Cardiotoxicity of commercial 5-fluorouracil vials stems from the alkaline hydrolysis of this drug

Laurent Lemaire 1, 2 Mc Malet-Martino M de Forni R. Martino 2 B Lasserre
1 MINT - Micro et Nanomédecines Translationnelles
2 IMRCP - Interactions moléculaires et réactivité chimique et photochimique
Abstract : The cardiotoxicity of 5-fluorouracil (FU) was attributed to impurities present in the injected vials. One of these impurities was identified as fluoroacetaldehyde which is metabolised by isolated perfused rabbit hearts into fluoroacetate (FAC), a highly cardiotoxic compound. FAC was also detected in the urine of patients treated with FU. These impurities were found to be degradation products of FU that are formed in the basic medium employed to dissolve this compound. To avoid chemical degradation of this antineoplastic drug, the solution of FU that will be injected should be prepared immediately before use.
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https://hal.univ-angers.fr/hal-02374741
Contributeur : Laurent Lemaire <>
Soumis le : jeudi 21 novembre 2019 - 16:17:25
Dernière modification le : vendredi 22 novembre 2019 - 01:36:54

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UNIV-ANGERS | UNIV-TLSE3 | INC-CNRS | CNRS

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Laurent Lemaire, Mc Malet-Martino, M de Forni, R. Martino, B Lasserre. Cardiotoxicity of commercial 5-fluorouracil vials stems from the alkaline hydrolysis of this drug. British Journal of Cancer, Cancer Research UK, 1992, 66 (1), pp.119-127. ⟨10.1038/bjc.1992.227⟩. ⟨hal-02374741⟩

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