5-Fluorouracil derivatives: a patent review (2012 – 2014)

Abstract

Although in the past few years there has been a great advancement in the antitumor effectiveness and selectivity of 5-FU-based therapies, it is envisaged that future approaches using 'omics' technologies that could determine the tumor heterogeneity may help in identifying additional candidate genes, microRNAs or cytokines involved in both the path mechanisms of 5-FU-related toxicity and its therapeutic efficacy. Moreover, the development of novel targeted 5-FU derivatives or 5-FU-based therapies tailored to individual patients opens up new possibilities in the improvement of the quality of life and survival for those suffering from this devastating disease.

Patient–doctor relationship and adherence to capecitabine in outpatients of a German comprehensive cancer center

“…1 Such protocols are regarded as crucial for the treatment of patients in the upcoming years. 2 – 4 5-FU, which is usually administered intravenously, typically causes various side effects common in drugs directed nonspecifically at fast growing cells. 5 The prodrug capecitabine, that converts to 5-FU within tumors, allowed to reduce the spectrum and magnitude of side effects.…”

New insights into frequency and contents of fear of cancer progression/recurrence (FOP/FCR) in outpatients with colorectal carcinoma (CRC) receiving oral capecitabine: a pilot study at a comprehensive cancer center

“…1 In fact, chemotherapy protocols based on 5-fluorouracil (5-FU; F. Hoffmann-La Roche AG, Basel, Switzerland) are expected to constitute the backbone of drug treatment for patients with CRC for the upcoming years. 4 – 6 Usually administered intravenously, 5-FU leads to a range of side effects typical for drugs acting non-specifically on fast growing cells. 7 With the prodrug capecitabine (Xeloda ® ; F. Hoffmann-La Roche AG) converting predominantly to 5-FU within tumors, not only the spectrum but also the magnitude of side effects could be reduced.…”

Evaluation of cardioprotective activity of Lepidium sativum seed powder in albino rats treated with 5-fluorouracil

“…The main mechanism of action is interfering with DNA synthesis and mRNA transcription. However, cardiotoxicity is one of the most important associated side effects resulting from its nonspecific cytotoxicity in cancer cells (Álvarez et al, 2012;Carrillo et al, 2015). Clinical cardiac toxicities associated with intravenous infusion of 5-FU covers a wide range of manifestations like angina, myocardial ischemia, congestive heart failure, myocardial infarction, pulmonary edema, and sudden death (Polk et al, 2014;Sorrentino et al, 2012;Tsavaris et al, 2002).…”