Drug intelligence / Profile preview

5-fluorouracil + hydroxyurea

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen of two cytotoxic small molecule chemotherapeutic agents, 5-fluorouracil (5-FU) and hydroxyurea. Both drugs are antineoplastic agents with distinct but complementary mechanisms of action. 5-fluorouracil is a pyrimidine analog that inhibits thymidylate synthase, thereby disrupting DNA synthesis and repair. Hydroxyurea inhibits ribonucleotide reductase, reducing the conversion of ribonucleotides to deoxyribonucleotides and further impairing DNA synthesis. The combination has demonstrated synergistic activity in vitro and in clinical settings for certain cancers—most notably head and neck cancer—where both drugs also act as radiosensitizers when used alongside radiotherapy[1][3][4]. This regimen has been investigated primarily for poor-prognosis or advanced head and neck cancers as well as metastatic gastrointestinal malignancies[1][2]. The combination may be administered sequentially or concurrently; dosing regimens vary depending on indication and protocol.

Other names
5-FU + hydroxyureafluorouracil + hydroxyureaHU + 5-FU
02

Targets

RNR (Ribonucleotide reductase)TS (Thymidylate synthase)

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