and
5 fluorouracil regimen) is a biochemical modulation of
5 fluorouracil (
5FU) by
leucovorin (LV). In the USA and Europe d,l-LV and
5FU regimen is frequently administered for
colorectal cancer treatment and recognized as the standard regimen. In Japan, multi-institutional clinical trials of l-
leucovorin (l-LV), a bioactive diastereomer of
leucovorin, and
5FU combination were conducted for the treatment of advanced
gastrointestinal cancer with comparable results to the US/Europe data. This l-LV and
5FU regimen was approved in August 1999 for the indications of advanced
gastric cancer and
colorectal cancer. The dosage and administration is referred to the weekly method developed at RPMI. Recently, the
irinotecan (CPT-11) or oxariplatin plus LV and
5FU combination showed higher antitumor activities than the LV and
5FU combination with increased progression-free survival. These regimens, however, are not yet properly established because clinical trial results with Japanese patients are not completed for agreement of the dosage and administration schedule. For the l-LV and
5FU regimen
diarrhea and
leukocytopenia, including grade 3 and higher, were reported as the major adverse events. Administration for eligible patients with periodical monitoring of diagnostic data is necessary.