Fluorouracil (Systemic)

Class: Antineoplastic Agents
VA Class: AN300
Chemical Name: 5-fluoro-2,4(1H,3H)-Pyrimidinedione
Molecular Formula: C₄H₃FN₂O₂
CAS Number: 51-21-8
Brands: Adrucil

Medically reviewed by Drugs.com on Jul 26, 2021. Written by ASHP.

Introduction

Pyrimidine antagonist; antimetabolite; antineoplastic agent.

Uses for Fluorouracil (Systemic)

Cancers

Treatment of adenocarcinoma of the colon, rectum, breast, stomach, and pancreas.

Adjunct to surgery for the treatment of various solid tumors (e.g., adenocarcinoma of the colon, rectal carcinoma).

Colorectal Cancer

Drug of choice (combined with leucovorin or levoleucovorin and other drugs [e.g., irinotecan, oxaliplatin]) for advanced colorectal cancer in the adjuvant or metastatic setting.

Doublet regimens (i.e., fluorouracil, oxaliplatin, and leucovorin or levoleucovorin [FOLFOX]; fluorouracil, irinotecan, and leucovorin or levoleucovorin [FOLFIRI]; capecitabine and oxaliplatin [CapeOx; CapOx]) are the current standard of care for the adjuvant or palliative treatment of advanced colorectal cancer.

Fluorouracil combined with leucovorin or levoleucovorin is an acceptable treatment option in limited-resource settings or in patients unable to tolerate a doublet regimen.

Weekly schedule of fluorouracil/leucovorin (high-dose leucovorin or Roswell Park regimen) has equal efficacy as monthly schedule (low-dose or Mayo Clinic schedule), but the weekly schedule is a preferred regimen for adjuvant therapy because of ease of use and less toxicity. (See Colorectal Cancer under Dosage and Administration.)

Bimonthly, continuous IV infusion schedule of fluorouracil/leucovorin (LV5FU2 or deGramont regimen) also evaluated as adjuvant therapy and shown to be safer than direct IV injection regimen of these drugs. Simplified version of this regimen also evaluated. (See Colorectal Cancer under Dosage and Administration.)

Role of regional adjuvant therapy (e.g., p...