How to optimize the effect of 5-fluorouracil modulated therapy in advanced colorectal cancer

Synthesis and Evaluation of N-acyl-2-(5-Fluorouracil-1-yl)-d,l-Glycine as a Colon-Specific Prodrug of 5-Fluorouracil

“…5‐Fluorouracil (5‐FU) has been used for varieties of cancers including colorectal cancer 15. It is administered parenterally because oral administration of the drug shows low and variable bioavailability due to the incomplete absorption and marked bioinactivation by dihydrouracil dehydrogenase in the liver and the mucosal membrane of the gastrointestinal tract 16.…”

Synthesis and Antitumor Activity of Amino Acid Ester Derivatives Containing 5-Fluorouracil

“…5-Fluorouracil (5-FU) is an antimetabolite of the pyrimidine analogue type, which is frequently used for treating solid tumors, such as colorectal, gastric tract, and liver carcinomas [ 1 , 2 , 3 ]. However, the clinical applications of 5-FU are greatly limited by its short plasma half-life, poor tumor affinity, myelosuppression, and strong intestinal toxicity.…”