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Antimetabolites
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Tegafur (UftoralTM) is a prodrug of 5-fluorouracil in which a tetrahydro-2-furyl moiety is joined to the N1-position of 5-FU (Figure 3.11). It was patented in 1967 and approved for use in cancer treatment in 1972. Tegafur is often given in combination with agents that modify its bioavailability and toxicity, such as gimeracil, oteracil, or uracil (Figure 3.11). Gimeracil and uracil work by inhibiting the enzyme dihydropyrimidine dehydrogenase (DPD), which is responsible for metabolizing fluoropyrimidines such as tegafur, 5-fluorouracil, and capecitabine, thereby reducing their degradation in the body and maintaining plasma and tissue levels. Oteracil inhibits the enzyme phosphoribosyl transferase, thus decreasing the activity of fluorouracil in normal gastrointestinal mucosa and reducing potential toxicity to this tissue.
Body-on-a-Chip for Pharmacology and Toxicology
Published in Brian J. Lukey, James A. Romano, Salem Harry, Chemical Warfare Agents, 2019
Anthony Atala, Mahesh Devarasetty, Steven. D. Forsythe, Russell. M. Dorsey, Harry Salem, Thomas. D. Shupe, Aleksander Skardal, Shay Soker
Platforms to test the toxicity of chemotherapeutic drugs used liver organoids in combination with tumor cells. A microfluidic system containing the hepatic cell line HepG2, colon carcinoma cells (HCT116), and myeloblasts (Kasumi-1) was used to test whether Tegafur, an oral pro-drug of the chemotherapeutic drug 5-fluorouracil (5-FU), can be metabolized by the liver organoids (Sung and Shuler, 2009). Tegafur has better bioavailability than 5-FU due to rapid enzymatic degradation of 5-FU (Malet-Martino and Martino, 2002). The body-on-a-chip system was able to reproduce the metabolism of Tegafur to 5-FU in the liver organoids, and it was carried by the microfluidic system to the cancer cells, where it induced cytotoxicity. In contrast, when Tegafur was added directly to the cancer cells, it did not have the same effect, because it was not converted to 5-FU.
Drug-induced hyperpigmention
Published in Dimitris Rigopoulos, Alexander C. Katoulis, Hyperpigmentation, 2017
Hairs, nails, and/or mucous membrane may also be involved, with some distinctive aspects, such as dyschromia of the glans penis, during tegafur treatment course. Tegafur is a chemotherapeutic fluorouracil prodrug used in the treatment of cancers. Dyschromia of the tongue and oral mucosa during use of fluorouracil, doxorubicin, cisplatin, and hydroxyurea (hydroxycarbamide). Dyschromia of hairs occurs during treatment course with cisplatin and methotrexate. Nails may be affected by many agents, including cisplatin, doxorubicin, idarubicin,47 and fluorouracil.48 Bleomycin, docetaxel, dacarbazine, and hydroxyurea can cause dispigmentation of the nails with longitudinal or transverse pigmented bands or diffuse nail pigmentation, sometimes coexisting with leukonychia or even onycholysis in case of docetaxel.
Comparisons of effects of SOX and mFOLFOX6 chemotherapy regimens on patients with locally advanced gastric cancer
Published in Journal of Chemotherapy, 2022
Gui-dong Chen, Bin-xiao Cao, Ying Shi, Jie-min Lv, Dong-hai Wang, Lun-bo Shi
This study showed that the clinical efficacy of the two chemotherapy regimens was comparable for locally advanced gastric cancer, and the proportion of patients who reached complete or partial remission, responses of neoadjuvant chemotherapy and type of resection showed no significant differences between two groups. The Teggio capsule is an oral compound preparation constitute of tegafur, gimeracil and oteracil potassium. Tegafur was a precursor of 5-fluorouracil, it can gradually become 5-fluorouracil in vivo after orally intaking, that will generate anti-tumour effect similar as 5-fluorouracil for locally advanced gastric cancer with lower incidence of gastrointestinal adverse reactions. Moreover, gimeracil can inhibit the activity of dihydropyrimidine dehydrogenase, increase the concentration and prolonged the retention time of 5-fluorouracil in plasma. As a biologically activated regulator, oteracil potassium has a benefit for reducing the gastrointestinal toxicity [26]. In this study, the incidence of abdominal pain, diarrhoea, nausea and vomiting in the observation group were obviously lower than those in the control group. The lower gastrointestinal adverse reactions may correlated with above mechanisms of Teggio capsule.
Predictors of early progression after curative resection followed by platinum-based adjuvant chemoradiotherapy in oral cavity squamous cell carcinoma
Published in Postgraduate Medicine, 2021
Hsueh-Ju Lu, Szu-Wen Tseng, Chih-Yu Peng, Hsien-Chun Tseng, Chung-Han Hsin, Hsin-Lin Chen, Wei-Shiou Huang, Ming-Fang Wu, Muh-Hwa Yang, Peter Mu-Hsin Chang
During radiation, chemotherapy with cisplatin 25 mg/m2 per week (day 1) plus daily oral tegafur-uracil (2 capsules twice per day, days 1–7) and cisplatin 30 mg/m2 per week (day 1) was concurrently administered in the training and validation cohorts, respectively; seven cycles of chemotherapy were scheduled until the completion of radiotherapy. Although triweekly high-dose cisplatin has been recommended as the standard for adjuvant CRT in high-risk OCSCC, severe adverse effects of this regimen cause low compliance, and only half of the enrolled patients are able to complete the treatment course [3,4]. The use of adjusted weekly low-dose cisplatin has therefore been widely discussed. In the adjuvant setting, the superiority of triweekly high-dose cisplatin over weekly low-dose cisplatin in terms of survival has been controversial, as the PFS and OS between both groups were found to be similar [15–17]. Fesneau et al. and our previous studies also showed that adjusted weekly cisplatin-based regimens, such as weekly cisplatin plus daily oral tegafur-uracil, provided good efficacy, compliance, and less toxicity in clinical practice, especially for those without an intravenous catheter [6,18]. The use of oral tegafur-uracil as a radiosensitizer enhanced antitumor activity, and avoided the complications of continuous 5-FU infusions.
The effect of postoperative gemcitabine on overall survival in patients with resected pancreatic cancer: A nationwide population-based Danish register study
Published in Acta Oncologica, 2019
Louise Skau Rasmussen, Benny Vittrup, Morten Ladekarl, Per Pfeiffer, Mette Karen Yilmaz, Laurids Østergaard Poulsen, Kell Østerlind, Carsten Palnæs Hansen, Michael Bau Mortensen, Frank Viborg Mortensen, Mogens Sall, Sönke Detlefsen, Martin Bøgsted, Claus Wilki Fristrup
Improvements in the effects of adjuvant chemotherapy in PC have been reported recently. Significantly prolonged mOS was shown for combined treatment with gemcitabine and capecitabine compared to gemcitabine monotherapy (28 versus 25 months, respectively) [30]. An impressive treatment effect with modified FOLFIRINOX compared to gemcitabine showed an increased mOS of 54.4 versus 35 months, respectively [15]. Tegafur/gimeracil/oteracil (S-1) compared to gemcitabine has also shown an increased mOS of 45.5 versus 25.5 months, respectively, in Japanese patients [39]. Adjuvant therapy with the combination of gemcitabine and capecitabine was implemented in Denmark in autumn 2016 and then with modified FOLFIRINOX in autumn 2018. Combination chemotherapy improves clinical outcomes but worsens side effects, making the selection of patients with a good PS necessary [15]. Obviously, there will still be a subgroup of patients who can only be offered gemcitabine monotherapy. In light of the new standard therapies, the results of the present study will be useful as a clinical reference in the future for comparing the OS in unselected PC patients receiving new adjuvant combination chemotherapy regimens. Danish national real-time register data will be available in the DPCD during the next three years.