PURPOSE Gastrointestinal cancers frequently exhibit mutational activation of the Ras/MAPK pathway, which is implicated in resistance to ionizing radiation (IR) and chemotherapy. Concurrent radiotherapy and 5-fluorouracil (5-FU) based chemotherapy is commonly used for treatment of gastrointestinal malignancies. We previously reported radiosensitization with selumetinib, an inhibitor of MEK1/2. T...

Objective(s): The significant contribution of nanoparticles to cancer treatment has attracted therapeutic attention. The present study aimed to evaluate the synergistic effects of 5-fluorouracil (5-FU) and zinc oxide nanoparticles (ZnO NPs) as multimodal drug delivery on human breast cancer MCF-7 cells.Materials and Methods: In this in-vitro study, the impact of 5-FU and ZnO NPs in the sin...

Herein, 1F2, an anti-HER2 monoclonal antibody (mAb), was covalently coupled to the surface of 5-Fluorouracil (5-FU) loaded bovine serum albumin (BSA) nanoparticles. Concerning two different crosslinkers for conjugation of 1F2, Maleimide-poly (ethylene glycol)-Succinimidyl carbonate (Mal-PEG5000-NHS) was selected due to its higher conjugation efficiency (23±4 %) obtained in comparison to N-succi...

Herein, 1F2, an anti-HER2 monoclonal antibody (mAb), was covalently coupled to the surface of 5-Fluorouracil (5-FU) loaded bovine serum albumin (BSA) nanoparticles. Concerning two different crosslinkers for conjugation of 1F2, Maleimide-poly (ethylene glycol)-Succinimidyl carbonate (Mal-PEG5000-NHS) was selected due to its higher conjugation efficiency (23±4 %) obtained in comparison to N-succi...

JNCI | Review 1543 The fluoropyrimidine 5-fluorouracil (5-FU) has been used in daily clinical oncology practice for nearly 50 years, and it has been well established that a good correlation exists between 5-FU plasma levels and the biological effects of 5-FU treatment, both in terms of clinical efficacy and toxicity ( 1 – 6 ). Although 5-FU pharmacokinetic studies using cell-based and physical ...

BACKGROUND This study was performed to evaluate the pharmacokinetics, bioequivalence, and feasibility of a combined oral formulation of 5-flurouracil (5-FU) and eniluracil (Glaxo Wellcome Inc., Research Triangle Park, North Carolina), an inactivator of dihydropyrimidine dehydrogenase (DPD). The rationale for developing a combined eniluracil/5-FU formulation oral dosing form is to simplify treat...

5-fluoropyrimidine (2-HFP) were measured on Sarcoma 180 ascites cells. A marked extension of the life-span of tumor-bearing mice was afforded by i.p. injections of 5-FU, whereas both 4-HFP and 2-HFP were only weakly active. Sarcoma 180 ascites cells converted both 4-HFP and 5-FU into mono-, di-, and trinucleotide forms of 5-FU and incorporated the 5-fluoropyrimidines into RNA exclusively as 5-F...

Aims 5-FU is used as the main backbone of chemotherapy regimens for patients with colorectal and other gastrointestinal cancers. Despite development of new strategies that allowed enhancing clinical effectiveness and tolerability of 5-FU, 10-30% of patients treated with 5-FU-based regimens experience severe treatment-related toxicity. In our study, we evaluated the 5-FU exposure-toxicity relati...