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Original Article

5-Fluorouracil Pharmacokinetics: Causes for Variability and Strategies for Modulation in Cancer Chemotherapy

New Drugs

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Pages 494-506 | Published online: 11 Jun 2009

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Pei-Jian Peng, Hua Cheng, Xue-Qing Ou, Lin-Juan Zeng, Xuan Wu, Yu-Meng Liu, Zhong Lin, Yan-Na Tang, Si-Yang Wang, Hong-Yu Zhang & Zhi-Bin Chen. (2014) Safety and efficacy of S-1 chemotherapy in recurrent and metastatic nasopharyngeal carcinoma patients after failure of platinum-based chemotherapy: multi-institutional retrospective analysis. Drug Design, Development and Therapy 8, pages 1083-1087.
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Muhammad Wasif Saif, Kostas N Syrigos & Nikos A Katirtzoglou. (2009) S-1: a promising new oral fluoropyrimidine derivative. Expert Opinion on Investigational Drugs 18:3, pages 335-348.
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Hedy L Kindler & Richard L Schilsky. (2000) Eniluracil: an irreversible inhibitor of dihydropyrimidine dehydrogenase. Expert Opinion on Investigational Drugs 9:7, pages 1635-1649.
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Jacob Lokich. (1999) Pharmacokinetic Modulation of 5-Fluorouracil: Emulating Continuous Infusion?. Cancer Investigation 17:7, pages 543-544.
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Articles from other publishers (26)

Mengya Zang, Xiaoyun Hu, Guosheng Yuan, Rong Li, Wenli Li, Huajin Pang, Qi Li & Jinzhang Chen. (2023) Tyrosine kinase inhibitors, immune checkpoint inhibitors combined with hepatic arterial infusion of oxaliplatin and raltitrexed versus oxaliplatin, 5-fluorouracil and leucovorin for intermediate and advanced hepatocellular carcinoma: A retrospective study. International Immunopharmacology 125, pages 111019.
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Himanshu Verma, Gera Narendra, Baddipadige Raju, Pankaj Kumar Singh & Om Silakari. (2022) Dihydropyrimidine Dehydrogenase-Mediated Resistance to 5-Fluorouracil: Mechanistic Investigation and Solution. ACS Pharmacology & Translational Science 5:11, pages 1017-1033.
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Jaffer A. Ajani, Milind Javle, Cathy Eng, David Fogelman, Jackie Smith, Barry Anderson, Chun Zhang & Kenzo Iizuka. (2020) Phase I study of DFP-11207, a novel oral fluoropyrimidine with reasonable AUC and low Cmax and improved tolerability, in patients with solid tumors. Investigational New Drugs 38:6, pages 1763-1773.
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Bee Koon Gan, Kamal Rullah, Chean Yeah Yong, Kok Lian Ho, Abdul Rahman Omar, Noorjahan Banu Alitheen & Wen Siang Tan. (2020) Targeted delivery of 5-fluorouracil-1-acetic acid (5-FA) to cancer cells overexpressing epithelial growth factor receptor (EGFR) using virus-like nanoparticles. Scientific Reports 10:1.
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Shiguang Chen, Kongzhi Zhang, Weifu Liu & Wenchang Yu. (2020) Hepatic arterial infusion of oxaliplatin plus raltitrexed in patients with intermediate and advanced stage hepatocellular carcinoma: A phase II, single-arm, prospective study. European Journal of Cancer 134, pages 90-98.
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Luis Correia Pinheiro, Julie Durand & Jean‐Michel Dogné. (2020) An Application of Machine Learning in Pharmacovigilance: Estimating Likely Patient Genotype From Phenotypical Manifestations of Fluoropyrimidine Toxicity. Clinical Pharmacology & Therapeutics 107:4, pages 944-947.
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Yan Liu, Dongyang Zhao, Mengchi Sun, Wei Wei, Yingli Wang, Jiahua Zhou, Ruoshi Zhang, Jian Wang, Haotian Zhang, Zhonggui He, Qiming Kan & Jin Sun. (2018) Covalently mucoadhesive amphiphilic prodrug of 5-fluorouracil for enhanced permeation and improved oral absorption. Drug Delivery and Translational Research 8:3, pages 645-656.
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Sibylle Schirm, Christoph Engel, Sibylle Loibl, Markus Loeffler & Markus Scholz. (2017) Model-based optimization of G-CSF treatment during cytotoxic chemotherapy. Journal of Cancer Research and Clinical Oncology 144:2, pages 343-358.
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Man Li, Zhen Liang, Xun Sun, Tao Gong & Zhirong Zhang. (2014) A Polymeric Prodrug of 5-Fluorouracil-1-Acetic Acid Using a Multi-Hydroxyl Polyethylene Glycol Derivative as the Drug Carrier. PLoS ONE 9:11, pages e112888.
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Wei‐Bin Shi, Van‐Minh Le, Chun‐Hua Gu, Yuan‐Hong Zheng, Mei‐Dong Lang, Yan‐Hua Lu & Jian‐Wen Liu. (2014) Overcoming Multidrug Resistance in 2D and 3D Culture Models by Controlled Drug Chitosan‐Graft Poly(Caprolactone)‐Based Nanoparticles. Journal of Pharmaceutical Sciences 103:4, pages 1064-1074.
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William H. FissellIVIV & Marc Earl. 2014. Renal Disease in Cancer Patients. Renal Disease in Cancer Patients 251 269 .
Max E. Scheulen, Kaku Saito, Ralf A. Hilger, Bastian Mende, Christopher Zergebel & Dirk Strumberg. (2011) Effect of food and a proton pump inhibitor on the pharmacokinetics of S-1 following oral administration of S-1 in patients with advanced solid tumors. Cancer Chemotherapy and Pharmacology 69:3, pages 753-761.
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Zengpei Dou, Yingying Xu, Hongfang Sun & Yuanfang Liu. (2012) Synthesis of PEGylated fullerene–5-fluorouracil conjugates to enhance the antitumor effect of 5-fluorouracil. Nanoscale 4:15, pages 4624.
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B Glimelius, H Garmo, Å Berglund, L A Fredriksson, M Berglund, H Kohnke, P Byström, H Sørbye & M Wadelius. (2010) Prediction of irinotecan and 5-fluorouracil toxicity and response in patients with advanced colorectal cancer. The Pharmacogenomics Journal 11:1, pages 61-71.
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N. Janus, J. Thariat, H. Boulanger, G. Deray & V. Launay-Vacher. (2010) Proposal for dosage adjustment and timing of chemotherapy in hemodialyzed patients. Annals of Oncology 21:7, pages 1395-1403.
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Y.F. LI, S. FU, W. HU, J.H. LIU, K.W. FINKEL, D.M. GERSHENSON & J.J. KAVANAGH. (2007) Systemic anticancer therapy in gynecological cancer patients with renal dysfunction. International Journal of Gynecological Cancer 17:4, pages 739-763.
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Naruto Taira, Kenjiro Aogi, Shozo Ohsumi, Shigemitsu Takashima, Rieko Nishimura, Hiroyoshi Doihara & Toshiaki Saeki. (2006) S-1 (TS-1) maintained complete response for approximately 10 years in a case of metastatic breast cancer. Breast Cancer 13:2, pages 220-224.
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R. Goel, E. Chouinard, D. J. Stewart, S. Huan, H. Hirte, S. Stafford, B. Waterfield, J. Roach, C. Lathia, V. Agarwal, R. Humphrey, W. Walsh, S. Matthews & L. Seymour. (2005) An NCIC CTG phase I/pharmacokinetic study of the matrix metalloproteinase and angiogenesis inhibitor BAY 12-9566 in combination with 5-fluorouracil/leucovorin. Investigational New Drugs 23:1, pages 63-71.
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Yukito Ichinose, Kozo Yoshimori, Hiroshi Sakai, Yushi Nakai, Takahiko Sugiura, Masaaki Kawahara & Hisanobu Niitani. (2004) S-1 Plus Cisplatin Combination Chemotherapy in Patients with Advanced Non–Small Cell Lung Cancer. Clinical Cancer Research 10:23, pages 7860-7864.
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Stuart M. Lichtman, J.Andrew Skirvin & Sunitha Vemulapalli. (2003) Pharmacology of antineoplastic agents in older cancer patients. Critical Reviews in Oncology/Hematology 46:2, pages 101-114.
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Veena John, Sandeep Mashru & Stuart M Lichtman. (2003) Pharmacological Factors Influencing Anticancer Drug Selection in the Elderly. Drugs & Aging 20:10, pages 737-759.
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Richard F. Branda, Zhuan Chen, Elice M. Brooks, Shelly J. Naud, Thomas D. Trainer & John J. McCormack. (2002) Diet modulates the toxicity of cancer chemotherapy in rats. Journal of Laboratory and Clinical Medicine 140:5, pages 358-368.
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M. Malet-Martino & R. Martino. (2002) Clinical Studies of Three Oral Prodrugs of 5-Fluorouracil (Capecitabine, UFT, S-1): A Review. The Oncologist 7:4, pages 288-323.
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J. Andrew Skirvin & Stuart M. Lichtman. (2002) Pharmacokinetic Considerations of Oral Chemotherapy in Elderly Patients with Cancer. Drugs & Aging 19:1, pages 25-42.
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Cathy Eng, Hedy L. Kindler & Richard L. Schilsky. (2001) Oral Fluoropyrimidine Treatment of Colorectal Cancer. Clinical Colorectal Cancer 1:2, pages 95-103.
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