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5-Fluorouracil derivatives: a patent review

Álvarez, Pablo J. and Marchal Corrales, Juan Antonio and Boulaiz, Houria and Carrillo Delgado, Esmeralda Esperanza and Vélez, Celia and Rodríguez-Serrano, Fernando and Melguizo, Consolación and Prados Salazar, José Carlos and Madeddu, Roberto Beniamino and Aranega Jiménez, Antonia (2012) 5-Fluorouracil derivatives: a patent review. Expert Opinion on Therapeutic Patents, Vol. 22 (2), p. 107-123. eISSN 1744-7674. Article.

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DOI: 10.1517/13543776.2012.661413


Introduction: The fluorinated analog of uracil 5-FU is an antimetabolite, active against a wide range of solid tumors. The main mechanism of action consists in interfering with DNA synthesis and mRNA translation. However, patients treated with 5-FU display several side effects, a result of its nonspecific cytotoxicity for tumor cells. Numerous modifications of the 5-FU structure have been performed in order to overcome these disadvantages.
Areas covered: In this review, the metabolic pathways, pharmacokinetics and clinical pharmacology of 5-FU are briefly introduced. Moreover, several derivatives developed and patented, including oral 5-FU prodrugs and combinations with other active compounds, are presented. Finally, new innovative methods for administration and vehiculization of 5-FU and its derivatives are described.
Expert opinion: The search for less toxic 5-FU derivatives, which diminish or circumvent some of its disadvantages, has allowed the development of selective antitumor prodrugs and novel methods for tissue-specific drug delivery. Although some of these oral prodrugs are being used clinically, either alone or in combination therapy with other anticancer agents, it seems that the potential of personalized medicine, including pharmacogenomics and targeted therapy with novel 5-FU derivatives, will improve the management and clinical responses of patients treated with 5-FU-based therapy.

Item Type:Article
ID Code:7332
Uncontrolled Keywords:5-fluorouracil, nanomedicine, O,N-acetals, oral prodrugs, solid tumors, targeted therapy
Subjects:Area 05 - Scienze biologiche > BIO/17 Istologia
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Scienze Biomediche
Publisher:Informa Healthcare
Deposited On:05 Apr 2012 09:07

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