Overview

Generic Name(s):
fluorouracil and 5-fu
Trade Name(s):
Fluril, Cytosafe, Flurox, Flurablastin, Timazin, Fluroblastin, Efudex, Arumel, Actino-Hermal, Adrucil, Efurix, Fiverocil, Fluracil, Fluoroplex, Accusite, Fluracedyl, and Ribofluor
NCI Definition [1]:
An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions.

Biomarker-Directed Therapies

Fluorouracil has been investigated in 116 clinical trials, of which 103 are open and 13 are closed. Of the trials investigating fluorouracil, 3 are early phase 1 (3 open), 17 are phase 1 (13 open), 16 are phase 1/phase 2 (13 open), 47 are phase 2 (43 open), 5 are phase 2/phase 3 (5 open), 27 are phase 3 (26 open), and 1 is no phase specified (0 open).

ERBB2 Amplification, HER2 Overexpression, and HER2 Positive are the most frequent biomarker inclusion criteria for fluorouracil clinical trials.

Adenocarcinoma of the gastroesophageal junction, pancreatic adenocarcinoma, and gastric adenocarcinoma are the most common diseases being investigated in fluorouracil clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Fluorouracil
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Fluorouracil
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating fluorouracil and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
dermik brand of fluorouracil, fluorouracil®, 5 fluorouracil, fluouracil, 5-fluoropyrimidine-2,4-dione, roche brand of fluorouracil, fu, fluorouracil injection, teva brand of fluorouracil, fluorouracilum, dermatech brand of fluorouracil, 5-fu, 51-21-8, 5-fluoro-2,4(1h,3h)-pyrimidinedione, 5-fu topical, 5fluorouracil, 2,4-dioxo-5-fluoropyrimidine, 5-fluorouracil, icn brand of fluorouracil, flurodex, ro-2-9757, fluorouracil teva brand, 19893, 5-fluorouracil, 5-fu injection, fluorouracil [chemical/ingredient], 5fluracil, fluoruracil, 5-fluoro-2,4(1h,3h)-pyrimidinedione, fluorouracilo, fluorouracil (substance), 5fu, 2,4-dioxo-5-fluoropyrimidine, csp brand of fluorouracil, 5-fluoro-2,4(1h, 3h)-pyrimidinedione, fluorouracil (product), 5-fluorouracil injection, allergan brand of fluorouracil, 5-fluracil, fluoro uracil, fluoro uracile icn, 5-fluoracil, 5-fu, ro 2-9757, 5fu injection, fluouracil, fluorouracil, Fluroblastin, Flurox, Ribofluor, Timazin, fluorouracil, ribosepharm brand of fluorouracil, Fluril, Fluracil, Fluracedyl, Flurablastin, Fiverocil, Efurix, Cytosafe, Arumel, Actino-Hermal, AccuSite, Fluoroplex, Efudex, Adrucil, carac, 5fu - fluorouracil, 2,4(1h,3h)-pyrimidinedione, 5-fluoro-, fluoro-uracile icn
Drug Categories [2]:
Antimetabolites
NCIT ID [1]:
C505
SNOMED ID [1]:
F-61A3B

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.