Tegafur — a Review of Pharmacology and Toxicology

Brade, W.; Herdrich, K.

doi:10.1159/000407948

Cited by 10 publications

(6 citation statements)

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“…Tegafur is an established drug that has been used in Japan as an oral pro-drug to treat metastatic gastrointestinal cancer [193,194] and, since 1991, as adjuvant therapy [195]. Adding uracil to tegafur increased antitumor activity [196], which led to the development of an oral compound containing tegafur and uracil in a molar ratio of 1:4 (UFT).…”

Section: Uracil-tegafurmentioning

confidence: 99%

Monotherapy of Metastatic Breast Cancer: A Review of Newer Agents

Vogel

Nabholtz

1999

The Oncologist

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Key Words. Breast neoplasms · Docetaxel · Paclitaxel · Vinorelbine · Review ABSTRACT Purpose. New agents for the palliative treatment of metastatic breast cancer have emerged in the 1990s. This review summarizes the response rates of these agents with an emphasis on recent findings, such as presentations from the 1998 Meeting of the American Society of Clinical Oncology. Methods. The English medical literature was reviewed to identify clinical trials involving monotherapy for the treatment of metastatic breast cancer. Three agents-paclitaxel, vinorelbine, and docetaxel-are emphasized because their databases are extensive enough to allow interesting comparisons. Liposomal-encapsulated anthracyclines, losoxantrone, gemcitabine, oral surrogates of continuous-infusion fluorouracil, raltitrexed, LY 231514, edatrexate, topoisomerase I inhibitors, and trastuzumab are reviewed briefly.Results. Many of the new agents produce response rates approaching or even surpassing those achievable with doxorubicin monotherapy. Compared with older agents, some new agents have improved or at least different safety profiles, and some are easier to administer.Discussion and conclusions. The new agents offer useful therapeutic options that make them suitable for combining with each other and with older agents, which could result in more effective regimens for metastatic disease, and, ultimately, primary disease in the adjuvant setting. The chemotherapeutic paradigms governing the management of breast cancer for the past three decades are likely to change as we move into the 21st century.

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Section: Uracil-tegafurmentioning

confidence: 99%

Monotherapy of Metastatic Breast Cancer: A Review of Newer Agents

Vogel

Nabholtz

1999

The Oncologist

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“…Our goal was to define the relative stability of the N(1) and N(3) anions of 5FU as well as their concentration ratios in solution at various pH levels. The technique of the quantitative analysis of the condensed phase was tested on a model compound, 1‐(tetrahydrofuranyl‐2)‐5‐fluoro‐pyrimidinedione‐2,4 (tegafur, THF‐5FU), which was widely used as an anticancer drug in which the proton on N(1) to position was replaced by tetrahydrofuran group.…”

Section: Introductionmentioning

confidence: 99%

5-Fluorouracil solutions: NMR study of acid-base equilibrium in water and DMSO

Abdrakhimova

Ovchinnikov

Лобов

et al. 2014

J. Phys. Org. Chem.

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A comprehensive analysis of solutions of 5‐fluorouracil (5FU) in water and an organic medium (dimethylsulfoxide, DMSO) was carried out using quantum chemical methods and nuclear magnetic resonance (NMR) spectroscopy. The details of anionic form generation in the solution of 5FU with an equimolar amount of potassium hydroxide were studied by 13С, 1Н, 15N and 19F NMR. Interpretation of NMR spectral data was carried out using quantum chemical calculations at the TPSSTPSS/6‐311+G(d,p) level of theory. Specific solvation of 5FU and 1THF‐5FU was modeled in approximation using the five‐water cluster model and solvate complex including two DMSO molecules. It was established that in an alkaline medium in DMSO 5FU occurred mainly as a type of an anion with a deprotonation on N(1) position of a pyrimidine ring whereas in water alkaline solution—as a mixture of two anions with a deprotonation on N(1) and N(3) positions with a predominant content of the latter form. For the quantitative definition of the deprotonation forms of 5FU the technique based on the data of theoretical and experimental NMR 13C spectroscopy, tested on a model compound 1‐(tetrahydrofuranyl‐2)‐5‐fluoro‐pyrimidinedione‐2,4 (tegafur, THF‐5FU), was offered. The N(3) anion was found from spectral data to be more thermodynamically stable than the N(1) anion by 2.40 kJ mol−1 (calculated value 2.24 kJ mol−1) in an alkaline–water solution. Both alkaline–water and alkaline–DMSO solutions of THF‐5FU (THF‐5FU/KOH = 1/1) were characterized by the ratio of the equilibrium concentrations of the anion and diketo‐tautomer as 9:1 and 4.3:1, respectively. Copyright © 2014 John Wiley & Sons, Ltd.

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“…Tegafur (TG) is a highly lipophilic prodrug that is slowly metabolized into 5-FU in vivo 2 and has practically complete oral bioavailability, with a serum half-life of 10 hours. 2 Phase I studies recommend a 1 g/m 2 /day dose by continuous oral administration, with diarrhea being the toxic limitation of the dose. 2 In controlled studies, TG achieved response rates, mean duration of response, and survival similar to intravenous 5-FU in patients with advanced colorectal carcinoma.…”

mentioning

confidence: 99%

“…2 Phase I studies recommend a 1 g/m 2 /day dose by continuous oral administration, with diarrhea being the toxic limitation of the dose. 2 In controlled studies, TG achieved response rates, mean duration of response, and survival similar to intravenous 5-FU in patients with advanced colorectal carcinoma. [3][4][5] Protracted administration of oral TG comes closest to reproducing the pharmacokinetics of true 5-FU infusions.…”

mentioning

confidence: 99%